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Description

A selective 5-HT1A receptor antagonist (pKi = 7.9-9.2). WAY-100635 has been reported to have good inhibitory action centrally and peripherally (1mg/kg dose in rats) but has low intrinsic effects, making it a silent 5-HT1A receptor antagonist. WAY-100635 displaced specific binding of the 5-HT1A radioligand, [3H]8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tetralin), to rat hippocampal membranes with a pIC50 of 8.87. This represented a greater than 100-fold selectivity relative to binding at other 5-HT receptor subtypes and major neurotransmitter receptor, reuptake and ion channel sites. WAY-100635 has been used in a variety of vertebrate species in vivo and in vitro.