Drug Information

Drug General Information
Drug ID
D0N1GB
Former ID
DIB010078
Drug Name
APD-916
Synonyms
Histamine H3 antagonists (sleep disorder), Arena; Biphenyl derivatives/aryl ethers/anilines (sleep disorder), Arena
Indication Sleep disorders [ICD9: 307.4, 327, 780.5; ICD10:F51, G47] Phase 1 [522988]
Company
Arena Pharmaceuticals Inc
Structure
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2D MOL

3D MOL
Canonical SMILES
O=S(=O)(c1ccc(cc1)c1ccc(cc1)CCN1CCCC1C)NC1CCOCC1
Target and Pathway
Target(s) Histamine H3 receptor Target Info Antagonist [531737]
KEGG Pathway Neuroactive ligand-receptor interaction
Reactome Histamine receptors
G alpha (i) signalling events
WikiPathways Monoamine Transport
GPCRs, Class A Rhodopsin-like
GPCR ligand binding
GPCR downstream signaling
References
Ref 522988ClinicalTrials.gov (NCT01093508) Single-dose Safety Study of APD916 in Healthy Volunteers. U.S. National Institutes of Health.
Ref 531737Identification of biaryl sulfone derivatives as antagonists of the histamine H??receptor: discovery of (R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916). Bioorg Med Chem Lett. 2012 Jan 1;22(1):71-5.

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