Pergolide
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Also known as PergolidaSID26754330SID26754331SID90341767SID104171354Pergolide mesylate
Summary
Pergolide (CHEMBL531) is an approved small-molecule antiparkinson drug (ATC N04BC02) targeting HTR6, HTR7, and HTR1A; indicated across 3 conditions including parkinson disease and cocaine dependence.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: N04BC02
- Targets: 16 (HTR6, HTR7, HTR1A…)
- Indications: 3 conditions
- Clinical trials: 8
- Chemistry: 314.5 Da · C19H26N2S
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL531 |
| Name | Pergolide |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 47811 |
| ChEBI | CHEBI:63617 |
| ATC | N04BC02 |
| Molecular formula | C19H26N2S |
| Molecular weight | 314.5 |
| InChIKey | YEHCICAEULNIGD-MZMPZRCHSA-N |
SMILES: CCCN1C[C@@H](C[C@H]2[C@H]1CC3=CNC4=CC=CC2=C34)CSC
IUPAC name: (6aR,9R,10aR)-9-(methylsulfanylmethyl)-7-propyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinoline
ChEBI definition: A diamine that is ergoline in which the β-hydrogen at position 8 is replaced by a (methylthio)methyl group and the hydrogen attached to the piperidine nitrogen (position 6) is replaced by a propyl group. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used as the mesylate salt in the management of Parkinson’s disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction.
Pharmacological roles (ChEBI): antiparkinson drug, dopamine agonist.
Also known as: Pergolida, Pergolide, pergolide, SID26754330, SID26754331, SID90341767, SID104171354, PERGOLIDE, Pergolide mesylate
Parent form; salt/anhydrous children: CHEMBL1275
Patent coverage: 5,530 distinct patent families (23,128 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 23,093 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| HTR6 | 5-HT6 receptor | Full agonist | 7.5 | 0.2% | P50406 |
| HTR7 | 5-HT7 receptor | Full agonist | 9 | 0.8% | P34969 |
| HTR1A | 5-HT1A receptor | Partial agonist | 8.7 | 0% | P08908 |
| DRD1 | D1 receptor | Full agonist | 6.5 | 0% | P21728 |
| DRD2 | D2 receptor | Full agonist | 7.6 | 0% | P14416 |
| DRD3 | D3 receptor | Partial agonist | 8.3 | 0% | P35462 |
| DRD4 | D4 receptor | Partial agonist | 7.2 | 0% | P21917 |
| DRD5 | D5 receptor | Full agonist | 7.5 | 0% | P21918 |
| ADRA2A | α2A-adrenoceptor | Partial agonist | 7.3 | 0.1% | P08913 |
| ADRA2B | α2B-adrenoceptor | Partial agonist | 7.5 | 0.2% | P18089 |
| ADRA2C | α2C-adrenoceptor | Agonist | 7.2 | 0% | P18825 |
| HTR1B | 5-HT1B receptor | Full agonist | 6.6 | 0.2% | P28222 |
| HTR1D | 5-HT1D receptor | Partial agonist | 7.9 | 0% | P28221 |
| HTR2A | 5-HT2A receptor | Full agonist | 8.1 | 0% | P28223 |
| HTR2B | 5-HT2B receptor | Full agonist | 8.2 | 0.4% | P41595 |
| HTR2C | 5-HT2C receptor | Partial agonist | 6.5 | 0% | P28335 |
Broader ChEMBL bioactivity targets: 38 (assay-derived). Sample: 4’-phosphopantetheinyl transferase ffp, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Adrenergic receptor alpha-1, Alpha-2C adrenergic receptor, Histamine H2 receptor, Alpha-2B adrenergic receptor, D(1A) dopamine receptor, Adrenergic receptor alpha-2, Dopamine receptor.
Bioactivity
ChEMBL activities: 105 potent at pChembl ≥ 5 of 111 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| DRD2 | 9.45 | EC50 | 0.35 | nM | CHEMBL_ACT_16879808 |
| DRD2 | 9.21 | Ki | 0.62 | nM | CHEMBL_ACT_25553902 |
| DRD3 | 9.07 | Ki | 0.85 | nM | CHEMBL_ACT_1500317 |
| P61169 | 9 | Ki | 1 | nM | CHEMBL_ACT_412896 |
| P18901 | 8.8 | IC50 | 1.6 | nM | CHEMBL_ACT_1260057 |
| P61169 | 8.8 | IC50 | 1.6 | nM | CHEMBL_ACT_325683 |
| HTR1A | 8.74 | Ki | 1.8 | nM | CHEMBL_ACT_412895 |
| DRD3 | 8.74 | Ki | 1.83 | nM | CHEMBL_ACT_7727836 |
| P19020 | 8.62 | IC50 | 2.41 | nM | CHEMBL_ACT_12456226 |
| P18901 | 8.51 | IC50 | 3.1 | nM | CHEMBL_ACT_1092838 |
| P18901 | 8.51 | IC50 | 3.1 | nM | CHEMBL_ACT_825081 |
| HTR2A | 8.41 | Ki | 3.9 | nM | CHEMBL_ACT_7729974 |
| DRD2 | 8.4 | Ki | 4 | nM | CHEMBL_ACT_118891 |
| DRD3 | 8.4 | Ki | 4 | nM | CHEMBL_ACT_118892 |
| HTR1A | 8.4 | Ki | 4 | nM | CHEMBL_ACT_118893 |
| P61169 | 8.4 | Kd | 4 | nM | CHEMBL_ACT_219411 |
| DRD2 | 8.4 | Ki | 4 | nM | CHEMBL_ACT_25917656 |
| DRD3 | 8.4 | Ki | 4 | nM | CHEMBL_ACT_25917670 |
| P18901 | 8.39 | IC50 | 4.1 | nM | CHEMBL_ACT_1260059 |
| P19020 | 8.37 | EC50 | 4.31 | nM | CHEMBL_ACT_12456198 |
| HTR2A | 8.31 | AC50 | 4.9 | nM | CHEMBL_ACT_25226713 |
| P19020 | 8.29 | IC50 | 5.12 | nM | CHEMBL_ACT_12456215 |
| DRD3 | 8.27 | IC50 | 5.39 | nM | CHEMBL_ACT_7727835 |
| P19020 | 8.25 | IC50 | 5.59 | nM | CHEMBL_ACT_12456253 |
| HTR1A | 8.24 | Ki | 5.7 | nM | CHEMBL_ACT_25917694 |
| P19020 | 8.23 | IC50 | 5.85 | nM | CHEMBL_ACT_12456239 |
| DRD4 | 8.21 | Ki | 6.2 | nM | CHEMBL_ACT_25917679 |
| P61169 | 8.11 | EC50 | 7.86 | nM | CHEMBL_ACT_12456208 |
| HTR2B | 8.08 | AC50 | 8.4 | nM | CHEMBL_ACT_25164298 |
| P19327 | 8.07 | Ki | 8.47 | nM | CHEMBL_ACT_7729970 |
Target pathways
Aggregated over 16 target gene(s): HTR6, HTR7, HTR1A, DRD1, DRD2, DRD3, DRD4, DRD5, ADRA2A, ADRA2B, ADRA2C, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C.
Top Reactome pathways
24 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 11 | ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| Signaling by GPCR | 11 | ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| Class A/1 (Rhodopsin-like receptors) | 11 | ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| Amine ligand-binding receptors | 11 | ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| GPCR ligand binding | 11 | ADRA2A, ADRA2B, ADRA2C, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| GPCR downstream signalling | 10 | ADRA2A, ADRA2B, ADRA2C, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| Serotonin receptors | 8 | HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| G alpha (i) signalling events | 7 | ADRA2A, ADRA2B, ADRA2C, DRD3, DRD4, HTR1B, HTR1D |
| Dopamine receptors | 5 | DRD1, DRD2, DRD3, DRD4, DRD5 |
| G alpha (s) signalling events | 4 | DRD1, DRD5, HTR6, HTR7 |
| Hemostasis | 3 | ADRA2A, ADRA2B, ADRA2C |
| Adrenoceptors | 3 | ADRA2A, ADRA2B, ADRA2C |
| Adrenaline signalling through Alpha-2 adrenergic receptor | 3 | ADRA2A, ADRA2B, ADRA2C |
| G alpha (q) signalling events | 3 | HTR2A, HTR2B, HTR2C |
| G alpha (z) signalling events | 3 | ADRA2A, ADRA2B, ADRA2C |
| Platelet activation, signaling and aggregation | 3 | ADRA2A, ADRA2B, ADRA2C |
| Platelet Aggregation (Plug Formation) | 3 | ADRA2A, ADRA2B, ADRA2C |
| Metabolism | 2 | ADRA2A, ADRA2C |
| Integration of energy metabolism | 2 | ADRA2A, ADRA2C |
| Metabolism of proteins | 2 | ADRA2A, ADRA2C |
| Adrenaline,noradrenaline inhibits insulin secretion | 2 | ADRA2A, ADRA2C |
| Regulation of insulin secretion | 2 | ADRA2A, ADRA2C |
| Surfactant metabolism | 2 | ADRA2A, ADRA2C |
| RHOBTB3 ATPase cycle | 1 | HTR7 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| signal transduction | 16 |
| G protein-coupled receptor signaling pathway | 16 |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | 10 |
| chemical synaptic transmission | 10 |
| G protein-coupled serotonin receptor signaling pathway | 7 |
| intracellular calcium ion homeostasis | 7 |
| positive regulation of MAPK cascade | 6 |
| adenylate cyclase-activating G protein-coupled receptor signaling pathway | 5 |
| response to xenobiotic stimulus | 5 |
| behavioral response to cocaine | 5 |
| phospholipase C-activating dopamine receptor signaling pathway | 5 |
| synaptic transmission, dopaminergic | 5 |
| response to cocaine | 5 |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | 4 |
| vasoconstriction | 4 |
Indications & clinical
Indications
3 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| Parkinson disease | 4 | MONDO:0005180 | MONDO:0005180 |
| cocaine dependence | 3 | MONDO:0005186 | EFO:0002610 |
| drug dependence | 2 | MONDO:0005303 | EFO:0003890 |
Clinical trials
Total trials: 8.
Phase distribution
| Phase | Trials |
|---|---|
| Not specified | 5 |
| PHASE2 | 2 |
| PHASE3 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00000248 | PHASE3 | COMPLETED | Dose Response Trial of Pergolide for Cocaine Dependence - 1 |
| NCT00000215 | PHASE2 | COMPLETED | IV Cocaine Abuse: A Laboratory Model - 4 |
| NCT00000269 | PHASE2 | COMPLETED | Pergolide Treatment for Substance Abusers - 4 |
| NCT00004433 | Not specified | COMPLETED | Randomized Study of Pergolide in Children With Tourette Syndrome |
| NCT00197483 | Not specified | SUSPENDED | Effective Adjunctive Use of Pergolide for Cognitive Impairment and Negative Symptoms in Schizophrenia |
| NCT00252044 | Not specified | UNKNOWN | Pergolide for Cognitive Symptoms in Schizotypal Personality Disorder |
| NCT00624741 | Not specified | NO_LONGER_AVAILABLE | Compassionate Use Study of Pergolide in Patients With Parkinson’s Disease |
| NCT01066403 | Not specified | COMPLETED | Adjuvant Therapy With Pergolide in Treating Cognitive Deficits in Schizophrenia |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
990 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| BREXPIPRAZOLE | ChEMBL + PubChem | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| DIHYDROERGOTAMINE | ChEMBL + PubChem | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| CARIPRAZINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| RISPERIDONE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| CLOZAPINE | ChEMBL + PubChem | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| OLANZAPINE | ChEMBL + PubChem | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| TEGASEROD | ChEMBL + PubChem | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| IMIPRAMINE | ChEMBL | Phase 4 (approved) | ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| NEFAZODONE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| AMOXAPINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| DOXEPIN | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| FLUPHENAZINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| HALOPERIDOL | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| KETANSERIN | ChEMBL | Phase 4 (approved) | ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| LOXAPINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| MIANSERIN | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| PROMAZINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| PENFLURIDOL | ChEMBL | Phase 2 | ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| RITANSERIN | ChEMBL | Phase 2 | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR2A, HTR2C, HTR6, HTR7 |
| PALIPERIDONE | ChEMBL + PubChem | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1B, HTR1D, HTR2A, HTR2C, HTR7 |
| PRAMIPEXOLE | ChEMBL + PubChem | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1B, HTR2A, HTR2B, HTR7 |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| AZELASTINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| CARVEDILOL | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| ERGOTAMINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C, HTR6 |
| KETOTIFEN | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD5, HTR1B, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| QUETIAPINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| SERTINDOLE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1B, HTR2A, HTR2B, HTR2C, HTR6 |
| THIORIDAZINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| THIOTHIXENE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| ZIPRASIDONE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| SPIPERONE | ChEMBL | Phase 2 | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| Pyrazinamide | PubChem | Approved | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| DESLORATADINE | ChEMBL + PubChem | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6 |
| APOMORPHINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR2A, HTR2B, HTR2C |
| ASENAPINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6 |
| BROMOCRIPTINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6 |
| CYPROHEPTADINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| EBASTINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6 |
| ILOPERIDONE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6 |
| MAPROTILINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD5, HTR1A, HTR2A, HTR2B, HTR2C, HTR6 |
| METHYSERGIDE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| PIMOZIDE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6 |
| PROCHLORPERAZINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6 |
| PROMETHAZINE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6 |
| SILODOSIN | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR1B, HTR1D, HTR2B, HTR7 |
| SUNITINIB | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6 |
| VILAZODONE | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD2, DRD3, DRD4, HTR1A, HTR1B, HTR1D, HTR2B, HTR6, HTR7 |
| LISURIDE | ChEMBL | Phase 3 | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C, HTR6 |
| YOHIMBINE | ChEMBL | Phase 3 | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR1B, HTR1D, HTR2A, HTR2B, HTR6 |
| METERGOLINE | ChEMBL | Phase 2 | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| NIGULDIPINE | ChEMBL | Phase 2 | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD5, HTR1A, HTR1B, HTR2C, HTR6, HTR7 |
| SPIRAMIDE | ChEMBL | Phase 2 | ADRA2A, ADRA2B, ADRA2C, DRD2, DRD3, DRD4, HTR1A, HTR1D, HTR2A, HTR2B, HTR6, HTR7 |
| CINACALCET | ChEMBL + PubChem | Phase 4 (approved) | ADRA2B, ADRA2C, DRD2, DRD3, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7 |
| Fidaxomicin | ChEMBL + PubChem | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C |
| Propoxyphene | ChEMBL + PubChem | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C |
| BENPERIDOL | ChEMBL | Phase 4 (approved) | ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2B, HTR2C |
Related Atlas pages
- Genes: HTR6, HTR7, HTR1A, DRD1, DRD2, DRD3, DRD4, DRD5, ADRA2A, ADRA2B, ADRA2C, HTR1B, HTR1D, HTR2A, HTR2B, HTR2C
- Diseases: Parkinson disease, cocaine dependence
- Drugs: Brexpiprazole, Dihydroergotamine, Aripiprazole, Cariprazine, Risperidone, Clozapine, Olanzapine, Tegaserod, Imipramine, Nefazodone, Amoxapine, Chlorpromazine, Doxepin, Fluphenazine, Haloperidol, Ketanserin, Loxapine, Mianserin, Promazine, Paliperidone, Pramipexole, Amitriptyline, Astemizole, Azelastine, Carvedilol, Ergotamine, Ketotifen, Quetiapine, Sertindole, Thioridazine, Thiothixene, Ziprasidone, Pyrazinamide, Desloratadine, Apomorphine, Asenapine, Bromocriptine, Cyproheptadine, Ebastine, Iloperidone, Maprotiline, Methysergide, Pimozide, Prochlorperazine, Promethazine, Silodosin, Sunitinib, Vilazodone, Lisuride, Yohimbine, Cinacalcet, Fidaxomicin, Propoxyphene, Benperidol