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BMY 14802 hydrochloride Catalog No.GC13796

Sigma receptor antagonist

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 105565-55-7 SDF
Chemical Name (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
Formula C18H22F2N4O.HCl M.Wt 384.86
Solubility <9.62mg/ml in H2O Storage Desiccate at RT
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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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].

[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.