SML3692
SSR149415
≥98% (HPLC), selective vasopressin V1b receptor antagonist, powder
别名:
(-)-(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
生化/生理作用
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.).
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
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)
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)
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)
Carol A Dannenhoffer et al.
Psychopharmacology, 235(10), 3065-3077 (2018-08-25)
Adolescent intermittent ethanol exposure (AIE) produces lasting, sex-specific social anxiety-like alterations in male, but not female rats. Oxytocin (OXT) and vasopressin (AVP) brain systems play opposite roles in regulating social preference/avoidance, with OXT increasing approach to, and AVP increasing avoidance
Felix Leroy et al.
Nature, 564(7735), 213-218 (2018-12-07)
Although the hippocampus is known to be important for declarative memory, it is less clear how hippocampal output regulates motivated behaviours, such as social aggression. Here we report that pyramidal neurons in the CA2 region of the hippocampus, which are
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系客户支持