A selective 5-HT1B/1D receptor antagonist. Selectivity was found to be similar for B (pki = 9.2-9.8 )and D (pki = 8.6-9.1) receptor types. GR 127935 works well in vivo and was shown to block (+)-MDMA-induced hyperactivity in rats. It alters release of serotonin in the brain, as well as reducing drug-seeking behaviour in cocaine addicted rats. In transformed rat C5 glioma cells, this inhibitor blocked 5HT with an IC50 = 97 pM.
Toxicity: Standard Handling (A)
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Rex, A. et al. 2008. Pharmacology, Biochemistry, and Behavior.88, 196.
Przegalinski, E. et al. 2008. Pharmacol. Rep.60, 798.
Bannai, M. et al. 2007. Psychopharmacol.93, 295.
McCreary A. C. et al. 1999. J. Pharmacol. Exp. Ther.290, 965.
Pauwels, P. J. et al. 1996. J. Neurochem.66, 65.
Skingle, M. et al. 1996. Behav.Brain Res.73, 157.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany