BMY-14802 hydrochloride

• 常用名: BMY-14802 hydrochloride
• 英文名: BMY 14802 hydrochloride
• CAS号: 105565-55-7
• 分子量: 384.85100
• 密度: N/A
• 沸点: 520.8ºC at 760mmHg
• 分子式: C₁₈H₂₃ClF₂N₄O
• 熔点: N/A
• 闪点: 268.8ºC

BMY-14802 hydrochloride用途

BMY-14802盐酸盐(BMY-14802-1)是一种选择性口服活性西格玛受体拮抗剂,IC50为112 nM。BMY-14802盐酸盐也是5-HT1A和肾上腺素能α1受体激动剂。BMY-14802盐酸盐具有抗精神病作用[1][2][3]。

BMY-14802 hydrochloride名称

• 英文名: BMY 14802 hydrochloride,α-(4-Fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanolhydrochloride

BMY-14802 hydrochloride生物活性

• 描述: BMY-14802盐酸盐(BMY-14802-1)是一种选择性口服活性西格玛受体拮抗剂,IC50为112 nM。BMY-14802盐酸盐也是5-HT1A和肾上腺素能α1受体激动剂。BMY-14802盐酸盐具有抗精神病作用[1][2][3]。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体
  研究领域 >> 神经疾病
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> Sigma Receptor
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体
  信号通路 >> 神经信号通路 >> 5-HT受体
• 靶点实验:

  5-HT1A Receptor

  α1-adrenergic receptor

  sigma Receptor:112 nM (IC50)

• 体外研究: 与其他5-HT1A激动剂类似,BMY-14802盐酸盐以5-HT1A敏感的方式影响5-HT能神经元和儿茶酚胺能神经元的放电,并影响5-HT介导的行为。BMY-14802盐酸盐对D2受体缺乏显著亲和力[3]。
• 体内研究: BMY-14802(5 mg/kg、10 mg/kg或20 mg/kg,ip；一次)盐酸盐在4倍剂量范围内对左旋多巴诱导的运动障碍(LID)显示出抗运动障碍功效,并且在减少D1和D2受体激动剂诱导的运动障碍方面也有效。重要的是,在抗LID剂量下,BMY-14802盐酸盐不会影响左旋多巴对病变诱导的运动障碍的疗效[2]。
• 参考文献:

  [1]. J P Yevich, et al. Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. J Med Chem. 1992 Nov 27;35(24):4516-25.

  [2]. Nirmal Bhide, et al. The effects of BMY-14802 against L-DOPA- and dopamine agonist-induced dyskinesia in the hemiparkinsonian rat. Psychopharmacology (Berl). 2013 Jun;227(3):533-44.

  [3]. Melanie A Paquette, 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.

BMY-14802 hydrochloride物理化学性质

• 沸点: 520.8ºC at 760mmHg
• 分子式: C₁₈H₂₃ClF₂N₄O
• 分子量: 384.85100
• 闪点: 268.8ºC
• 精确质量: 384.15300
• PSA: 52.49000
• LogP: 3.19550
• InChIKey: NIBVEFRJDFVQLM-UHFFFAOYSA-N
• SMILES: Cl.OC(CCCN1CCN(c2ncc(F)cn2)CC1)c1ccc(F)cc1
• 蒸汽压: 1.13E-11mmHg at 25°C

BMY-14802 hydrochloride靶点实验

查看更多实验

实验名称：Enzymatic assay of human HDAC6 with commercial peptide substrate 来源：ChEMBL 靶标：Histone deacetylase 6 External Id：CHEMBL4808149

实验名称：Enzymatic assay of human HDAC6 with custom peptide substrate 来源：ChEMBL 靶标：Histone deacetylase 6 External Id：CHEMBL4808150

实验名称：Cell-based high throughput primary assay to identify activators of GPR151 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=G-protein coupled receptor 151; AltName: Full=G-protein coupled receptor PGR7; AltName: Full=GPCR-2037; AltName: Full=Galanin receptor 4; AltName: Full=Galanin-receptor-like protein; Short=GalRL External Id：GPR151_PHUNTER_AG_LUMI_1536_1X%ACT

实验名称：AlphaScreen-based biochemical high throughput primary assay to identify activators of... 来源：The Scripps Research Institute Molecular Screening Center 靶标：N/A External Id：FBW7_ACT_ALPHA_1536_1X%ACT PRUN

实验名称：AlphaScreen-based biochemical high throughput primary assay to identify inhibitors of... 来源：The Scripps Research Institute Molecular Screening Center External Id：MITF_INH_Alpha_1536_1X%INH PRUN

实验名称：Tocris HTS for Inhibitors of Aerobactin Synthetase lucA 来源：23265 External Id：IucA Pilot Assay Tocris Library

共6条，当前第1页，共1页

1