S2193
SB-221284
>98% (HPLC), solid
别名:
5-(Methylthio)-1-(3-pyridylcarbamoyl)-6-(trifluoromethyl)indoline
方案
>98% (HPLC)
表单
solid
颜色
white
溶解性
DMSO: soluble ~14 mg/mL
SMILES字符串
CSc1cc2CCN(C(=O)Nc3cccnc3)c2cc1C(F)(F)F
基因信息
human ... CYP1A2(1544), CYP2C19(1557), CYP2C9(1559), CYP2D6(1565), CYP3A4(1576), HTR2A(3356), HTR2B(3357), HTR2C(3358)
应用
SB-221284 was administered to rats to study the effect of 5-HT2C receptor-mediated signaling in escape behavior.
生化/生理作用
5-HT2B/2C serotonin receptor antagonist.
SB-221284 inhibits the centrally-mediated hypolocomotion induced by m-chlorophenylpiperazine, an agonist of 5-HT2C/2B when administered orally. It exhibits anxiolytic-like activity and may be effective in treatment of anxiety, depression and psychiatric syndromes.
法律信息
Sold for research purposes under agreement from GlaxoSmithKline
储存分类代码
13 - Non Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
法规信息
新产品
此项目有
Nicholas Jones et al.
Psychopharmacology, 164(2), 214-220 (2002-10-31)
m-Chlorophenylpiperazine (mCPP) induces panic in humans and dose dependently increases unconditioned escape behaviour in a novel pre-clinical model of extreme anxiety in rats, the unstable elevated exposed plus maze (UEEPM). Numerous studies indicate that the anxiogenic effects of mCPP may
F Jenck et al.
Expert opinion on investigational drugs, 7(10), 1587-1599 (2005-07-05)
5-HT(2C) receptors are predominantly localised in the brain and their dysregulation may contribute to particular symptoms of anxiety and depression. The marked affinity of several clinically established psychotropic agents sites (e.g., tricyclic antidepressants, clozapine, fluoxetine) for 5-HT(2C) receptor has generated
S M Bromidge et al.
Journal of medicinal chemistry, 43(6), 1123-1134 (2000-03-29)
The evolution, synthesis, and biological activity of a novel series of 5-HT(2C) receptor inverse agonists are reported. Biarylcarbamoylindolines have been identified with excellent 5-HT(2C) affinity and selectivity over 5-HT(2A) receptors. In addition, (pyridyloxypyridyl)carbamoylindolines have been discovered with additional selectivity over
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