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BMY 14802 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMY 14802 hydrochloride图片
CAS NO:105565-55-7
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
BMY 14802 hydrochloride (BMY-14802-1) 是一种选择性和口服活性的 sigma 受体拮抗剂,IC50 为 112 nM。
Cas No.105565-55-7
别名BMY-14802-1; BMS 181100 hydrochloride
化学名(R)-1-(4-fluorophenyl)-4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)butan-1-ol hydrochloride
Canonical SMILESFC1=CN=C(N=C1)N2CCN(CCC[C@H](C(C=C3)=CC=C3F)O)CC2.Cl
分子式C18H22F2N4O.HCl
分子量384.86
溶解度<9.62mg/ml in Water
储存条件Desiccate at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 112 nM for (+)-[3H]-3-PPP

The theoretical role of sigma receptors in psychosis has led to the discovery of selective sigma receptor ligands as potential antipsychotic agents. BMY 14802 is a sigma receptor ligand.

In vitro: BMY 14802 has its most potent binding at the sigma binding site, with some degree of serotonin subtype 1A and negligible dopamine receptor binding [1].

In vivo: BMY 14802 is atypical of standard neuroleptics in that it does not induce catalepsy in rats. In addition, it has been shown to have efficacy in animal models of psychosis [1].

Clinical trial: After 1 week of single-blind placebo treatment, 28 patients were treated with BMY 14802 (up to 3000 mg/day) for up to 4 weeks. However, there was no significant improvement in psychiatric symptoms. There were no changes in involuntary movements, as measured by the Abnormal Involuntary Movement Scale, or in extrapyramidal symptoms as measured by the Simpson-Angus Scale [1].

Reference:
[1] Gewirtz GR, Gorman JM, Volavka J, Macaluso J, Gribkoff G, Taylor DP, Borison R. BMY 14802, a sigma receptor ligand for the treatment of schizophrenia. Neuropsychopharmacology. 1994 Feb;10(1):37-40.