General 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.
Biochem/physiol Actions
Primary Target
5-HT1A
Warning
Toxicity: Standard Handling (A)
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.
Other Notes
Hunt, G. E. et al. 2011. Brain Res. Bull.86, 65.
Caamano, R. I. et al. 2010. J. Exp. Biol.213, 1813.
Newman-Tancredi, A. et al. 1998. Naunyn Schmiedebergs Arch. Pharmacol.357, 205.
Forster, E. A. et al. 1995. Eur. J. Pharmacol.281, 81.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51293703
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5081460001
