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Merck
CN

5.08014

GR 127935 Hydrochloride

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

别名:

GR 127935 Hydrochloride, 5-HT 1B/1D Serotonin Receptor Antagonist, GR 127935 Hydrochloride, GR-127935 hydrochloride, GR127935 hydrochloride

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关于此项目

经验公式(希尔记法):
C29H31N5O3 · xHCl
化学文摘社编号:
分子量:
497.59 (free base basis)
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
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产品名称

GR 127935 Hydrochloride,

assay

≥98% (HPLC)

Quality Level

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

General description

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.

Biochem/physiol Actions

Primary Target
5-HT1B/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)


存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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货号GTIN
508014000104055977242744