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RS 102221 hydrochloride
Other Information:
Sold with
the permission of Roche Bioscience
Chemical Name:8-[5-(2,4-Dimethoxy-5-(4-trifluoromethylphenylsulphonam
ido)phenyl-5-oxopentyl]-1,3,8-triazaspiro[4.5]decane-2,
4-dione hydrochloride
Biological Activity:
Potent and selective 5-HT2C antagonist (pKi
= 8.7). Displays ~ 100-fold selectivity over the 5-HT2A and 5-HT2B
subtypes and is > 100-fold selective over other 5-HT receptors, α- and β-adrenergic and
muscarinic ACh receptors.
Weinhardtet al (1996) Some benzenesulphonamido-substituted
valerophenones that are selective antagonists for the 5-HT2C receptor.
Bioorg.Med.Chem.Lett. 6 2687. Bonhaus et al (1997)
RS-102221: a novel high affinity and selective 5-HT2C receptor
antagonist. Neuropharmacology 36 621. Bonhauset al
(1998) Absorption and brain penetration of a high affinity, highly selective
5-HT2C receptor antagonist, RS-102221. Ann.N.Y.Acad.Sci. 861
269.
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.
