Biochem/physiol Actions

Primary Target5-HT_1A

General description

A selective 5-HT_1A 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-HT_1A receptor antagonist. WAY-100635 displaced specific binding of the 5-HT_1A 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Hunt, G. E. et al. 2011. Brain Res. Bull.86, 65.r>Caamano, R. I. et al. 2010. J. Exp. Biol.213, 1813. r>Newman-Tancredi, A. et al. 1998. Naunyn Schmiedebergs Arch. Pharmacol.357, 205.Forster, E. A. et al. 1995. Eur. J. Pharmacol.281, 81.

Packaging

10 mg in Glass bottle

Preparation Note

Warming is required for complete solubilization.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)