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SSR 149415

Names

[ CAS No. ]:
439687-69-1

[ Name ]:
SSR 149415

[Synonym ]:
Nelivaptan
Nelivaptan [INN]
UNII-3TY57MQ4OA

Biological Activity

[Description]:

Nelivaptan (SSR-149415) is a selective and orally active vasopressin V1b Receptor antagonist (Ki: 3.7 and 1.3 nM for native and recombinant rat V1b receptors, respectively). Nelivaptan inhibits arginine vasopressin (AVP)-induced Ca2+ increase and corticotropin secretion. Nelivaptan can be used for research of stress and anxiety[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Vasopressin Receptor
Research Areas >> Neurological Disease

[References]

[1]. Claudine Serradeil-Le Gal, et al. Characterization of (2S,4R)-1-[5-Chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a Selective and Orally Active Vasopressin V1b Receptor Antagonist. Journal of Pharmacology and Experimental Therapeutics March 2002, 300 (3) 1122-1130.

[2]. Serradeil-Le Gal C, et al. An overview of SSR149415, a selective nonpeptide vasopressin V(1b) receptor antagonist for the treatment of stress-related disorders. CNS Drug Rev. 2005 Spring;11(1):53-68.  

Chemical & Physical Properties

[ Molecular Formula ]:
C30H32ClN3O8S

[ Molecular Weight ]:
630.11

[ Exact Mass ]:
629.16000

[ PSA ]:
134.30000

[ LogP ]:
3.95200

Related Compounds