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.
生化/生理作用
Primary Target 5-HT1B/1D
警告
Toxicity: Standard Handling (A)
重構
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他說明
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.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany