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SB 200646 hydrochloride
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Chemical Name:N-(1-Methyl-1H-indol-5-yl)-N'-3-pyridinylurea
Biological Activity:
5-HT2C/2B receptor antagonist, selective over 5-HT1A.
Affinities are 7.4 (pA2), 6.9 (pKi) and 5.2 (pKi)
for 5-HT2B, 2C and 2A respectively. Orally
active in vivo.
Forbeset al (1993) N-(1-Methyl-5-indolyl)-N¢-(3-pyridyl)urea
hydrochloride: the first selective 5-HT1C receptor antagonist.
J.Med.Chem. 36 1104. Kennettet al (1994) In
vivo properties of SB 200646A, a 5-HT2C/2B recepor antagonist.
Br.J.Pharmacol. 111 797. Kennettet al (1995)
Effect of SB 200646A, a 5-HT2C/5-HT2B receptor
antagonist, in two conflict models of anxiety. Psychopharmacol. 118
178.
Dual serotonin / noradrenaline reuptake inhibitor that displays ~ 30-fold higher affinity for SERT than NET (Ki values are 82 and 2480 nM respectively). Anti-depressant; increases swimming and climbing behaviour in the forced-swim test in rats.
