Biochem/physiol Actions

Primary Target5-HT_1B/1D

General description

A selective 5-HT_1B/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.

Legal Information

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

Other Notes

Rex, A. et al. 2008. Pharmacology, Biochemistry, and Behavior.88, 196.r>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.r>Pauwels, P. J. et al. 1996. J. Neurochem.66, 65. Skingle, M. et al. 1996. Behav.Brain Res.73, 157.

Packaging

10 mg in Glass bottle

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)