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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.
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.
GR 127935 Hydrochloride - CAS 148642-42-6 - Calbiochem 分析证书
标题
批号
508014
参考
参考信息概述
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.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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.
Form
Off-white solid
CAS number
148642-42-6
Chemical formula
C₂₉H₃₁N₅O₃·HCl
Structure formula
Purity
≥98% by HPLC
Solubility
H₂O
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
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.
