Antazoline

Summary

Antazoline (CHEMBL1305) is an approved small-molecule H1-receptor antagonist (ATC R01AC04); indicated across 2 conditions including allergic disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R01AC04 (+1 more)
• Indications: 2 conditions
• Clinical trials: 2
• Chemistry: 265.35 Da · C17H19N3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1305
Name	Antazoline
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	2200
ChEBI	CHEBI:84115
ATC	R01AC04, R06AX05
Molecular formula	C17H19N3
Molecular weight	265.35
InChIKey	REYFJDPCWQRWAA-UHFFFAOYSA-N

SMILES: C1CN=C(N1)CN(CC2=CC=CC=C2)C3=CC=CC=C3

IUPAC name: N-benzyl-N-(4,5-dihydro-1H-imidazol-2-ylmethyl)aniline

ChEBI definition: A member of the class of imidazolines that is 2-aminomethyl-2-imidazoline in which the exocyclic amino hydrogens are replaced by benzyl and phenyl groups. Antazoline is only found in individuals that have taken the drug.

Pharmacological roles (ChEBI): H1-receptor antagonist, cholinergic antagonist.

Other ChEBI roles (chemical / environmental): xenobiotic.

Also known as: Antaz sulf, Antazolina, Antazoline, Atazoline, Vasocon-a, SID11112519, SID11113348, SID50100471, SID50100472, SID124882433, ANTAZOLINE, ANTAZOLINE PHOSPHATE

Parent form; salt/anhydrous children: CHEMBL1200550, CHEMBL1256819

Patent coverage: 2,441 distinct patent families (9,182 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 23 (assay-derived). Sample: Prelamin-A/C, Inositol monophosphatase 1, Histone-lysine N-methyltransferase 2A, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Thyrotropin receptor, 5-hydroxytryptamine receptor 1A, Alpha-1A adrenergic receptor, Histamine H1 receptor, Mu-type opioid receptor.

Bioactivity

ChEMBL activities: 17 potent at pChembl ≥ 5 of 34 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
LMNA	8.6	Potency	2.5	nM	CHEMBL_ACT_3643800
P31389	7.14	Kd	72.44	nM	CHEMBL_ACT_18289117
P31389	7.14	Kd	72.44	nM	CHEMBL_ACT_18423109
P31389	7.14	Kd	72.44	nM	CHEMBL_ACT_19449080
P31389	7.14	Kd	72.44	nM	CHEMBL_ACT_19487121
ADRA1A	6.47	AC50	340	nM	CHEMBL_ACT_25209090
P97697	6.3	Potency	501.2	nM	CHEMBL_ACT_4828813
PDE3A	5.92	AC50	1200	nM	CHEMBL_ACT_25191405
ADRA1A	5.82	AC50	1528	nM	CHEMBL_ACT_25138319
HRH1	5.66	AC50	2200	nM	CHEMBL_ACT_25213224
CYP2D6	5.6	Potency	2512	nM	CHEMBL_ACT_4998219
CYP2D6	5.6	AC50	2512	nM	CHEMBL_ACT_6019643
ADRA2A	5.59	AC50	2540	nM	CHEMBL_ACT_25157048
ADRA2A	5.54	AC50	2916	nM	CHEMBL_ACT_25156123
SLC6A3	5.29	AC50	5110	nM	CHEMBL_ACT_25125578
PDE6A	5.25	AC50	5684	nM	CHEMBL_ACT_25115942
PDE4D	5.17	AC50	6800	nM	CHEMBL_ACT_25186040

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

2 indications (0 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
allergic disease	2	MONDO:0005271	MONDO:0005271

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 2.

Phase distribution

Phase	Trials
PHASE4	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01527279	PHASE4	COMPLETED	Antazoline in Rapid Cardioversion of Paroxysmal Atrial Fibrillation
NCT05720572	PHASE4	UNKNOWN	Antazoline in Comparison to Propafenone in Pharmacological Cardioversion of Atrial Fibrillation.

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).