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5.08014

GR 127935 Hydrochloride

Name: GR 127935 Hydrochloride
Brand: MM

≥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

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About This Item

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

Quality level:

100

Storage condition:

OK to freeze, protect from light

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Properties

Product Name

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

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)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c