S2193
SB-221284
>98% (HPLC), solid
Synonym(s):
5-(Methylthio)-1-(3-pyridylcarbamoyl)-6-(trifluoromethyl)indoline
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About This Item
Empirical Formula (Hill Notation):
C16H14N3F3OS
CAS Number:
Molecular Weight:
353.36
UNSPSC Code:
12352200
PubChem Substance ID:
MDL number:
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
Storage Class
13 - Non Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
Regulatory Information
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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
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
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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