Sigma-Aldrich Gr 127935 Hydrochloride

Assay

≥98% (HPLC)

Quality Level

100

Form

solid

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

off-white

Solubility

water: soluble

Storage Temp.

2-8°C

Inchi

1S/C29H31N5O3.ClH/c1-19-17-23(28-30-20(2)37-32-28)9-11-25(19)21-5-7-22(8-6-21)29(35)31-24-10-12-27(36-4)26(18-24)34-15-13-33(3)14-16-34;/h5-12,17-18H,13-16H2,1-4H3,(H,31,35);1H

Inchi Key

SRVVUYIJVBLEJI-UHFFFAOYSA-N

General Description

A selective 5-HT_1B/1Dreceptor 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 wellin vivoand 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.

Biochem/Physiol Actions

Primary Target
5-HT_1B/1D

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

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