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Category: 7TM Receptorsarrow5-HT Receptorsarrow5-HT2 Receptorsarrow5-HT2C
Cat.No. Product Name
1379 SB 221284
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SB 221284

Other Information:

Sold under licence
Chemical Name: 2,3-Dihydro-5-(methylthio)-N-3-pyridinyl-6-(trifluorome thyl)-1H-indole-1-carboxamide

Biological Activity:

Potent, selective 5-HT2C/2B receptor antagonist. pKi values are 6.4, 7.9 and 8.6 for 5-HT2A, 2B and 2C receptors respectively. Centrally active upon systemic administration in vivo.

Technical Data:

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M.Wt: 353.36
Formula: C16H14F3N3OS
Storage: Store at +4°C
Solubility: Soluble to 100 mM in DMSO
Purity: >99%
CAS No: [196965-14-7]

Resources:

  • Certificate of Analysis / MSDS:

    Certificate of Analysis: View current batch
    Product/Material Safety Data Sheet: View current batch

    References:

    Bromidge et al (1998) Novel and selective 5-HT2C/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. Hutson et al (2000) Activation of mesolimbic dopamine function by phencyclidine is enhanced by 5-HT2C/2B receptor antagonists: neurochemical and behavioural studies. Neuropharmacology 39 2318. Bristow et al (2000) Evidence for accelerated desensitisation of 5-HT2C receptors following combined treatment with fluoxetine and the 5-HT1A receptor antagonist, WAY 100,635, in the rat. Neuropharmacology 39 1222.
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    Keywords: SB 221284, 5-HT Receptors, Potent, Selective 5-HT2C / 2B Antagonist, SB221284, Tocris Bioscience

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