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Merck
CN

S2193

Sigma-Aldrich

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
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
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Assay

>98% (HPLC)

form

solid

color

white

solubility

DMSO: soluble ~14 mg/mL

SMILES string

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

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 Code

13 - Non Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Regulatory Information

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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
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
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

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