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Merck
CN

SML3692

SSR149415

≥98% (HPLC), selective vasopressin V1b receptor antagonist, powder

Synonym(s):

(-)-(2S,4R)-1-[5-Chloro-1-[(2,4-dimethoxyphenyl)sulphonyl]-3-(2-methoxyphenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine-carboxamide, (2S,4R)-1-[(3R)-5-Chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-2,3-dihydro-3-(2-methoxyphenyl)-2-oxo-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidinecarboxamide, Nelivaptan, SSR 149415, SSR-149415

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About This Item

Empirical Formula (Hill Notation):
C30H32ClN3O8S
CAS Number:
439687-69-1
Molecular Weight:
630.11
UNSPSC Code:
51111800
NACRES:
NA.21
MDL number:
MFCD06199090

Key Documents

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Product Name

SSR149415, ≥98% (HPLC)

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Quality Level

100

Related Categories

Biochem/physiol Actions

Orally active, selective vasopressin V1b receptor antagonist in vitro and in vivo.
SSR149415 is an orally active, selective vasopressin V1b receptor antagonist (human/rat Ki in nM = 1.5/1.3/V1b, 91/1050/V1a, 1412/2897/V2, 174/270/OT) that inhibits 30 nM AVP-induced Ca2+ response in human and rat V1b CHO transfectants (Ki = 1.26/2.0 nM). SSR149415 suppresses AVP-mediated physiological responses in vivo, including corticotropin secretion (1-30 mg/kg p.o. or i.p. in rats) upon exogenous AVP administration (0.3 µg/kg alone or 0.03 µg/kg with 0.1 µg corticoliberin/kg via i.v.), restraint stress-Induced corticotropin secretion (EC50 = 10 mg/kg i.p. in rats), and in a murine model of anxiety (four-plate test; 1-10 mg/kg i.p. or 3-10 mg/kg p.o. acute or 10 mg/kg/day p.o.).

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000289654
0000289655
0000289655
0000289654
0000266887

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V1b Receptor Antagonist SSR149415 and Naltrexone Synergistically Decrease Excessive Alcohol Drinking in Male and Female Mice
Alcohol, clinical & experimental research, 42(1), 195-205 (2018)
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, 300(3), 1122-1130 (2002)
Differential activation of arginine-vasopressin receptor subtypes in the amygdaloid modulation of anxiety in the rat by arginine-vasopressin
Psychopharmacology, 235(4), 1015-1027 (2018)
The role of the vasopressin system and dopamine D1 receptors in the effects of social housing condition on morphine reward
Drug and Alcohol Dependence, 188, 113-118 (2018)
Identification of avian vasotocin receptor subtype-specific antagonists involved in the stress response of the chicken, Gallus gallus
Journal of Biomolecular Structure & Dynamics, 37(7), 1685-1699 (2019)
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