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SB 221284

Cat. No. 1379

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Chemical Name: 2,3-Dihydro-5-(methylthio)-N-3-pyridinyl-6-(trifluoromethyl)-1H-indole-1-carboxamide

Biological Activity

Potent, selective 5-HT_2C/2B receptor antagonist. pK_i values are 6.4, 7.9 and 8.6 for 5-HT_2A, _2B and _2C receptors respectively. Centrally active upon systemic administration in vivo.

Licensing Information

Sold under license

Technical Data

M.Wt:

353.36

Formula:

C₁₆H₁₄F₃N₃OS

Solubility:

Soluble to 100 mM in DMSO

Purity:

>99 %

Storage:

Store at +4°C

CAS No:

196965-14-7

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Bromidge et al (1998) Novel and selective 5-HT_2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines. J.Med.Chem. 41 1598. PMID: 9572885.

Bristow et al (2000) Evidence for accelerated desensitisation of 5-HT_2C receptors following combined treatment with fluoxetine and the 5-HT_1A receptor antagonist, WAY 100,635, in the rat. Neuropharmacology 39 1222. PMID: 10760364.

Hutson et al (2000) Activation of mesolimbic dopamine function by phencyclidine is enhanced by 5-HT_2C/2B receptor antagonists: neurochemical and behavioural studies. Neuropharmacology 39 2318. PMID: 10974315.

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