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Chemical Name:3,5-Dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']di
pyrrole-1(2H)-carboxamide hydrochloride
Biological Activity:
Potent
and selective 5-HT2B/5-HT2C receptor antagonist (rat 5-HT2B
pA2 = 8.89, human 5-HT2C pKi = 7.92). Displays
> 80-fold selectivity over all other 5-HT receptor subtypes and a variety of
other receptors (pKi < 6). Centrally active following oral
administration in vivo.
Forbes et al (1995)
5-Methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrrolo[2,3-f]indole: a novel
5-HT2C/5-HT2B receptor antagonist with improved affinity,
selectivity and oral activity. J.Med.Chem. 38 2524. Kennettet al (1996) In vitro and in vivo profile of SB 206553, a
potent 5-HT2C/5-HT2B receptor antagonist with
anxiolytic-like properties. Br.J.Pharmacol. 117 427. Porraset al (2002) 5-HT2A and 5-HT2C/2B receptor
subtypes modulate dopamine release induced in vivo by amphetamine and morphine
in both the rat nucleus accumbens and striatum. Neuropsychopharmacology 26
311.
Selective 5-HT7 receptor antagonist that displays > 100-fold selectivity over a range of other receptors. Reverses the hypothermic effect of 5-CT in mice following i.p. administration.
