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BMY 14802 hydrochloride Sale

(Synonyms: BMY-14802-1; BMS 181100 hydrochloride) 目录号 : GC13796

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。

BMY 14802 hydrochloride Chemical Structure

Cas No.:105565-55-7

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10mg
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Sample solution is provided at 25 µL, 10mM.

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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.

Chemical Properties

Cas No. 105565-55-7 SDF
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 SMILES FC1=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
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1 mg 5 mg 10 mg
1 mM 2.5983 mL 12.9917 mL 25.9835 mL
5 mM 0.5197 mL 2.5983 mL 5.1967 mL
10 mM 0.2598 mL 1.2992 mL 2.5983 mL
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