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
产品名称
GR 127935 Hydrochloride,
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
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
water: soluble
Quality Level
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
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.
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
法规信息
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