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Merck
CN

S2193

SB-221284

>98% (HPLC), solid

别名:

5-(Methylthio)-1-(3-pyridylcarbamoyl)-6-(trifluoromethyl)indoline

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关于此项目

经验公式（希尔记法）:
C16H14N3F3OS
化学文摘社编号:
196965-14-7
分子量:
353.36
UNSPSC Code:
12352200
PubChem Substance ID:
24724604
MDL number:
MFCD00950075

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SMILES string

CSc1cc2CCN(C(=O)Nc3cccnc3)c2cc1C(F)(F)F

assay

>98% (HPLC)

form

solid

color

white

solubility

DMSO: soluble ~14 mg/mL

Gene Information

human ... CYP1A2(1544), CYP2C19(1557), CYP2C9(1559), CYP2D6(1565), CYP3A4(1576), HTR2A(3356), HTR2B(3357), HTR2C(3358)

Application

SB-221284 was administered to rats to study the effect of 5-HT2C receptor-mediated signaling in escape behavior.

Biochem/physiol Actions

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.

Legal Information

Sold for research purposes under agreement from Glaxo­Smith­Kline

存储类别

13 - Non Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
053K4611

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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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