ADRA2B

Summary

ADRA2B (adrenoceptor alpha 2B, HGNC:282) is a protein-coding gene on chromosome 2q11.2, encoding Alpha-2B adrenergic receptor (P18089). Alpha-2 adrenergic receptors are G protein-coupled receptors for catecholamines that activate G(i/o) protein pathway, thereby promoting adenylyl cyclase inhibition, ERK1/2 stimulation, and voltage-gated calcium channels suppression.

This intronless gene encodes a seven-pass transmembrane protein. This protein is a member of a subfamily of G protein-coupled receptors that regulate neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system.

Source: NCBI Gene 151 — RefSeq curated summary.

At a glance

• Gene–disease (curated): benign adult familial myoclonic epilepsy (Supportive, GenCC) — +3 more curated relationships
• GWAS associations: 1
• Clinical variants (ClinVar): 115 total — 10 pathogenic, 6 likely-pathogenic
• GTEx eGene: eQTL in 37 tissues, sQTL in 0 (q < 0.05)
• Phenotypes (HPO): 8
• Drug target: yes — 38 via a complex or family; 316 molecules with ChEMBL bioactivity (top 1% of genes corpus-wide)
• Approved drugs acting on a complex or family including it: 33 — Alseroxylon, Apraclonidine Hydrochloride, Brimonidine Tartrate, +30 more (Adrenergic receptor alpha; Adrenergic receptor alpha-2)
• Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 1.56 (unconstrained)
• MANE Select transcript: NM_000682
• Notable: 115 clinical variants but no curated precision-oncology (CIViC) evidence yet

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:282
Approved symbol	ADRA2B
Name	adrenoceptor alpha 2B
Location	2q11.2
Locus type	gene with protein product
Status	Approved
Aliases	ADRARL1
Ensembl gene	ENSG00000274286
Ensembl biotype	protein_coding
OMIM	104260
Entrez	151

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

MANE Select: ENST00000620793

ENST00000620793

RefSeq mRNA: 1 — MANE Select: NM_000682 NM_000682

CCDS: CCDS56129

Canonical transcript exons

ENST00000620793 — 1 exons

Exon	Start	End
ENSE00003744297	96112876	96116571

Expression profiles

Bgee: expression breadth ubiquitous, 147 present calls, max score 85.18.

FANTOM5 (CAGE): breadth broad, TPM avg 1.8198 / max 132.1735, expressed in 347 samples.

Highest expression (Bgee): apex of heart, tendon of biceps brachii, gastrocnemius, heart left ventricle, muscle of leg.

Genetic regulation across tissues (GTEx eQTL / sQTL)

ADRA2B is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 37 tissues and its splicing (sQTL) in 0 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

showing 20 of 37 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Artery Aorta	eqtl	2.4e-63	-0.86	2:96072837:G:C
Testis	eqtl	1.1e-48	+1.66	2:96082306:A:G
Thyroid	eqtl	1.6e-29	+0.50	2:96070820:T:C
Brain Cerebellar Hemisphere	eqtl	1.8e-26	-1.19	2:96072837:G:C
Brain Cerebellum	eqtl	1.5e-25	-1.12	2:96072837:G:C
Nerve Tibial	eqtl	8.6e-22	+0.45	2:96009511:G:A
Adipose Subcutaneous	eqtl	2.3e-20	+0.35	2:95892729:C:T
Esophagus Gastroesophageal Junction	eqtl	2.5e-17	+0.44	2:95935361:C:T
Adipose Visceral Omentum	eqtl	8.8e-17	+0.39	2:95814433:G:A
Esophagus Muscularis	eqtl	2.1e-15	+0.36	2:95892652:C:T
Colon Transverse	eqtl	2.5e-15	+0.32	2:95897125:C:A
Minor Salivary Gland	eqtl	7.7e-14	+1.75	2:96092356:C:T
Stomach	eqtl	5.4e-09	+0.32	2:95892729:C:T
Breast Mammary Tissue	eqtl	7.7e-08	+0.33	2:95758771:C:A
Muscle Skeletal	eqtl	8.9e-08	+0.27	2:95892598:C:T
Heart Left Ventricle	eqtl	1.7e-07	+0.23	2:95930962:G:C
Spleen	eqtl	4.4e-07	+0.48	2:96087401:G:A
Esophagus Mucosa	eqtl	1.0e-06	+0.61	2:95815543:C:T
Skin Sun Exposed Lower leg	eqtl	3.2e-06	+0.20	2:95834541:T:C
Colon Sigmoid	eqtl	3.5e-06	+0.27	2:96070820:T:C

FANTOM5 promoters

3 alternative TSS:

Promoter ID	TPM avg	Samples expressed
29701	0.6831	120
29703	0.6576	223
29702	0.4791	172

Top tissues by expression

showing 100 of 282 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
apex of heart	UBERON:0002098	85.18	gold quality
tendon of biceps brachii	UBERON:0008188	85.06	silver quality
gastrocnemius	UBERON:0001388	76.19	gold quality
heart left ventricle	UBERON:0002084	75.38	gold quality
muscle of leg	UBERON:0001383	75.34	gold quality
buccal mucosa cell	CL:0002336	74.95	gold quality
cardiac ventricle	UBERON:0002082	74.76	gold quality
right lobe of liver	UBERON:0001114	72.15	gold quality
spleen	UBERON:0002106	72.08	gold quality
type B pancreatic cell	CL:0000169	71.91	gold quality
lower esophagus muscularis layer	UBERON:0035833	71.71	gold quality
lower esophagus	UBERON:0013473	71.62	gold quality
metanephros cortex	UBERON:0010533	71.53	gold quality
cervix squamous epithelium	UBERON:0006922	71.51	gold quality
omental fat pad	UBERON:0010414	71.17	gold quality
peritoneum	UBERON:0002358	71.12	gold quality
adipose tissue of abdominal region	UBERON:0007808	70.79	gold quality
muscle organ	UBERON:0001630	70.53	gold quality
subcutaneous adipose tissue	UBERON:0002190	70.07	gold quality
hindlimb stylopod muscle	UBERON:0004252	69.60	gold quality
triceps brachii	UBERON:0001509	69.05	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	69.02	gold quality
heart	UBERON:0000948	68.97	gold quality
tibial nerve	UBERON:0001323	68.67	gold quality
ascending aorta	UBERON:0001496	68.12	gold quality
tongue squamous epithelium	UBERON:0006919	67.89	gold quality
thoracic aorta	UBERON:0001515	67.74	gold quality
squamous epithelium	UBERON:0006914	67.31	gold quality
adipose tissue	UBERON:0001013	67.12	gold quality
connective tissue	UBERON:0002384	66.77	gold quality
mucosa of stomach	UBERON:0001199	66.61	gold quality
tendon	UBERON:0000043	66.49	gold quality
aorta	UBERON:0000947	66.42	gold quality
pancreatic ductal cell	CL:0002079	66.18	silver quality
olfactory bulb	UBERON:0002264	66.17	gold quality
liver	UBERON:0002107	65.77	gold quality
secondary oocyte	CL:0000655	65.73	gold quality
esophagus squamous epithelium	UBERON:0006920	65.64	gold quality
cerebellar vermis	UBERON:0004720	65.62	gold quality
popliteal artery	UBERON:0002250	65.54	gold quality
tibial artery	UBERON:0007610	65.52	gold quality
right adrenal gland cortex	UBERON:0035827	65.40	gold quality
left uterine tube	UBERON:0001303	65.36	gold quality
gingiva	UBERON:0001828	65.32	gold quality
male germ cell	CL:0000015	65.26	gold quality
muscle layer of sigmoid colon	UBERON:0035805	65.16	gold quality
gingival epithelium	UBERON:0001949	65.15	gold quality
body of uterus	UBERON:0009853	64.93	gold quality
sperm	CL:0000019	64.90	gold quality
gluteal muscle	UBERON:0002000	64.70	gold quality
cartilage tissue	UBERON:0002418	64.67	gold quality
oocyte	CL:0000023	64.66	gold quality
right adrenal gland	UBERON:0001233	64.39	gold quality
epithelial cell of pancreas	CL:0000083	64.34	gold quality
medial globus pallidus	UBERON:0002477	64.28	gold quality
right atrium auricular region	UBERON:0006631	64.13	gold quality
myocardium	UBERON:0002349	64.04	gold quality
bone marrow	UBERON:0002371	63.64	gold quality
adult mammalian kidney	UBERON:0000082	63.59	gold quality
epithelium of esophagus	UBERON:0001976	63.55	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	63.51	gold quality
sural nerve	UBERON:0015488	63.37	silver quality
fundus of stomach	UBERON:0001160	63.29	gold quality
descending thoracic aorta	UBERON:0002345	63.28	gold quality
cardiac atrium	UBERON:0002081	63.23	gold quality
small intestine Peyer’s patch	UBERON:0003454	63.07	gold quality
body of stomach	UBERON:0001161	62.67	gold quality
right coronary artery	UBERON:0001625	62.57	gold quality
left adrenal gland	UBERON:0001234	62.54	gold quality
globus pallidus	UBERON:0001875	62.37	gold quality
endothelial cell	CL:0000115	62.36	gold quality
adrenal cortex	UBERON:0001235	62.34	gold quality
left adrenal gland cortex	UBERON:0035825	62.34	gold quality
oral cavity	UBERON:0000167	62.15	gold quality
adrenal gland	UBERON:0002369	62.09	gold quality
vena cava	UBERON:0004087	61.99	gold quality
right ovary	UBERON:0002118	61.88	gold quality
esophagus	UBERON:0001043	61.83	gold quality
putamen	UBERON:0001874	61.83	gold quality
small intestine	UBERON:0002108	61.80	gold quality
left coronary artery	UBERON:0001626	61.67	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	61.45	gold quality
colon	UBERON:0001155	61.40	gold quality
large intestine	UBERON:0000059	61.38	gold quality
coronary artery	UBERON:0001621	61.36	gold quality
skin of leg	UBERON:0001511	61.35	gold quality
mouth mucosa	UBERON:0003729	61.30	gold quality
nucleus accumbens	UBERON:0001882	61.25	gold quality
minor salivary gland	UBERON:0001830	61.19	gold quality
blood vessel layer	UBERON:0004797	61.18	gold quality
intestine	UBERON:0000160	61.10	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	61.10	gold quality
transverse colon	UBERON:0001157	61.05	gold quality
cortex of kidney	UBERON:0001225	60.97	gold quality
saliva-secreting gland	UBERON:0001044	60.89	gold quality
adrenal tissue	UBERON:0018303	60.81	gold quality
mucosa of sigmoid colon	UBERON:0004993	60.79	gold quality
metanephros	UBERON:0000081	60.53	gold quality
myometrium	UBERON:0001296	60.51	gold quality
stomach	UBERON:0000945	60.02	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	3.88
E-CURD-53	no	34.92

HPA expression

RNA tissue specificity: Low tissue specificity

showing 60 of 76 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Choroid plexus	tissue	9.5
Skeletal muscle	tissue	4.8	low
Tongue	tissue	4.7
Epididymis	tissue	3.6	not detected
Liver	tissue	2.8	low
Nucleus accumbens	tissue	2.6
Adipose tissue	tissue	2.5	not detected
Heart muscle	tissue	2.4	not detected
Spleen	tissue	2.4	not detected
Basal ganglia	tissue	2.2	not detected
Ventral forebrain	tissue	2.0
Septum	tissue	2.0
Amygdala	tissue	1.7
Vagina	tissue	1.6	not detected
Spinal cord	tissue	1.6
Superior colliculi	tissue	1.5
Hippocampus	tissue	1.5	not detected
Hippocampal formation	tissue	1.5
Seminal vesicle	tissue	1.4	low
Kidney	tissue	1.4	not detected
Putamen	tissue	1.3
Cerebellum	tissue	1.2	high
Adrenal gland	tissue	1.2	not detected
Substantia nigra	tissue	1.1
Caudate putamen	tissue	1.1
Salivary gland	tissue	1.0	not detected
Prefrontal cortex	tissue	0.8
Cerebral cortex	tissue	0.8	not detected
Medulla oblongata	tissue	0.8
Thalamus	tissue	0.8
Hypothalamus	tissue	0.8
Bone marrow	tissue	0.8	not detected
Insular cortex	tissue	0.8
Ovary	tissue	0.7	not detected
Motor cortex	tissue	0.7
Placenta	tissue	0.7	not detected
Small intestine	tissue	0.7	not detected
Entorhinal cortex	tissue	0.7
Retrosplenial and cingulate cortex	tissue	0.7
Temporal cortex	tissue	0.7
Pons	tissue	0.6
Smooth muscle	tissue	0.6	not detected
Midbrain	tissue	0.6
Gallbladder	tissue	0.6	low
Locus coeruleus	tissue	0.6
Retrosplenial cortex	tissue	0.6
Testis	tissue	0.5	medium
Colon	tissue	0.5	not detected
Somatosensory cortex	tissue	0.5
Occipital cortex	tissue	0.5
Pituitary gland	tissue	0.4
Stomach 1	tissue	0.4	not detected
Esophagus	tissue	0.4	not detected
Parathyroid gland	tissue	0.4	not detected
Endometrium 1	tissue	0.4	not detected
Corpus callosum	tissue	0.4
Periaqueductal gray	tissue	0.4
Olfactory bulb	tissue	0.4
Fallopian tube	tissue	0.4	not detected
Breast	tissue	0.3	not detected

Brain sub-regions (HPA Brain Atlas): detected in 188; highest nTPM — Blood vessel (7.2), Lateral geniculate body (4.6), Inferior parietal lobule (4.0), Parieto-temporal junction (white matter) (4.0), Temporal white matter (4.0).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): SP1, STAT6, TFAP2A

miRNA regulators (miRDB)

Targeting ADRA2B by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 81 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-4747-5P	100.00	67.90	2681
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-4283	100.00	66.42	2097
HSA-MIR-6873-3P	100.00	71.42	2626
HSA-MIR-6748-5P	100.00	65.81	1057
HSA-MIR-6778-3P	99.96	67.29	2693
HSA-MIR-6825-5P	99.96	69.81	3431
HSA-MIR-145-5P	99.92	71.13	1836
HSA-MIR-5195-3P	99.92	70.92	1877
HSA-MIR-589-3P	99.91	69.62	2088
HSA-MIR-6794-5P	99.76	66.38	1048
HSA-MIR-3150A-3P	99.76	64.44	1640
HSA-MIR-6763-5P	99.76	64.68	1767
HSA-MIR-6764-5P	99.75	67.89	2304
HSA-MIR-6752-3P	99.72	66.71	1587
HSA-MIR-4716-3P	99.69	66.73	1022
HSA-MIR-7-5P	99.67	70.53	1809
HSA-MIR-6887-3P	99.66	67.83	1778
HSA-MIR-3175	99.65	66.30	2031
HSA-MIR-1827	99.63	68.57	3265
HSA-MIR-4516	99.61	67.78	3390
HSA-MIR-6132	99.60	65.83	1554
HSA-MIR-6836-5P	99.60	65.62	1538
HSA-MIR-6752-5P	99.59	67.32	1243
HSA-MIR-4310	99.59	68.84	2527
HSA-MIR-1915-3P	99.58	66.79	1988
HSA-MIR-3136-3P	99.57	66.59	781
HSA-MIR-7155-3P	99.57	66.48	794
HSA-MIR-4441	99.49	66.56	3216

Functional genomics

gnomAD constraint: pLI 8.38e-07, LOEUF 1.56, missense Z 0.309 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000620793 — one region, missense o/e 1.00.

Literature-anchored findings (GeneRIF, showing 40)

• findings show that NPC1b is expressed in the midgut epithelium and is essential for growth during larval development; findings suggest that NPC1b plays an early role in sterol absorption (PMID:17339027)
• Middle-aged white men carrying the DD genotype of the alpha(2B)-AR have a significantly increased risk for sudden cardiac death and myocardial infarction, especially before the age of 55 years. (PMID:12535806)
• No major functional significance of the alpha(2B) adrenergic receptor polymorphism in the present sample of morbidly obese subjects was found. (PMID:12822042)
• Alpha2-ARs in vascular smooth muscle cells reflect differential activity of alpha2-AR gene promoters. Alpha2C-ARs can be induced via p38 MAPK-dependent pathway. (PMID:12946937)
• A polymorphism in the (alpha)2B adrenoceptor gene associates with hypertension. (PMID:14744925)
• body fat response to exercise training in older adults is associated with the combined effects of the Glu12/Glu9 alpha2b-adrenergic receptor, Trp64Arg beta3-adrenergic receptor, and Gln27Glu beta2-adrenergic receptor gene variants (PMID:15166301)
• The 12Glu9 polymorphism of ADRA2B is associated with impaired insulin secretion and may predict the development of Type 2 diabetes. (PMID:15309292)
• ADRA2A and ADRA2B each had a single haplotype block at least 11 and 16 kb in size (PMID:15592690)
• the del301-303 polymorphism of ADRA2B does not contribute significantly to interindividual in vivo variability in response to alpha2-AR activation in the hand vein (PMID:15864122)
• analysis of stability of ADRA2B and binding to small molecules after detergent solubilization (PMID:15893292)
• In Chinese men, the I allele of the ADRA2B gene is associated with higher blood pressure, but also with a more favourable metabolic phenotype. (PMID:16269962)
• Multiple stepwise linear regression identified alpha2B genotype as an independent predictor of age at onset of type 2 diabetes. (PMID:17039423)
• Leisure-time physical activity decreased the risk of type 2 diabetes in those with the 12Glu and 9Glu alleles of the ADRA2B gene. (PMID:17277585)
• study showed that genotype distribution and the frequency of the alpha 2 beta adrenergic receptor alleles was not different in Greek women with polycystic ovary syndrome and controls (PMID:17370102)
• alpha-2CDel AR appears to play only a minor role in presynaptic regulation of NA release and/or to be not hypofunctional in vivo in humans, but functional responsiveness of presynaptic alpha-2 AR declines with ageing. (PMID:17410123)
• Evidence for an association of the D allele with both presence and severity of neuropathy in patients with type 2 diabetes mellitus. (PMID:17516297)
• The decrease in intermuscular fat (IMF) in ADRalpha2bGlu9 carriers was significantly different from a nonsignificant increase in ADRalpha2bGlu9 noncarriers. (PMID:17595424)
• main finding was that men with the DD polymorphism of the ADRA2B gene and job strain have significantly higher blood pressure than all other gene-work characteristics combinations (PMID:17620957)
• {alpha}2-adrenergic receptor-mediated antilipolysis in human adipose tissue is inhibited by long chain fatty acids (PMID:17625217)
• a deletion variant of ADRA2B, the gene encoding the alpha2b-adrenergic receptor, is related to enhanced emotional memory in healthy Swiss subjects and in survivors of the Rwandan civil war who experienced highly aversive emotional situations. (PMID:17660814)
• These data indicate that alpha-2 adrenergic receptors contribute significantly to CBR-induced vasoconstriction in the human leg under resting conditions. (PMID:18054844)
• A vascular smooth muscle cell line stably expressing the human alpha 2B-adrenoceptor was generated by transfection of rat cells (PMID:18456256)
• we could not replicate the association of blood pressure and the metabolic phenotypes with ADRA2B I/D polymorphism (PMID:18596718)
• The ADRA2B D allele is associated with a favorable anthropometric and metabolic profile in Chinese population. (PMID:18854756)
• A variant of the ADRA2B gene is associated with essential hypertension with or without type 2 diabetes in Malaysian subjects. (PMID:18953403)
• The alpha(2C) Del322-325 polymorphism exclusively or in combination with the beta(1)Arg389 allele is not associated with an increased risk of adverse events in HF. (PMID:19477404)
• The I/D polymorphism is not consistently associated with metabolic syndrome and metabolic/anthropometric parameters but with diastolic blood pressure in an urban-based population of middle-aged Swedes. (PMID:19593211)
• A novel polymorphism in the coding region of the human alpha-2B adrenergic receptor has been identified and demonstrated to affect receptor function. (PMID:19728989)
• A functional deletion variant of ADRA2B is related to increased responsivity and connectivity of brain regions implicated in emotional memory. (PMID:19826083)
• The ADRA2B 301-303 deletion allele (ins/del and del/del, n = 18) was associated with resistance to desensitization. (PMID:20051907)
• carriage of the ADRA2B deletion abolished the relative memory impairment in homozygous COMT val158 carriers compared to met158 carriers. (PMID:20110158)
• gene x exercise interactions were observed for A2BGlu9/12 and B2Gln27Glu on change in lean soft tissue (LST, p = 0.02); exercisers on the A2BGlu9- background gained LST compared to a loss among controls over 12 months (p\0.05) (PMID:20401689)
• Data provide strong evidence indicating that Rab8 GTPase interacts with distinct motifs in the C termini of alpha(2B)-AR and beta(2)-AR and differentially modulates their traffic from the TGN to the cell surface. (PMID:20424170)
• the findings of this study do not support a functional significance of ADRA2B indel polymorphism at position -4825 relative to the start codon in the far upstream region of the promoter in the present migraine subjects. (PMID:20651814)
• Homozygote for insertion [I]/deletion allele of alpha(2B)-AR gene polymorphism is associated with silent myocardial ischemia in type 2 diabetes mellitus patients with coronary artery disease. (PMID:20692245)
• The noradrenaline-mediated depolarization of vascular smooth muscle cells is produced by activation of both alpha(1)-and alpha(2)-adrenoceptors. (PMID:20739228)
• Data do not show any association between the presence of the alpha2B-adrenergic receptor deletion allele and the occurrence of spontaneous abortions. (PMID:21159032)
• the ADRA2B polymorphism influences emotional memory formation but not memory retrieval in the amygdala and left inferior frontal gyrus. (PMID:21259387)
• Alpha2B-adrenergic receptor interaction with tubulin controls its transport from the endoplasmic reticulum to the cell surface (PMID:21357695)
• The significant novel finding from this study is that the affective modulation of T2 detection is influenced by a non-additive (epistatic) interaction between the ADRA2B and 5-HTTLPR insertion/deletion polymorphisms. (PMID:21854681)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	adra2b	ENSDARG00000102096
mus_musculus	Adra2b	ENSMUSG00000058620
rattus_norvegicus	Adra2b	ENSRNOG00000013887
caenorhabditis_elegans	ser-5	WBGENE00008890

Paralogs (18): ADRB1 (ENSG00000043591), ADRA1A (ENSG00000120907), DRD2 (ENSG00000149295), ADRA2A (ENSG00000150594), GPR101 (ENSG00000165370), ADRB2 (ENSG00000169252), ADRA1B (ENSG00000170214), ADRA1D (ENSG00000171873), OR5T3 (ENSG00000172489), OR56A1 (ENSG00000180934), OR5T1 (ENSG00000181698), OR5T2 (ENSG00000181718), OR56A4 (ENSG00000183389), ADRA2C (ENSG00000184160), OR56A3 (ENSG00000184478), OR13F1 (ENSG00000186881), OR56A5 (ENSG00000188691), ADRB3 (ENSG00000188778)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:87935) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 16 distinct phenotype terms.

Mouse phenotype (MP)	Records
abnormal fertility/fecundity	2
abnormal vasoconstriction	1
abnormal lung development	1
atelectasis	1
thick pulmonary interalveolar septum	1
cyanosis	1
respiratory failure	1
postnatal lethality	1
abnormal pulmonary alveolus morphology	1
dilated heart right ventricle	1
decreased lung weight	1
increased systemic arterial systolic blood pressure	1
slow postnatal weight gain	1
decreased birth weight	1
neonatal lethality, incomplete penetrance	1
increased mesenchymal cell proliferation involved in lung development	1

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Pan troglodytes	P60026	100.0%	Diamond
Sus scrofa	Q29005	100.0%	Diamond
Pan paniscus	Q49SQ2	99.7%	Diamond
Locusta migratoria	Q25321	99.4%	Diamond
Chlorocebus aethiops	P52702	99.1%	Diamond
Canis lupus familiaris	Q6XXX9	99.1%	Diamond
Macaca mulatta	P56494	97.4%	Diamond
Lacunicambarus ludovicianus	O16017	97.3%	Diamond
Mustela putorius furo	Q6TLI9	97.3%	Diamond
Drosophila melanogaster	P06002	97.1%	Diamond
Drosophila pseudoobscura pseudoobscura	P28678	97.1%	Diamond
Bos taurus	P20288	96.8%	Diamond
Cavia porcellus	P47745	95.4%	Diamond
Ovis aries	Q28756	94.1%	Diamond
Oryctolagus cuniculus	P34970	93.0%	Diamond
Xenopus laevis	P24628	92.9%	Diamond
Mastomys natalensis	P30796	92.7%	Diamond
Camponotus atriceps	Q17292	92.1%	Diamond
Elephas maximus	O19014	91.3%	Diamond
Dugong dugon	O77713	91.3%	Diamond
Procavia capensis habessinica	O19054	90.7%	Diamond
Amblysomus hottentotus	O18935	90.2%	Diamond
Orycteropus afer	O19032	89.7%	Diamond
Caenorhabditis briggsae	Q61H86	89.1%	Diamond
Macroscelides proboscideus	O19025	88.1%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
GPAT2	protein-coding	150763
ASTL	protein-coding	431705
DUSP2	protein-coding	1844
STARD7-AS1	ncRNA	285033
STARD7	protein-coding	56910
SNORA112	snoRNA	109623481
LINC00342	ncRNA	150759
ANKRD36C	protein-coding	400986

Protein

Protein identifiers

Alpha-2B adrenergic receptor — P18089 (reviewed: P18089)

Alternative names: Alpha-2 adrenergic receptor subtype C2, Alpha-2B adrenoreceptor

All UniProt accessions (1): P18089

UniProt curated annotations — full annotation on UniProt →

Function. Alpha-2 adrenergic receptors are G protein-coupled receptors for catecholamines that activate G(i/o) protein pathway, thereby promoting adenylyl cyclase inhibition, ERK1/2 stimulation, and voltage-gated calcium channels suppression. Control a variety of physiological processes, such as regulation of blood pressure, lipolysis and insulin release. The rank order of potency for agonists of ADRA2B is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phentolamine > mianserine > spiperone > prazosin > alprenolol > propanolol > pindolol.

Subunit / interactions. Interacts with RAB26; RAB26 mediates cell surface transport from the Golgi. Interacts with PPP1R9B. Interacts with GGA1, GGA2 and GGA3; GGA1, GGA2 and GGA3 mediates transport from the Golgi to the cell membrane. Interacts with RAB43 (GTP-bound); RAB43 mediates ADRA2B ER-to-Golgi cell transport.

Subcellular location. Cell membrane.

Disease relevance. Epilepsy, familial adult myoclonic, 2 (FAME2) [MIM:607876] A form of familial myoclonic epilepsy, a neurologic disorder characterized by cortical hand tremors, myoclonic jerks and occasional generalized or focal seizures with a non-progressive or very slowly progressive disease course. Usually, myoclonic tremor is the presenting symptom, characterized by tremulous finger movements and myoclonic jerks of the limbs increased by action and posture. In a minority of patients, seizures are the presenting symptom. Some patients exhibit mild cognitive impairment. FAME2 inheritance is autosomal dominant. The disease is caused by variants affecting the gene represented in this entry.

Polymorphism. A rare polymorphic frameshift in position 451 produces a protein of 545 residues.

Similarity. Belongs to the G protein-coupled receptor 1 family. Adrenergic receptor subfamily. ADRA2B sub-subfamily.

RefSeq proteins (1): NP_000673* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000207	ADRA2B_rcpt	Family
IPR000276	GPCR_Rhodpsn	Family
IPR002233	ADR_fam	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (48 total): helix 13, topological domain 8, transmembrane region 7, sequence variant 6, compositionally biased region 3, site 3, region of interest 2, turn 2, chain 1, lipid moiety-binding region 1, disulfide bond 1, sequence conflict 1

Structure

Experimental structures (PDB)

2 structures by resolution:

PDB	Title	Method	Resolution (Å)
6K41	cryo-EM structure of alpha2BAR-GoA complex	ELECTRON MICROSCOPY	2.9
6K42	cryo-EM structure of alpha2BAR-Gi1 complex	ELECTRON MICROSCOPY	4.1

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P18089-F1	72.81	0.42

Antibody-complex structures (SAbDab)

2 antibodies co-crystallized with this protein: 6K41, 6K42

Human Protein Atlas

Protein class: G-protein coupled receptors, GPCRs excl olfactory receptors, Predicted membrane proteins, GPCRHMM predicted membrane proteins, Disease related genes, FDA approved drug targets, Small molecule drugs

Protein evidence: Evidence at protein level

Subcellular location (HPA, imaging): vesicles; cytosol

Antibody reliability (HPA): IH approved · IF supported

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (3)

Position	Role
92	implicated in ligand binding
176	implicated in catechol agonist binding
180	implicated in catechol agonist binding

Post-translational modifications (1)

Type	Positions
S-palmitoyl cysteine	442

Disulfide bonds (1)

Type	Positions
Disulfide bond	85–164

Function

Pathways and Gene Ontology

Reactome pathways

4 curated (TAS) of 13; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

13 pathways:

ID	Pathway	Evidence
R-HSA-392023	Adrenaline signalling through Alpha-2 adrenergic receptor	curated
R-HSA-390696	Adrenoceptors	curated
R-HSA-418594	G alpha (i) signalling events	curated
R-HSA-418597	G alpha (z) signalling events	curated
R-HSA-375280	Amine ligand-binding receptors	—
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)	—
R-HSA-388396	GPCR downstream signalling	—
R-HSA-500792	GPCR ligand binding	—
R-HSA-109582	Hemostasis	—
R-HSA-76009	Platelet Aggregation (Plug Formation)	—
R-HSA-76002	Platelet activation, signaling and aggregation	—
R-HSA-162582	Signal Transduction	—
R-HSA-372790	Signaling by GPCR	—

MSigDB gene sets: 193 (showing top): MODULE_92, GGTGTGT_MIR329, GOBP_REGULATION_OF_BLOOD_PRESSURE, GOBP_CIRCULATORY_SYSTEM_PROCESS, REACTOME_PLATELET_AGGREGATION_PLUG_FORMATION, REACTOME_PLATELET_ACTIVATION_SIGNALING_AND_AGGREGATION, REACTOME_G_ALPHA_Z_SIGNALLING_EVENTS, GOBP_PLATELET_ACTIVATION, MODULE_64, GOBP_POSITIVE_REGULATION_OF_NEURON_DIFFERENTIATION, GOBP_REGULATION_OF_SMOOTH_MUSCLE_CONTRACTION, GOBP_POSITIVE_REGULATION_OF_MAPK_CASCADE, GOCC_CELL_SURFACE, GOBP_NEUROGENESIS, GOBP_CELL_CELL_SIGNALING

GO Biological Process (19): regulation of vascular associated smooth muscle contraction (GO:0003056), epidermal growth factor receptor signaling pathway (GO:0007173), G protein-coupled receptor signaling pathway (GO:0007186), adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway (GO:0007193), cell-cell signaling (GO:0007267), female pregnancy (GO:0007565), negative regulation of norepinephrine secretion (GO:0010700), platelet activation (GO:0030168), negative regulation of epinephrine secretion (GO:0032811), positive regulation of MAPK cascade (GO:0043410), positive regulation of neuron differentiation (GO:0045666), positive regulation of blood pressure (GO:0045777), positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction (GO:0051897), positive regulation of uterine smooth muscle contraction (GO:0070474), adrenergic receptor signaling pathway (GO:0071875), adenylate cyclase-inhibiting adrenergic receptor signaling pathway (GO:0071881), regulation of smooth muscle contraction (GO:0006940), signal transduction (GO:0007165), regulation of vasoconstriction (GO:0019229)

GO Molecular Function (5): alpha2-adrenergic receptor activity (GO:0004938), epinephrine binding (GO:0051379), G protein-coupled receptor activity (GO:0004930), adrenergic receptor activity (GO:0004935), protein binding (GO:0005515)

GO Cellular Component (3): plasma membrane (GO:0005886), cell surface (GO:0009986), membrane (GO:0016020)

Reactome top-level categories

9 top-level categories:

Category	Pathways
GPCR downstream signalling	2
Signaling by GPCR	2
Amine ligand-binding receptors	1
Platelet Aggregation (Plug Formation)	1
Signal Transduction	1
GPCR ligand binding	1
Class A/1 (Rhodopsin-like receptors)	1
Hemostasis	1
Platelet activation, signaling and aggregation	1

GO top-level categories

53 GO namespaces:

Category	Terms
cell communication	2
signaling	2
negative regulation of catecholamine secretion	2
positive regulation of intracellular signal transduction	2
G protein-coupled receptor signaling pathway	2
adrenergic receptor signaling pathway	2
cellular anatomical structure	2
regulation of smooth muscle contraction	1
vascular associated smooth muscle contraction	1
regulation of vasoconstriction	1
ERBB signaling pathway	1
G protein-coupled receptor activity	1
signal transduction	1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase inhibitor activity	1
multi-organism reproductive process	1
multi-multicellular organism process	1
regulation of norepinephrine secretion	1
norepinephrine secretion	1
cell activation	1
blood coagulation	1
regulation of epinephrine secretion	1
epinephrine secretion	1
MAPK cascade	1
regulation of MAPK cascade	1
neuron differentiation	1
positive regulation of cell differentiation	1
regulation of neuron differentiation	1
regulation of blood pressure	1
phosphatidylinositol 3-kinase/protein kinase B signal transduction	1
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	1
positive regulation of smooth muscle contraction	1
uterine smooth muscle contraction	1
regulation of uterine smooth muscle contraction	1
adrenergic receptor activity	1
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	1
regulation of muscle contraction	1
smooth muscle contraction	1
cellular process	1
regulation of cellular process	1
cellular response to stimulus	1
vasoconstriction	1
blood vessel diameter maintenance	1
regulation of blood circulation	1
alpha-adrenergic receptor activity	1
hormone binding	1
cation binding	1
catecholamine binding	1
transmembrane signaling receptor activity	1
G protein-coupled amine receptor activity	1
binding	1
membrane	1
cell periphery	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 12 of 27 annotations. The rest are phylogenetic / computational / electronic (IEA).

12 experimentally-supported GO terms:

GO term	NS	Evidence
G protein-coupled receptor signaling pathway	BP	direct assay
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	BP	mutant phenotype
adenylate cyclase-inhibiting adrenergic receptor signaling pathway	BP	mutant phenotype
adrenergic receptor signaling pathway	BP	direct assay
epidermal growth factor receptor signaling pathway	BP	direct assay
positive regulation of MAPK cascade	BP	direct assay
positive regulation of neuron differentiation	BP	direct assay
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	BP	direct assay
cell surface	CC	direct assay
plasma membrane	CC	direct assay
alpha2-adrenergic receptor activity	MF	direct assay
epinephrine binding	MF	direct assay

Protein interactions and networks

STRING

showing 16 of 720 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ADRA2B	RBP3	P10745	512
ADRA2B	JRK	O75564	446
ADRA2B	DBH	P09172	432
ADRA2B	SLC6A4	P31645	421
ADRA2B	VWF	P04275	419
ADRA2B	GABRG2	P18507	397
ADRA2B	GNG7	O60262	379
ADRA2B	DUSP2	Q05923	370
ADRA2B	RASGRP2	Q7LDG7	370
ADRA2B	PLCB4	Q15147	370
ADRA2B	ZP2	Q05996	370
ADRA2B	PDE1C	Q14123	369
ADRA2B	PDE1B	Q01064	366
ADRA2B	SLC35A2	P78381	365
ADRA2B	APOB	P04114	363
ADRA2B	CLN6	Q9NWW5	363

IntAct

Human interaction partners of ADRA2B in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

8 partners by confidence:

Partner	Interaction type	MIscore	Records
RAB26	physical association	0.630	4
ACKR3	proximity	0.420	2
RAMP3	physical association	0.400	3
RAMP1	physical association	0.400	2
RAMP2	physical association	0.400	2
GGA2	physical association	0.400	1
SH3GL1	physical association	0.400	1
SH3GL2	physical association	0.400	1

BioGRID (9 interactions; top human partners by supporting records): GGA2 (Affinity Capture-Western; 2 records), GGA3 (Affinity Capture-Western; 2 records), EIF2B1 (Reconstituted Complex), GGA1 (Reconstituted Complex), GOLGA4 (Co-localization), PPP1R9B (Reconstituted Complex), UCHL1 (Reconstituted Complex)

SIGNOR signaling

showing 18 of 22 signaling interactions:

A	Effect	B	Mechanism
ADRA2B	“up-regulates activity”	GNAI1	binding
ADRA2B	“up-regulates activity”	GNAI3	binding
ADRA2B	“up-regulates activity”	GNAO1	binding
ADRA2B	“up-regulates activity”	GNAZ	binding
ADRA2B	“up-regulates activity”	GNA12	binding
(R)-noradrenaline	“up-regulates activity”	ADRA2B	“chemical activation”
brimonidine	“up-regulates activity”	ADRA2B	“chemical activation”
clonidine	“up-regulates activity”	ADRA2B	“chemical activation”
dexmedetomidine	“up-regulates activity”	ADRA2B	“chemical activation”
Guanabenz	“up-regulates activity”	ADRA2B	“chemical activation”
tolazoline	“down-regulates activity”	ADRA2B	“chemical inhibition”
oxymetazoline	“up-regulates activity”	ADRA2B	“chemical activation”
Guanfacine	“up-regulates activity”	ADRA2B	“chemical activation”
N-(2,6-dimethylphenyl)-5,6-dihydro-4H-1,3-thiazin-2-amine	“up-regulates activity”	ADRA2B	“chemical activation”
ADRA2B	“up-regulates activity”	GNAI2	binding
ADRA2B	“up-regulates activity”	GNA15	binding
zotepine	“down-regulates activity”	ADRA2B	“chemical inhibition”
lofexidine	“up-regulates activity”	ADRA2B	“chemical activation”

Protein complexes (CORUM) (9)

Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).

9 complexes by size:

Complex	Subunits	Members
★ ACKR3-ADRA2B complex	2	ACKR3, ADRA2B
★ ADRA2B-RAB26 complex	2	ADRA2B, RAB26
★ ADRA2B-APLP1 complex	2	APLP1, ADRA2B
★ ADRA2B-RAB8A complex	2	ADRA2B, RAB8A
★ ADRA2B-ARF1 complex	2	ADRA2B, ARF1
★ ADRA2B-PPP1R9B complex	2	ADRA2B, PPP1R9B
★ ADRA2B-GGA1 complex	2	ADRA2B, GGA1
★ ADRA2B-GGA2 complex	2	ADRA2B, GGA2
★ ADRA2B-GGA3 complex	2	ADRA2B, GGA3

Ligand–receptor pairs (CellPhoneDB) (6)

Curated ligand–receptor partners (cell-cell communication), distinct from the protein–protein interactions above.

6 ligand–receptor pairs:

Partner	This gene’s role	Signaling class
DBH;SLC18A1	receptor	Signaling by Noradrenaline
DBH;SLC18A2	receptor	Signaling by Noradrenaline
DBH;SLC6A2	receptor	Signaling by Noradrenaline
PNMT	receptor	Signaling by Epinephrine
PNMT;SLC18A1	receptor	Signaling by Adrenaline
PNMT;SLC18A2	receptor	Signaling by Adrenaline

Disease & clinical

Genetic variants

Variant evidence for ADRA2B: 115 ClinVar records (16 pathogenic / likely pathogenic); 1 GWAS association. Per-variant detail is on Sugi Variant.

ClinVar

115 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	10
Likely pathogenic	6
Uncertain significance	72
Likely benign	20
Benign	4

Top pathogenic / likely-pathogenic (15)

Showing the 15 best-reviewed of 16 pathogenic / likely-pathogenic ClinVar records, ranked by ClinVar review status (expert panel → multiple submitters → single submitter), then by number of submitting labs.

Variant ID	HGVS	Classification	Review	Submitters
57434	GRCh38/hg38 2q11.2(chr2:96100812-97285797)x1	Pathogenic	criteria provided, single submitter	1
57543	GRCh38/hg38 2q11.1-11.2(chr2:95879602-97285797)x1	Pathogenic	criteria provided, single submitter	1
980466	GRCh37/hg19 2q11.1-11.2(chr2:96421161-97765561)x1	Pathogenic	criteria provided, single submitter	1
3024612	GRCh37/hg19 2q11.1-11.2(chr2:96780545-98098961)x1	Pathogenic	criteria provided, single submitter	1
4755375	GRCh38/hg38 2q11.1-11.2(chr2:95875947-97355895)x1	Pathogenic	criteria provided, single submitter	1
545284	NC_000002.12:g.(?96063558)(97079140_?)del	Likely pathogenic	criteria provided, single submitter	1
562641	GRCh37/hg19 2q11.1-11.2(chr2:96735977-98258828)x1	Likely pathogenic	criteria provided, single submitter	1
814283	GRCh37/hg19 2q11.1-11.2(chr2:96712139-98254657)x1	Likely pathogenic	criteria provided, single submitter	1
4682540	GRCh37/hg19 2p11.2-q11.2(chr2:85898497-97671333)x3	Likely pathogenic	criteria provided, single submitter	1
2664653	NM_000682.7(ADRA2B):c.116C>T (p.Thr39Ile)	Likely pathogenic	no assertion criteria provided	1
144712	GRCh38/hg38 2q11.1-11.2(chr2:95879602-97029672)x1	Pathogenic	no assertion criteria provided	1
146017	GRCh38/hg38 2q11.2(chr2:96073560-97062710)x1	Pathogenic	no assertion criteria provided	1
154733	GRCh38/hg38 2q11.2(chr2:96073560-97513144)x1	Pathogenic	no assertion criteria provided	1
997821	Single allele	Pathogenic	no assertion criteria provided	1
1708190	GRCh37/hg19 2p25.1-q13(chr2:11504318-111365996)x1	Pathogenic	no assertion criteria provided	1

Per-variant reference — Sugi Variant

Explore ADRA2B’s pathogenic and likely-pathogenic variants individually — each with its ClinVar classification and conditions, applied ACMG criteria (ClinGen expert panel, where curated), the calibrated in-silico predictors (AlphaMissense, REVEL, SaProt, conservation), gnomAD frequency, and the predictor-disagreement QC signal — on Sugi Variant.

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 10 predictions of 52):

Position(s)	Effect	Δscore	Sites
2:96115000	acceptor_gain	0.8700
2:96114387	acceptor_gain	0.6600
2:96114198	acceptor_gain	0.6500
2:96115001	acceptor_gain	0.6200
2:96114980	acceptor_gain	0.5800
2:96114986	acceptor_gain	0.5400
2:96114197	acceptor_gain	0.5200
2:96114802	donor_gain	0.4700
2:96114376	acceptor_gain	0.4400
2:96114798	donor_gain	0.4400

AlphaMissense

1,051 missense substitutions predicted likely pathogenic (of 2,882 scored), across 234 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

Residue	Likely-pathogenic substitutions	Mean am_pathogenicity	Max am_pathogenicity
M188	9	0.913	0.997
D58	8	0.999	1.000
N422	8	0.996	1.000
D92	8	0.995	0.997
N30	8	0.993	0.999
D109	8	0.993	0.997
F380	8	0.992	1.000
S419	8	0.987	0.999
F437	8	0.985	0.997
F433	8	0.983	0.999
N418	8	0.979	1.000
F387	8	0.978	0.998
F181	8	0.975	0.998
F388	8	0.974	0.997
F50	8	0.972	0.996
N48	8	0.965	0.996
H102	8	0.960	0.997
F429	8	0.958	0.994
F80	8	0.950	0.986
F369	8	0.950	0.988

HPA cancer prognostics

RNA cancer specificity: Low cancer specificity

Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.

2 prognostic cancer types:

Cancer	Prognostic	p-value
Kidney Renal Clear Cell Carcinoma (validation)	favorable	7.5e-07
Kidney Renal Clear Cell Carcinoma (TCGA)	favorable	0.000302

Disease associations

OMIM: gene MIM:104260 | disease phenotypes: MIM:181500

GenCC curated gene-disease

4 curated gene-disease records:

Disease	Classification	Inheritance	Records
benign adult familial myoclonic epilepsy	Supportive	Autosomal dominant
epilepsy, familial adult myoclonic, 2	Limited	Unknown
neurodevelopmental disorder	Limited	Autosomal recessive
epilepsy	Refuted Evidence	Autosomal dominant

ClinGen Gene-Disease Validity

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

1 validity classifications:

Disease	Classification	Inheritance
epilepsy	Refuted	AD

Mondo (6): schizophrenia (MONDO:0005090), intellectual disability (MONDO:0001071), epilepsy (MONDO:0005027), epilepsy, familial adult myoclonic, 2 (MONDO:0011930), benign adult familial myoclonic epilepsy (MONDO:0019448), neurodevelopmental disorder (MONDO:0700092)

Orphanet (2): NON RARE IN EUROPE: Schizophrenia (Orphanet:3140), NON RARE IN EUROPE: Unexplained intellectual disability (Orphanet:319658)

HPO phenotypes

8 phenotypes (HPO-id order):

HPO	Term
HP:0001249	Intellectual disability
HP:0001336	Myoclonus
HP:0002197	Generalized-onset seizure
HP:0002315	Headache
HP:0002353	EEG abnormality
HP:0002378	Hand tremor
HP:0007359	Focal-onset seizure
HP:0100576	Amaurosis fugax

GWAS associations

1 associations:

Study	Trait	p-value
GCST90002394_98	Monocyte percentage of white cells	2e-13

EFO canonical traits (from GWAS)

1 canonical traits:

EFO ID	Trait name
EFO:0007989	monocyte percentage of leukocytes

MeSH disease descriptors

4 disease descriptors:

Descriptor	Name	Tree numbers
D004827	Epilepsy	C10.228.140.490
D008607	Intellectual Disability	C10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539
D065886	Neurodevelopmental Disorders	F03.625
C564313	Epilepsy, Myoclonic, Benign Adult Familial, Type 2 *(supp.)*

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (4): CHEMBL1942 (SINGLE PROTEIN), CHEMBL2095158 (PROTEIN FAMILY), CHEMBL2095203 (PROTEIN FAMILY), CHEMBL2331074 (PROTEIN FAMILY)

Drugs acting on a complex or family that includes this protein

Curated ChEMBL mechanism-of-action drugs whose target is a protein complex or family of ≤10 members that includes ADRA2B — the drug acts on the assembly or class, not necessarily on this subunit alone.

38 drugs via a complex or family:

Drug	Target (ChEMBL)	Members	Max phase
ALSEROXYLON	Adrenergic receptor alpha	6	4
APRACLONIDINE HYDROCHLORIDE	Adrenergic receptor alpha-2	3	4
BRIMONIDINE TARTRATE	Adrenergic receptor alpha-2	3	4
CELIPROLOL	Adrenergic receptor alpha-2	3	4
CLONIDINE	Adrenergic receptor alpha-2	3	4
DEXMEDETOMIDINE HYDROCHLORIDE	Adrenergic receptor alpha-2	3	4
DIPIVEFRIN HYDROCHLORIDE	Adrenergic receptor	9	4
DROXIDOPA	Adrenergic receptor	9	4
EPHEDRINE SULFATE	Adrenergic receptor	9	4
EPINEPHRINE	Adrenergic receptor	9	4
ERGOLOID MESYLATES	Adrenergic receptor alpha	6	4
ERGOTAMINE TARTRATE	Adrenergic receptor alpha	6	4
GUANABENZ ACETATE	Adrenergic receptor alpha-2	3	4
GUANFACINE HYDROCHLORIDE	Adrenergic receptor alpha-2	3	4
HYDROXYAMPHETAMINE HYDROBROMIDE	Adrenergic receptor	9	4
LABETALOL HYDROCHLORIDE	Adrenergic receptor	9	4
LEVONORDEFRIN	Adrenergic receptor alpha-2	3	4
LOFEXIDINE HYDROCHLORIDE	Adrenergic receptor alpha-2	3	4
MEPHENTERMINE SULFATE	Adrenergic receptor	9	4
METHYLDOPA	Adrenergic receptor alpha-2	3	4
METHYLDOPATE HYDROCHLORIDE	Adrenergic receptor alpha-2	3	4
MIRTAZAPINE	Adrenergic receptor alpha-2	3	4
MOXISYLYTE	Adrenergic receptor alpha	6	4
NAPHAZOLINE HYDROCHLORIDE	Adrenergic receptor alpha	6	4
NOREPINEPHRINE BITARTRATE	Adrenergic receptor	9	4
OXYMETAZOLINE HYDROCHLORIDE	Adrenergic receptor alpha	6	4
PHENOXYBENZAMINE HYDROCHLORIDE	Adrenergic receptor alpha	6	4
PHENTOLAMINE MESYLATE	Adrenergic receptor alpha	6	4
RAUWOLFIA SERPENTINA	Adrenergic receptor alpha	6	4
TETRAHYDROZOLINE HYDROCHLORIDE	Adrenergic receptor alpha	6	4
TIZANIDINE HYDROCHLORIDE	Adrenergic receptor alpha-2	3	4
TOLAZOLINE HYDROCHLORIDE	Adrenergic receptor alpha	6	4
XYLOMETAZOLINE HYDROCHLORIDE	Adrenergic receptor alpha	6	4
AVIPTADIL	Adrenergic receptor alpha	6	3
ESMIRTAZAPINE MALEATE	Adrenergic receptor alpha-2	3	3
IDAZOXAN	Adrenergic receptor alpha-2	3	3
FADOLMIDINE HYDROCHLORIDE	Adrenergic receptor alpha-2	3	2
FIPAMEZOLE	Adrenergic receptor alpha-2	3	2

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,401,091 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

showing 60 of 316 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL1085	ACETOPHENAZINE	4	5,157
CHEMBL1173655	AFATINIB	4	15,878
CHEMBL709	ALFUZOSIN	4	6,651
CHEMBL1505	ALMOTRIPTAN	4	7,500
CHEMBL633	AMIODARONE	4	30,023
CHEMBL243712	AMISULPRIDE	4	10,675
CHEMBL629	AMITRIPTYLINE	4	53,007
CHEMBL1113	AMOXAPINE	4	20,303
CHEMBL43	AMSACRINE	4	83,286
CHEMBL53	APOMORPHINE	4	26,040
CHEMBL647	APRACLONIDINE	4	13,857
CHEMBL1112	ARIPIPRAZOLE	4	24,497
CHEMBL196	ASCORBIC ACID	4	1,043,187
CHEMBL3187365	ASENAPINE	4	146
CHEMBL296419	ASTEMIZOLE	4	21,684
CHEMBL641	ATOMOXETINE	4	13,258
CHEMBL1366	AURANOFIN	4
CHEMBL639	AZELASTINE	4	16,951
CHEMBL1200809	AZELASTINE HYDROCHLORIDE	4	3,838
CHEMBL46740	BAZEDOXIFENE	4	5,153
CHEMBL400599	BENFLUOREX	4
CHEMBL297302	BENPERIDOL	4
CHEMBL388590	BENZBROMARONE	4
CHEMBL1374379	BENZONATATE	4
CHEMBL3545985	BENZPHETAMINE	4
CHEMBL1201250	BENZQUINAMIDE	4
CHEMBL1201039	BENZTHIAZIDE	4
CHEMBL1201203	BENZTROPINE	4
CHEMBL1008	BEPRIDIL	4
CHEMBL290106	BITHIONOL	4
CHEMBL2105760	BREXPIPRAZOLE	4
CHEMBL844	BRIMONIDINE	4
CHEMBL493	BROMOCRIPTINE	4
CHEMBL28218	BROMPERIDOL	4
CHEMBL1295	BUTOCONAZOLE	4
CHEMBL2110816	BUTRIPTYLINE	4
CHEMBL1201087	CABERGOLINE	4
CHEMBL1014	CANDESARTAN CILEXETIL	4
CHEMBL190461	CANNABIDIOL	4
CHEMBL864	CARBINOXAMINE	4
CHEMBL2024517	CARIPRAZINE HYDROCHLORIDE	4
CHEMBL723	CARVEDILOL	4
CHEMBL186	CEFEPIME	4
CHEMBL118	CELECOXIB	4
CHEMBL790	CHLORHEXIDINE	4
CHEMBL76	CHLOROQUINE	4
CHEMBL505	CHLORPHENIRAMINE	4
CHEMBL71	CHLORPROMAZINE	4
CHEMBL43064	CINNARIZINE	4
CHEMBL1729	CISAPRIDE	4
CHEMBL1626	CLEMASTINE	4
CHEMBL415	CLOMIPRAMINE	4
CHEMBL134	CLONIDINE	4
CHEMBL1705	CLONIDINE HYDROCHLORIDE	4
CHEMBL104	CLOTRIMAZOLE	4
CHEMBL42	CLOZAPINE	4
CHEMBL516	CYPROHEPTADINE	4
CHEMBL1479	DANAZOL	4
CHEMBL1201216	DAPIPRAZOLE	4
CHEMBL1346	DARIFENACIN	4

PharmGKB: 1 entry (CPIC guideline: no)

PharmGKB variant annotations

Per-publication pharmacogenomic findings for this gene (significant associations).

1 published findings:

Variant	Drug(s)	Category	Finding	PMID
rs3813662	dexmedetomidine	Toxicity	Genotypes AA + CC is associated with increased likelihood of Bradycardia or Hypotensive disorder when treated with dexmedetomidine in children with Surgical procedure as compared to genotype AC.	PMID:39840108

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: gpcr — Adrenoceptors

Most potent curated ligand interactions (47 total), top 25:

Ligand	Action	Affinity	Parameter
dexmedetomidine	Full agonist	10.9	pIC50
medetomidine	Agonist	10.6	pIC50
detomidine	Agonist	10.2	pIC50
lisuride	Antagonist	9.9	pKi
terguride	Antagonist	9.4	pKi
[3H]rauwolscine	Antagonist	9.2	pKd
guanabenz	Agonist	9.0	pIC50
[3H]MK-912	Antagonist	8.9	pKd
spiroxatrine	Antagonist	8.8	pKi
guanfacine	Full agonist	8.7	pIC50
RX821002	Antagonist	8.7	pKi
atipamezole	Antagonist	8.6	pKi
RS79948	Antagonist	8.6	pKi
clonidine	Agonist	8.6	pIC50
yohimbine	Antagonist	8.4	pKi
WB 4101	Antagonist	8.4	pKi
brimonidine (UK14304)	Agonist	8.4	pIC50
chlorpromazine	Antagonist	8.3	pKi
rauwolscine	Antagonist	8.3	pKi
roxindole	Antagonist	8.3	pKi
zotepine	Antagonist	8.2	pKi
MK-912	Antagonist	8.2	pKi
phentolamine	Antagonist	8.2	pKi
[125I]p-iodoclonidine	Partial agonist	8.1	pKd
[3H]RX821002	Antagonist	8.1	pKd

Binding affinities (BindingDB)

685 measured of 789 human assays (878 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
[O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin-1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione	EC50	0.01 nM
2-(8-Bromo-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b’]difuran-4-yl)-ethylamine	EC50	0.029 nM
CHEMBL72441	EC50	0.11 nM
5-{4-[4-(5-Cyano-1H-indol-3-yl)-butyl]-piperazin-1-yl}-benzofuran-2-carboxylic acid amide	EC50	0.12 nM
3,3-diethyl-1-[(4R,7R)-6-methyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(15),2,9,12(16),13-pentaen-4-yl]urea	KI	0.15 nM
(R)-4-(3,4-Difluoro-phenyl)-2-methyl-6-oxo-1,4,5,6-tetrahydro-pyridine-3-carboxylic acid {3-[4-(2-cyano-4-fluoro-phenyl)-piperidin-1-yl]-propyl}-amide	KI	0.2 nM
SNAP-5089	KI	0.2 nM
CAS_163091	KI	0.21 nM
CHEMBL4083252	KI	0.22 nM
CHEMBL91022	KI	0.229 nM
2,6-Dimethyl-4-(4-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 3-[3-(4,4-diphenyl-piperidin-1-yl)-propyl] ester 5-methyl ester	KI	0.32 nM
Urapidil-5-methyl	KI	0.35 nM
1-(2-{4-[5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl]piperidin-1-yl}ethyl)imidazolidin-2-one	KI	0.38 nM
1N-{10-[2-hydroxy-(1R,2S,4aR,13bS,14aS)-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroisoquino[3,2-a]b-carbolin-1-ylcarboxamido]decyl}-2-hydroxy-(1R,2S,4aR,13bS,14aS)-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroisoquino[3, ;dihydrochloride	KI	0.39 nM
5-[3-(4,4-Diphenyl-piperidin-1-yl)-propylcarbamoyl]-2,6-dimethyl-4-(3-nitro-phenyl)-nicotinic acid methyl ester	KI	0.4 nM
(R)-4-(3,4-Difluoro-phenyl)-2-methyl-6-oxo-1,4,5,6-tetrahydro-pyridine-3-carboxylic acid {3-[4-(4-fluoro-phenyl)-piperidin-1-yl]-propyl}-amide	KI	0.4 nM
MK-912	KI	0.42 nM
CHEMBL70751	EC50	0.437 nM
2-(4-Ethylsulfanyl-2,5-dimethoxy-phenyl)-1-methyl-ethylamine	EC50	0.489 nM
2-(2-Amino-ethoxymethyl)-6-ethyl-4-(4-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 5-amide 3-{[3-(4,4-diphenyl-piperidin-1-yl)-propyl]-amide}	KI	0.5 nM
7-Methoxy-3-[4-((E)-3-phenyl-allyl)-piperazin-1-ylmethyl]-3a,4-dihydro-3H-chromeno[4,3-c]isoxazole	KI	0.5 nM
CHEMBL327931	KI	0.525 nM
1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydro-naphthalen-1-yl)-propyl]-piperazine	KI	0.68 nM
1N-{8-[2-hydroxy-(1R,2S,4aR,13bS,14aS)-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroisoquino[3,2-a]b-carbolin-1-ylcarboxamido]octyl}-2-hydroxy-(1R,2S,4aR,13bS,14aS)-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroisoquino[3,2 ; dihydrochloride	KI	0.76 nM
roxindole	IC50	0.8 nM
(R)-4-(3,4-Difluoro-phenyl)-1,2-dimethyl-6-oxo-1,4,5,6-tetrahydro-pyridine-3-carboxylic acid {3-[4-(2-cyano-4-fluoro-phenyl)-piperidin-1-yl]-propyl}-amide	KI	0.8 nM
8-Methoxy-3-[4-((E)-3-phenyl-allyl)-piperazin-1-ylmethyl]-3a,4-dihydro-3H-chromeno[4,3-c]isoxazole	KI	0.8 nM
7,8-Dimethoxy-3-[4-((E)-2-methyl-3-phenyl-allyl)-piperazin-1-ylmethyl]-3a,4-dihydro-3H-chromeno[4,3-c]isoxazole	KI	0.8 nM
1N-{7-[2-hydroxy-(1R,2S,4aR,13bS,14aS)-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroisoquino[3,2-a]b-carbolin-1-ylcarboxamido]heptyl}-2-hydroxy-(1R,2S,4aR,13bS,14aS)-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroisoquino[3, ;dihydrochloride	KI	0.87 nM
3-[4-((E)-3-Phenyl-allyl)-piperazin-1-ylmethyl]-3a,4-dihydro-3H-chromeno[4,3-c]isoxazole	KI	0.9 nM
8-(2,3-Dihydro-benzo[1,4]dioxin-2-ylmethyl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one	KI	1 nM
(R)-4-(3,4-Difluoro-phenyl)-2-methyl-6-oxo-1,4,5,6-tetrahydro-pyridine-3-carboxylic acid {3-[4-cyano-4-(2,4-difluoro-phenyl)-piperidin-1-yl]-propyl}-amide	KI	1 nM
(R)-4-(3,4-Difluoro-phenyl)-1,2-dimethyl-6-oxo-1,4,5,6-tetrahydro-pyridine-3-carboxylic acid {3-[4-cyano-4-(2,4-difluoro-phenyl)-piperidin-1-yl]-propyl}-amide	KI	1.1 nM
CHEMBL91550	KI	1.1 nM
CHEMBL91415	KI	1.1 nM
1N-{12-[2-hydroxy-(1R,2S,4aR,13bS,14aS)-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroisoquino[3,2-a]b-carbolin-1-ylcarboxamido]dodecyl}-2-hydroxy-(1R,2S,4aR,13bS,14aS)-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroisoquino[ ; dihydrochloride	KI	1.2 nM
CHEMBL89685	KI	1.2 nM
2,6-Dimethyl-4-(4-nitro-phenyl)-pyridine-3,5-dicarboxylic acid 3-amide 5-{[3-(4,4-diphenyl-piperidin-1-yl)-propyl]-amide}	KI	1.3 nM
1N-{9-[2-hydroxy-(1R,2S,4aR,13bS,14aS)-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroisoquino[3,2-a]b-carbolin-1-ylcarboxamido]nonyl}-2-hydroxy-(1R,2S,4aR,13bS,14aS)-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroisoquino[3,2 ;dihydrochloride	KI	1.3 nM
1N-{6-[2-hydroxy-(1R,2S,4aR,13bS,14aS)-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroisoquino[3,2-a]b-carbolin-1-ylcarboxamido]hexyl}-2-hydroxy-(1R,2S,4aR,13bS,14aS)-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroisoquino[3,2 ;dihydrochloride	KI	1.4 nM
(R)-4-(3,4-Difluoro-phenyl)-2-methyl-6-oxo-1,4,5,6-tetrahydro-pyridine-3-carboxylic acid {3-[4-cyano-4-(2-cyano-4-fluoro-phenyl)-piperidin-1-yl]-propyl}-amide	KI	1.4 nM
7,8-Dimethoxy-3-[4-((E)-3-phenyl-but-2-enyl)-piperazin-1-ylmethyl]-3a,4-dihydro-3H-chromeno[4,3-c]isoxazole	KI	1.4 nM
(1R,2S,4aR,13bS)-2-Hydroxy-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydro-indolo[2’,3’:3,4]pyrido[1,2-b]isoquinoline-1-carboxylic acid methyl ester	KI	1.4 nM
CHEMBL315914	KI	1.4 nM
CHEMBL47313	KI	1.4 nM
CHEMBL313160	KI	1.5 nM
5-[2-(4-Benzo[d]isothiazol-3-yl-piperazin-1-yl)-ethyl]-6-chloro-1,3-dihydro-indol-2-one	KI	1.6 nM
AGN-190837	EC50	1.6 nM
CHEMBL70691	EC50	1.6 nM
1N-{5-[2-hydroxy-(1R,2S,4aR,13bS,14aS)-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroisoquino[3,2-a]b-carbolin-1-ylcarboxamido]pentyl}-2-hydroxy-(1R,2S,4aR,13bS,14aS)-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroisoquino[3, ;dihydrochloride	KI	1.7 nM

ChEMBL bioactivities

1500 potent at pChembl≥5 of 1645 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.85	IC50	0.014	nM	CHEMBL553231
10.80	IC50	0.016	nM	CHEMBL557985
10.47	IC50	0.034	nM	CHEMBL537830
10.00	Ki	0.1	nM	RAUWOLSCINE
9.96	Ki	0.1096	nM	CHEMBL1256414
9.94	Ki	0.1148	nM	CHEMBL1256414
9.92	IC50	0.12	nM	CHEMBL538801
9.74	Ki	0.182	nM	CHEMBL1255723
9.70	Kd	0.1995	nM	CHEMBL279807
9.70	Kd	0.1995	nM	CHEMBL62912
9.69	Ki	0.2042	nM	CHEMBL1256378
9.62	Ki	0.237	nM	LISURIDE
9.60	IC50	0.25	nM	CHEMBL194837
9.60	Ki	0.2512	nM	CHEMBL5517941
9.60	Ki	0.25	nM	CHEMBL50390
9.59	EC50	0.26	nM	CHEMBL49137
9.59	IC50	0.26	nM	CHEMBL554581
9.56	Ki	0.2754	nM	CHEMBL1256414
9.52	Ki	0.3	nM	RAUWOLSCINE
9.46	Ki	0.3467	nM	CHEMBL1255724
9.40	Ki	0.4	nM	YOHIMBINE
9.40	Ki	0.4	nM	RAUWOLSCINE
9.30	EC50	0.5	nM	ASCORBIC ACID
9.30	AC50	0.5	nM	CEFEPIME
9.29	IC50	0.518	nM	LISURIDE
9.22	Ki	0.6	nM	YOHIMBINE
9.21	IC50	0.61	nM	CHEMBL164540
9.20	Kd	0.631	nM	CHEMBL25554
9.16	Ki	0.6918	nM	CHEMBL1256609
9.11	Ki	0.786	nM	PIPAMAZINE
9.10	Ki	0.8	nM	RAUWOLSCINE
9.09	Ki	0.82	nM	CHEMBL4755913
9.05	Ki	0.9	nM	YOHIMBINE
9.04	Ki	0.912	nM	CHEMBL10332
9.04	Ki	0.912	nM	CHEMBL1255771
9.02	IC50	0.955	nM	CHEMBL351483
8.94	Ki	1.16	nM	YOHIMBINE
8.94	Ki	1.148	nM	CHEMBL1255770
8.92	Ki	1.2	nM	RAUWOLSCINE
8.92	Ki	1.2	nM	CHEMBL298936
8.92	EC50	1.2	nM	CHEMBL298936
8.90	IC50	1.259	nM	CHEMBL163247
8.89	IC50	1.3	nM	CHEMBL189118
8.89	Ki	1.3	nM	RAUWOLSCINE
8.89	Ki	1.3	nM	CHEMBL49137
8.87	IC50	1.349	nM	CHEMBL165350
8.86	Ki	1.396	nM	ERGOCORNINE
8.85	Ki	1.413	nM	CHEMBL10332
8.85	Ki	1.413	nM	BRIMONIDINE
8.85	AC50	1.4	nM	ASENAPINE

PubChem BioAssay actives

1011 with measured affinity, of 3349 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
Naphazoline Hydrochloride	36185: Compound was evaluated for Adrenergic activity against Alpha-2 adrenergic receptor in human platelets	ic50	<0.0001	uM
5-(1-naphthalen-1-ylethyl)-1H-imidazole;hydrochloride	36187: Compound was tested for Adrenergic activity against Alpha-2 adrenergic receptor from rat aorta	ic50	<0.0001	uM
2-(1-naphthalen-2-ylethyl)-4,5-dihydro-1H-imidazole;hydrochloride	36185: Compound was evaluated for Adrenergic activity against Alpha-2 adrenergic receptor in human platelets	ic50	<0.0001	uM
2-(naphthalen-1-ylmethyl)-1H-imidazole;hydrochloride	36185: Compound was evaluated for Adrenergic activity against Alpha-2 adrenergic receptor in human platelets	ic50	<0.0001	uM
2-(1-naphthalen-1-ylethyl)-4,5-dihydro-1H-imidazole;hydrochloride	36185: Compound was evaluated for Adrenergic activity against Alpha-2 adrenergic receptor in human platelets	ic50	<0.0001	uM
5-(1-naphthalen-2-ylethyl)-1H-imidazole;hydrochloride	36185: Compound was evaluated for Adrenergic activity against Alpha-2 adrenergic receptor in human platelets	ic50	0.0001	uM
5-[(1aR,6aR)-1a,6-dihydro-1H-cyclopropa[a]inden-6a-yl]-1H-imidazole	516908: Displacement of [3H]-RX821002 from human adrenergic alpha2B receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting	ki	0.0001	uM
methyl (1S,15S,18S,19S,20S)-18-hydroxy-1,3,11,12,14,15,16,17,18,19,20,21-dodecahydroyohimban-19-carboxylate	36340: Compound was evaluated for inhibition of binding of [3H]rauwolscine to Alpha-2 adrenergic receptor in opossum kidney	ki	0.0001	uM
3-methoxy-12-methylsulfonyl-5,6,8,8a,9,10,11,12a,13,13a-decahydroisoquinolino[2,1-g][1,6]naphthyridine	80588: Ability to reverse inhibitory effects of UK-14304 on the contraction of guinea pig ileum as a measure of alpha-2 adrenergic receptor antagonism.	kd	0.0002	uM
5-[(1S,1aR,6aS)-1-methyl-1a,6-dihydro-1H-cyclopropa[a]inden-6a-yl]-1H-imidazole	516908: Displacement of [3H]-RX821002 from human adrenergic alpha2B receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting	ki	0.0002	uM
5-[(1S,1aR,6aS)-1-ethyl-1a,6-dihydro-1H-cyclopropa[a]inden-6a-yl]-1H-imidazole	516908: Displacement of [3H]-RX821002 from human adrenergic alpha2B receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting	ki	0.0002	uM
(8aR,12aR,13aS)-3-methoxy-12-methylsulfonyl-5,6,8,8a,9,10,11,12a,13,13a-decahydroisoquinolino[2,1-g][1,6]naphthyridine	80588: Ability to reverse inhibitory effects of UK-14304 on the contraction of guinea pig ileum as a measure of alpha-2 adrenergic receptor antagonism.	kd	0.0002	uM
2-(2,4-dichlorophenoxy)-N-[2-[2-(dimethylamino)ethoxy]-4-methylquinolin-6-yl]acetamide	254838: Inhibitory concentration against alpha-2 adrenergic receptor	ic50	0.0003	uM
(3R)-5-chlorospiro[2,4-dihydro-1H-naphthalene-3,2’-5H-1,3-oxazole]-4’-amine	2065718: Binding affinity to human alpha2B-adrenoceptor	ki	0.0003	uM
N-(4,5-dihydro-1H-imidazol-2-yl)-5-methylquinoxalin-6-amine	36513: Compound was tested for concentration that produced 50% contractile response relative to maximum response to norepinephrine for Alpha-2 adrenergic receptor in rabbit vas deferens	ec50	0.0003	uM
2-(1-naphthalen-1-ylethyl)-1H-imidazole;hydrochloride	36185: Compound was evaluated for Adrenergic activity against Alpha-2 adrenergic receptor in human platelets	ic50	0.0003	uM
5-[(1S,1aR,6aS)-1-propyl-1a,6-dihydro-1H-cyclopropa[a]inden-6a-yl]-1H-imidazole	516908: Displacement of [3H]-RX821002 from human adrenergic alpha2B receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting	ki	0.0003	uM
Yohimbine	36499: Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in opossum kidney	ki	0.0004	uM
3-[(6aR,9S)-7-methyl-6,6a,8,9-tetrahydro-4H-indolo[4,3-fg]quinolin-9-yl]-1,1-diethylurea	2060761: Ray2010 Assay 74 from Article : “Psychedelics and the human receptorome.”	ki	0.0005	uM
ascorbic acid	416324: Agonist activity at human adrenergic alpha2B receptor expressed in HEK293 cells coexpressing Gqi5 protein by FLIPR assay	ec50	0.0005	uM
2-(1-naphthalen-2-ylethyl)-1H-imidazole;oxalic acid	36185: Compound was evaluated for Adrenergic activity against Alpha-2 adrenergic receptor in human platelets	ic50	0.0006	uM
N-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)-2-(2,6-dimethoxyphenoxy)ethanamine	1123560: Binding affinity to alpha-adrenergic receptor (unknown origin) in central nervous system	kd	0.0006	uM
5-[(1aR,6S,6aR)-6-methyl-1a,6-dihydro-1H-cyclopropa[a]inden-6a-yl]-1H-imidazole	516908: Displacement of [3H]-RX821002 from human adrenergic alpha2B receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting	ki	0.0007	uM
1-[4-[[4-(4,5-dihydro-1H-imidazol-2-ylamino)phenyl]methyl]phenyl]-2-propylguanidine;dihydrochloride	1728108: Displacement of [3H]-RX821002 from adrenergic alpha 2 receptor in human brain membrane by liquid scintillation spectroscopy	ki	0.0008	uM
2-(3-methoxy-2H-1,4-benzodioxin-3-yl)-4,5-dihydro-1H-imidazole	297456: Displacement of [3H]RX821002 from adrenergic alpha2 receptor in human brain frontal cortex	ki	0.0009	uM
5-[(1aR,6aR)-1a-methyl-1,6-dihydrocyclopropa[a]inden-6a-yl]-1H-imidazole	516908: Displacement of [3H]-RX821002 from human adrenergic alpha2B receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting	ki	0.0009	uM
7-chloro-3-[2-(3,4-dihydro-1H-[1]benzofuro[3,2-c]pyridin-2-yl)ethyl]-2-methylpyrido[1,2-a]pyrimidin-4-one	35399: Binding affinity at human Alpha-2B adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.	ic50	0.0010	uM
5-[(1aR,6aR)-1,1-dimethyl-1a,6-dihydrocyclopropa[a]inden-6a-yl]-1H-imidazole	516908: Displacement of [3H]-RX821002 from human adrenergic alpha2B receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting	ki	0.0011	uM
N-(4,5-dihydro-1H-imidazol-2-yl)-5-methyl-3,4-dihydro-2H-1,4-benzoxazin-6-amine	36513: Compound was tested for concentration that produced 50% contractile response relative to maximum response to norepinephrine for Alpha-2 adrenergic receptor in rabbit vas deferens	ec50	0.0012	uM
7,9-dichloro-3-[2-(3,4-dihydro-1H-[1]benzofuro[3,2-c]pyridin-2-yl)ethyl]-2-methylpyrido[1,2-a]pyrimidin-4-one	35399: Binding affinity at human Alpha-2B adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.	ic50	0.0013	uM
7-bromo-3-[2-(3,4-dihydro-1H-[1]benzofuro[3,2-c]pyridin-2-yl)ethyl]-2-methylpyrido[1,2-a]pyrimidin-4-one	35399: Binding affinity at human Alpha-2B adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.	ic50	0.0013	uM
(E)-N-[2-[2-(dimethylamino)ethyl-methylamino]-4-methylquinolin-6-yl]-3-[4-(trifluoromethoxy)phenyl]prop-2-enamide	254838: Inhibitory concentration against alpha-2 adrenergic receptor	ic50	0.0013	uM
Brimonidine	368170: Binding affinity to alpha2 adrenoceptor in human cortical membrane	ki	0.0014	uM
(3R,3aS)-3-[[4-[(E)-3-(4-fluorophenyl)-2-methylprop-2-enyl]piperazin-1-yl]methyl]-7,8-dimethoxy-3a,4-dihydro-3H-chromeno[4,3-c][1,2]oxazole	288095: Displacement of [3H]rawolscine from human cloned adrenergic alpha-2B receptor transfected in CHO cells	ki	0.0015	uM
3-[2-(3,4-dihydro-1H-[1]benzofuro[3,2-c]pyridin-2-yl)ethyl]-2,7-dimethylpyrido[1,2-a]pyrimidin-4-one	35399: Binding affinity at human Alpha-2B adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.	ic50	0.0015	uM
3-[2-(3,4-dihydro-1H-[1]benzofuro[3,2-c]pyridin-2-yl)ethyl]-2,6-dimethylpyrido[1,2-a]pyrimidin-4-one	35399: Binding affinity at human Alpha-2B adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.	ic50	0.0015	uM
N-(2,6-dichloro-4-iodophenyl)-4,5-dihydro-1H-imidazol-2-amine	36188: Inhibition of [3H]p-aminoclonidine (PAC) binding to alpha-2 adrenergic receptor of purified human platelet plasma membranes	ic50	0.0015	uM
N-[4-[[4-(4,5-dihydro-1H-imidazol-2-ylamino)phenyl]methyl]phenyl]-4,5-dihydro-1H-imidazol-2-amine	1728108: Displacement of [3H]-RX821002 from adrenergic alpha 2 receptor in human brain membrane by liquid scintillation spectroscopy	ki	0.0016	uM
5-[(1aR,6S,6aS)-6-ethyl-1a,6-dihydro-1H-cyclopropa[a]inden-6a-yl]-1H-imidazole	516908: Displacement of [3H]-RX821002 from human adrenergic alpha2B receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting	ki	0.0016	uM
N-pyridin-4-ylisoquinolin-4-amine	2065718: Binding affinity to human alpha2B-adrenoceptor	ki	0.0017	uM
3-[2-(3,4-dihydro-1H-[1]benzofuro[3,2-c]pyridin-2-yl)ethyl]-9-hydroxy-2-methylpyrido[1,2-a]pyrimidin-4-one	35399: Binding affinity at human Alpha-2B adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.	ic50	0.0017	uM
1-[4-[[4-(4,5-dihydro-1H-imidazol-2-ylamino)phenyl]methyl]phenyl]-2-(furan-2-ylmethyl)guanidine;dihydrochloride	1728108: Displacement of [3H]-RX821002 from adrenergic alpha 2 receptor in human brain membrane by liquid scintillation spectroscopy	ki	0.0018	uM
Risperidone	36197: Binding affinity towards human alpha-2 adrenergic receptor	ki	0.0018	uM
Apraclonidine	36512: Compound was tested for concentration that produced 50% contractile relative response to maximum response to norepinephrine for Alpha-2 adrenergic receptor	ec50	0.0019	uM
9-chloro-3-[2-(3,4-dihydro-1H-[1]benzofuro[3,2-c]pyridin-2-yl)ethyl]-2-methyl-7-(trifluoromethyl)pyrido[1,2-a]pyrimidin-4-one	35399: Binding affinity at human Alpha-2B adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.	ic50	0.0019	uM
5-[(1aR,6aS)-spiro[1,1a-dihydrocyclopropa[a]indene-6,1’-cyclopropane]-6a-yl]-1H-imidazole	516908: Displacement of [3H]-RX821002 from human adrenergic alpha2B receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting	ki	0.0019	uM
Dexmedetomidine	2065729: Agonist activity at alpha2B-adrenoceptor (unknown origin) expressed in U2OS-EGFP-NFAT2-alpha2B-AR cells assessed as increase in intracellular calcium level measured after 15 mins incubation by Micro automated microscopy	ec50	0.0019	uM
3-[2-(3,4-dihydro-1H-[1]benzofuro[3,2-c]pyridin-2-yl)ethyl]-9-methoxy-2-methylpyrido[1,2-a]pyrimidin-4-one	35399: Binding affinity at human Alpha-2B adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.	ic50	0.0020	uM
3-[[4-[(E)-3-phenylprop-2-enyl]piperazin-1-yl]methyl]-3a,4-dihydro-3H-chromeno[4,3-c][1,2]oxazole	36227: In vitro binding affinity towards human alpha-2B adrenergic receptor using [3H]rauwolscine	ki	0.0020	uM
3-[2-(3,4-dihydro-1H-[1]benzofuro[3,2-c]pyridin-2-yl)ethyl]-7-iodo-2-methylpyrido[1,2-a]pyrimidin-4-one	35399: Binding affinity at human Alpha-2B adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.	ic50	0.0021	uM

CTD chemical–gene interactions

32 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	increases expression	2
Air Pollutants	increases abundance, increases expression	2
Epinephrine	increases expression, increases reaction, increases phosphorylation, affects binding, increases activity (+2 more)	2
aristolochic acid I	increases expression	1
bisphenol A	increases expression	1
xylometazoline	affects binding, increases activity, increases abundance, decreases reaction	1
butyraldehyde	increases expression	1
S-(1,2-dichlorovinyl)cysteine	affects response to substance, increases expression, affects cotreatment, decreases expression	1
pentanal	increases expression	1
2-methoxyidazoxan	affects binding, decreases reaction	1
licochalcone B	increases expression	1
theaflavin-3,3’-digallate	affects expression	1
Resveratrol	affects cotreatment, decreases expression	1
Sunitinib	increases expression	1
Arsenic Trioxide	decreases expression	1
Acetaminophen	decreases expression	1
Benzo(a)pyrene	decreases expression	1
Cadmium	increases expression	1
Calcium	affects binding, increases abundance, increases activity	1
Clonidine	affects binding, increases activity	1
Diethylhexyl Phthalate	decreases expression	1
Lipopolysaccharides	decreases expression, affects response to substance, increases expression, affects cotreatment	1
Norepinephrine	decreases reaction, affects binding, increases activity, increases abundance	1
Oxymetazoline	affects binding, increases activity, increases abundance, decreases reaction	1
Ozone	increases abundance, increases expression	1
Plant Extracts	affects cotreatment, decreases expression	1
Triclosan	decreases expression	1
Valproic Acid	increases methylation	1
1-Methyl-4-phenylpyridinium	increases expression	1
Aflatoxin B1	increases methylation	1

ChEMBL screening assays

596 unique, capped per target: 466 binding, 123 functional, 5 admet, 2 unclassified

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1016575	Binding	Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2B receptor expressed in CHO cells	Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior. — *J Med Chem*
CHEMBL1016576	Functional	Antagonist activity at human recombinant adrenergic alpha2B receptor expressed in CHO cells	Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior. — *J Med Chem*
CHEMBL1738037	Unclassified	PUBCHEM_BIOASSAY: Late-stage radioligand binding dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen Ki Set 2. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1792, AID1796, AID182	PubChem BioAssay data set

Cellosaurus cell lines

6 cell lines: 3 spontaneously immortalized cell line, 3 cancer cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_9114	L-NGC-alpha2B L-cells	Spontaneously immortalized cell line	Male
CVCL_B8B0	Abcam HCT 116 ADRA2B KO	Cancer cell line	Male
CVCL_B9D2	Abcam A-549 ADRA2B KO	Cancer cell line	Male
CVCL_D2DT	Abcam MCF-7 ADRA2B KO	Cancer cell line	Female
CVCL_H391	CHO-K1/ADRA2B/Gqi5	Spontaneously immortalized cell line	Female
CVCL_KW27	PathHunter CHO-K1 ADRA2B beta-arrestin	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

showing 60 of 600 trials:

NCT	Phase	Status	Title
NCT00004637	Phase 4	COMPLETED	Double-Blind, Placebo-Controlled Trial of Vitamin E as Add-on Therapy for Children With Epilepsy
NCT00043914	Phase 4	COMPLETED	Measurement Of Serum Levels Of Two Antiepileptic Drugs During Conversion In Patients With Epilepsy
NCT00132223	Phase 4	UNKNOWN	Effects on the Diagnostic Accuracy of Magnetic Imaging Angiographies of the Supra-Aortic Vessels by Three Different Magnetic Resonance Contrast Agents in Patients
NCT00133081	Phase 4	UNKNOWN	Study to Improve the Treatment of Epilepsy (SITE)
NCT00137709	Phase 4	UNKNOWN	Hormone Profiles in Adults With Newly Diagnosed Epilepsy
NCT00154076	Phase 4	COMPLETED	A Multicenter Comparative Trial of Zonisamide and Topiramate as Initial Monotherapy in Untreated Epilepsies
NCT00165828	Phase 4	TERMINATED	Efficacy and Safety of an add-on Treatment With Zonisamide in Adults With Focal Epileptic Seizures With or Without Secondary Generalization
NCT00181116	Phase 4	COMPLETED	Levetiracetam for Benign Rolandic Epilepsy
NCT00207935	Phase 4	COMPLETED	Use of Sustained Release Antiepileptic Medication (Depakote® ER) for Pediatric Epilepsy in a Mental Retardation/Developmental Disorder Population
NCT00215592	Phase 4	COMPLETED	Open Label, Zonegran (Zonisamide) In Partial Onset Seizures
NCT00266604	Phase 4	COMPLETED	A Study to Evaluate the Dosing, Effectiveness and Safety of Topiramate for the Treatment of Epilepsy
NCT00288639	Phase 4	COMPLETED	Lyrica (Pregabalin) Administered as an Add-on Therapy for Partial Seizures (LEADER).
NCT00312676	Phase 4	UNKNOWN	Compare Tolerability of an Overnight Switch to Gradual Switch Between Two Different Forms of Depakote
NCT00323947	Phase 4	COMPLETED	Methylphenidate for Treating Attention Deficit Hyperactivity Disorder in Children With Both ADHD and Epilepsy
NCT00385411	Phase 4	COMPLETED	Study of Valproate in Young Patients Suffering From Epilepsy
NCT00522418	Phase 4	TERMINATED	Study Comparing Best Medical Practice With or Without VNS Therapy in Pharmacoresistant Partial Epilepsy Patients
NCT00537940	Phase 4	COMPLETED	Comparative Study Of Pregabalin And Gabapentin As Adjunctive Therapy In Subjects With Partial Seizures
NCT00552526	Phase 4	UNKNOWN	Ketogenic Diet vs.Antiepileptic Drug Treatment in Drug Resistant Epilepsy
NCT00564915	Phase 4	COMPLETED	RCT of the Efficacy of the Ketogenic Diet in the Treatment of Epilepsy
NCT00571155	Phase 4	COMPLETED	Trial of Levetiracetam in Patients With Primary Brain Tumors and Symptomatic Seizures Who Undergo Surgery
NCT00572195	Phase 4	COMPLETED	RNS® System LTT Study
NCT00610532	Phase 4	TERMINATED	Evaluating the Transporter Protein Inhibitor Probenecid In Patients With Epilepsy
NCT00630357	Phase 4	COMPLETED	Trial to Evaluate the Safety and Efficacy of Keppra After Conversion to Mono-therapy in Subjects With Partial Epilepsy
NCT00630630	Phase 4	COMPLETED	Study on Safety and Efficacy of Levetiracetam in the Adjunctive Treatment of Female Subjects With C1 Catamenial Epilepsy
NCT00630968	Phase 4	COMPLETED	S.K.A.T.E.: Safety of Keppra as Adjunctive Therapy in Epilepsy
NCT00631150	Phase 4	COMPLETED	A Phase IV-Pharmacovigilance Study of Keppra Greece - S.K.A.T.E.: Safety of Keppra as Adjunctive Therapy in Epilepsy
NCT00659958	Phase 4	COMPLETED	ZAGAL Study: Evaluating Effectiveness and Tolerability of Zonisamide as Adjunctive Therapy in Patients With Partial Onset Seizures Treated With Two Antiepileptic Drugs
NCT00713622	Phase 4	COMPLETED	Comparing The Effect On Cognition Of Adjunctive Therapy With Zonisamide Versus Sodium Valproate
NCT00807989	Phase 4	COMPLETED	The Efficacy and Safety of Low Dose Combination of LTG and VPA Compared to CBZ Monotherapy
NCT00832884	Phase 4	COMPLETED	The Safety of Intravenous Lacosamide
NCT00869622	Phase 4	COMPLETED	Antiepileptic Drugs and Osteoporotic Prevention Trial
NCT00896987	Phase 4	COMPLETED	Lamotrigine Cognitive Function Study in Adult Untreated Epilepsies
NCT00952081	Phase 4	COMPLETED	A Pilot Study to Evaluate Efficacy and Safety of Clevidipine in Neurosurgical Patients
NCT01118455	Phase 4	TERMINATED	Trial to Assess Vagus Nerve Stimulation Therapy vs. Anti-Epileptic Drug (AED) Treatment in Children With Refractory Seizures
NCT01127165	Phase 4	COMPLETED	Low and High Dose Zonisamide in Children as Monotherapy
NCT01127256	Phase 4	COMPLETED	Comparative Study of Zonisamide and Carbamazepine as an Initial Monotherapy: Efficacy and Safety Evaluation
NCT01140867	Phase 4	COMPLETED	Open-label, Multi-center Trial of Zonisamide as Adjunctive Therapy in Patients With Uncontrolled Partial Epilepsy
NCT01175954	Phase 4	COMPLETED	Cognitive and Behavioral Effects of Lacosamide
NCT01229735	Phase 4	COMPLETED	Levetiracetam Versus Topiramate as Adjunctive Therapy to Evaluate Efficacy and Safety in Subjects With Refractory Partial Onset Seizures
NCT01244724	Phase 4	TERMINATED	Lexapro for Major Depression in Patients With Epilepsy
NCT01309074	Phase 4	WITHDRAWN	Does Pregabalin Improve Symptoms of Anxiety in Patients With Epilepsy? A Comparison With Sertraline
NCT01318408	Phase 4	COMPLETED	Levetiracetam: The Anti-Convulsant of Choice for Elderly Patients With Dementia
NCT01498822	Phase 4	COMPLETED	Levetiracetam Versus Oxcarbazepine as Monotherapy to Evaluate Efficacy and Safety in Subjects With Newly or Recently Diagnosed Partial Epilepsy
NCT01546688	Phase 4	TERMINATED	A Study to Evaluate the Safety and Tolerability and Explore the Efficacy of Zonisamide as add-on Therapy in Elderly Patients With Refractory Partial Seizures
NCT01607346	Phase 4	TERMINATED	An Open Label Study to Evaluate the Effects of Ezogabine/Retigabine Added to Existing Anti-epileptic Drug(s) on Urinary Voiding Function in Subjects With Partial Onset Seizures
NCT01627860	Phase 4	COMPLETED	First Add-on vs. Mono-therapy Study of Topiramate in Neuro-Surgical Patients
NCT01689649	Phase 4	COMPLETED	A Study to Assess Tolerability and Efficacy of Topiramate Monotherapy in Recently Diagnosed Patients With Epilepsy
NCT01713777	Phase 4	COMPLETED	Equivalence Among Antiepileptic Drug Generic and Brand Products in People With Epilepsy: Chronic-Dose 4-Period Replicate Design
NCT01733394	Phase 4	COMPLETED	Equivalence Among Antiepileptic Drug Generic and Brand Products in People With Epilepsy: Single-Dose 6-Period Replicate Design (EQUIGEN Single-Dose Study)
NCT01804322	Phase 4	COMPLETED	Standardized Educational Plan for Epilepsy Patients With Comorbidities
NCT01932502	Phase 4	UNKNOWN	Evaluation of Onfi Conversion Therapy Replacing Clonazepam in Patients With Medically Refractory Epilepsy
NCT01995825	Phase 4	COMPLETED	Lamotrigine Bioequivalence
NCT02100644	Phase 4	COMPLETED	Valproate Dose Reduction and Its Clinical Evaluation by Introducing Lamotrigine in Japanese Women With Epilepsy - Single Arm, Multicenter, and Open-label Study
NCT02178995	Phase 4	COMPLETED	Methylphenidate Treatment of Attention Deficits in Epilepsy
NCT02205931	Phase 4	UNKNOWN	Ketogenic Diet in Infants With Epilepsy (KIWE)
NCT02362373	Phase 4	COMPLETED	Women With Epilepsy: a Pilot Study of PK and PD Anti-epileptic Drug Effects in Levonorgestrel Intrauterine System Users
NCT02404168	Phase 4	COMPLETED	BEEP Follow Up: Evaluation of Repeatability of Lamotrigine Pharmacokinetics in Epileptic Patients
NCT02429596	Phase 4	UNKNOWN	A Trial of Generic Substitution of Antiepileptic Drugs
NCT02633241	Phase 4	COMPLETED	A Pilot Study of Dexmedetomidine-Propofol in Children Undergoing Magnetic Resonance Imaging
NCT02645279	Phase 4	UNKNOWN	Comparison of Oral 30 % Dextrose and iv Midazolam Sedation During MRI in Neonates

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for ADRA2B across ~30M SureChEMBL compounds — explore on Sugi Predict.