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Category:
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7TM Receptors 5-HT Receptors 5-HT2 Receptors 5-HT2C
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Cat.No.
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Product Name
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1379 |
SB 221284
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Price and Availability
Click here for full price details of
SB 221284
Other Information:
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licence
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Chemical Name:
2,3-Dihydro-5-(methylthio)-N-3-pyridinyl-6-(trifluorome
thyl)-1H-indole-1-carboxamide |
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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.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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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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