Molecule Details
InChIKeyQOIGKGMMAGJZNZ-UHFFFAOYSA-N
Compound NameGepirone
Canonical SMILESCC1(C)CC(=O)N(CCCCN2CCN(c3ncccn3)CC2)C(=O)C1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)2
Pfam Stratification Homologous
Avg pChEMBL7.37
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB12184
Drug NameGepirone
CAS Number83928-76-1
Groups approved
ATC Codes N06AX19
DescriptionGepirone, an azapirone, is a pharmacologic analog of [buspirone] that acts selectively on the pre- and post-synaptic 5HT<sub>1A</sub> receptors. Although earlier clinical trials showed promising results for gepirone, its formulation as an immediate-release tablet necessitates frequent administration...

Categories: Anti-Anxiety Agents Antidepressive Agents Central Nervous System Agents Central Nervous System Depressants Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 Substrates Nervous System Neurotransmitter Agents Psychoanaleptics Psychotropic Drugs Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome Serotonin Agents Serotonin Receptor Agonists Tranquilizing Agents
Cross-references: BindingDB: 50005132 ChEBI: 135990 CHEMBL284092 ChemSpider: 49836 PubChem:55191 PubChem:347828470 RxCUI: 2672253 Wikipedia: Gepirone ZINC: ZINC000002021499
Target Activities (2)
Target Gene Organism Category Pfam pChEMBL Type Source
P08908 HTR1A Homo sapiens Human PF00001 7.5 Ki ChEMBL;BindingDB
P14416 DRD2 Homo sapiens Human PF00001 7.2 Ki ChEMBL;BindingDB
DrugBank Target Actions (3)
Target Gene Target Name Action Type
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P08908 HTR1A 5-hydroxytryptamine receptor 1A agonist targets
P08908 HTR1A 5-hydroxytryptamine receptor 1A partial agonist targets