Nelivaptan  (Synonyms: SSR-149415)

Nelivaptan (SSR-149415) is a selective and orally active vasopressin V1b Receptor antagonist (K_i: 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].

630.11

C₃₀H₃₂ClN₃O₈S

439687-69-1

Solid

White to off-white

O=S(N(C(C=C1)=C2C=C1Cl)C([C@@]2(C3=CC=CC=C3OC)N4[C@@H](C[C@@H](O)C4)C(N(C)C)=O)=O)(C(C(OC)=C5)=CC=C5OC)=O

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]