alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine butanol

Names

[ Name ]:
alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine butanol

[Synonym ]:
1-[4-(4-fluorophenyl)-4-hydroxybutyl]-4-(5-fluoropyrimidin-2-yl)-piperazine
α-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine-butanol hydrochloride
BMS-181100
α-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine butanol monohydrochloride
BMY-14802
BMY 14802
1-(4-Fluoro-phenyl)-4-[4-(5-fluoro-pyrimidin-2-yl)-piperazin-1-yl]-butan-1-ol

Biological Activity

[Description]:

BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM[1][2].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Sigma Receptor

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

Sigma 1 Receptor

5-HT1A Receptor

α1-adrenergic receptor

[In Vivo]

BMY 14802 (15 mg/kg；腹腔注射；单次剂量) 在大鼠 PD 模型中显著抑制 AIM 并减少运动障碍，尤其是在处理后的第一个小时[1][2]。

[References]

[1]. Paquette MA, et al. The sigma-1 antagonist BMY-14802 inhibits L-DOPA-induced abnormal involuntary movements by a WAY-100635-sensitive mechanism. Psychopharmacology (Berl). 2009 Jul;204(4):743-54.

[2]. Paquette MA, et al. Sigma ligands, but not N-methyl-D-aspartate antagonists, reduce levodopa-induced dyskinesias. Neuroreport. 2008 Jan 8;19(1):111-5.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₈H₂₂F₂N₄O

[ Molecular Weight ]:
348.39000

[ Exact Mass ]:
348.17600

[ PSA ]:
52.49000

[ LogP ]:
2.39350