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SB 216641 hydrochloride
Other Information:
Sold with the permission of GlaxoSmithKline
Chemical Name:N-[3-[3-(Dimethylamino)ethoxy]-4-methoxyphenyl]-2'-meth
yl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4
-carboxamide hydrochloride
Biological Activity:
A
selective h5-HT1B antagonist with approximately 25-fold selectivity
over h5-HT1D and little or no affinity for a range of other receptor
types.
Haganet al (1997) Stimulation of 5-HT1B receptors
causes hypothermia in the guinea pig. Eur.J.Pharmacol. 331 169. Priceet al (1997) SB-216641 and BRL-15572 - compounds to pharmacologically
discriminate h5-HT1B and h5-HT1D receptors.
Naunyn-Schmied.Arch.Pharmacol. 356 312. Schlickeret al
(1997) Effects of selective h5-HT1B (SB-216641) and 5-HT1D
(BRL-15572) receptor ligands on guinea pig and human 5-HT auto- and
heteroreceptors. Naunyn-Schmied.Arch.Pharmacol. 356 321.
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.