5.08014

GR 127935 Hydrochloride

≥98% (HPLC), 5-HT1B/1D receptor antagonist, solid

• Synonym(s): GR 127935 Hydrochloride, 5-HT _1B/1D Serotonin Receptor Antagonist, GR 127935 Hydrochloride, GR-127935 hydrochloride, GR127935 hydrochloride
• Empirical Formula (Hill Notation): C₂₉H₃₁N₅O₃ · xHCl
• CAS Number: 148642-42-6
• Molecular Weight: 497.59 (free base basis)
• MDL number: MFCD08056244
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Product Name: GR 127935 Hydrochloride,
• assay: ≥98% (HPLC)
• Quality Segment: 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
• SMILES string: Cl.N1(CCN(CC1)c2c(ccc(c2)NC(=O)c3ccc(cc3)c4c(cc(cc4)c5n[o]c(n5)C)C)OC)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

Description

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.

Biochem/physiol Actions

Primary Target
5-HT_1B/1D

Preparation Note

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable