Drug General Information
Drug ID
D0E2IN
Former ID
DIB002021
Drug Name
LECOZOTAN HYDROCHLORIDE
Synonyms
Lecozotan hydrochloride < USAN; Prop INNM >; SRA-333; 4-Cyano-N-[2(R)-[4-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazin-1-yl]propyl]-N-(2-pyridyl)benzamide hydrochloride
Drug Type
Small molecular drug
Indication Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10:F01-F07, F04, F05, R41.3] Phase 2/3 [521788]
Structure
Download
2D MOL

3D MOL

Formula
C28H30ClN5O3
Canonical SMILES
C[C@H](CN(C(=O)c1ccc(cc1)C#N)c2ccccn2)N3CCN(CC3)c4cccc5<br />OCCOc45
InChI
1S/C28H29N5O3/c1-21(31-13-15-32(16-14-31)24-5-4-6-25-27(24)36-18-17-35-25)20-33(26-7-2-3-12-30-26)28(34)23-10-8-22(19-29)9-11-23/h2-12,21H,13-18,20H2,1H3/t21-/m1/s1
InChIKey
NRPQELCNMADTOZ-OAQYLSRUSA-N
PubChem Compound ID
Target and Pathway
Target(s) 5-hydroxytryptamine 1A receptor Target Info Antagonist [528845], [551871]
KEGG Pathway cAMP signaling pathway
Neuroactive ligand-receptor interaction
Serotonergic synapse
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
5HT1 type receptor mediated signaling pathway
Reactome Serotonin receptors
G alpha (i) signalling events
WikiPathways Serotonin HTR1 Group and FOS Pathway
SIDS Susceptibility Pathways
Monoamine GPCRs
GPCRs, Class A Rhodopsin-like
GPCR ligand binding
GPCR downstream signaling
References
Ref 521788ClinicalTrials.gov (NCT00277810) Study Evaluating the Safety, Tolerability, and Efficacy of Lecozotan SR in Outpatients With Alzheimer's Disease. U.S. National Institutes of Health.
Ref 528845A positron emission tomography study to assess binding of lecozotan, a novel 5-hydroxytryptamine-1A silent antagonist, to brain 5-HT1A receptors in healthy young and elderly subjects, and in patientswith Alzheimer's disease. Clin Pharmacol Ther. 2008 Jan;83(1):86-96. Epub 2007 May 16.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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