SKF 83959 hydrobromide

• 常用名: SKF 83959 hydrobromide
• 英文名: SKF 83959 hydrobromide
• CAS号: 67287-95-0
• 分子量: 398.72200
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₈H₂₁BrClNO₂
• 熔点: N/A
• 闪点: N/A

SKF 83959 hydrobromide用途

SKF83959氢溴酸盐是一种有效的选择性多巴胺D1样受体部分激动剂。大鼠D1、D5、D2和D3受体的SKF83959氢溴酸钾Ki值分别为1.18、7.56、920和399 nM。SKF83959氢溴酸盐是西格玛(σ)-1受体的有效变构调节剂。氢溴酸SKF83959属于苯扎地平家族,对认知功能障碍有改善作用。SKF83959氢溴酸盐可用于阿尔茨海默病和抑郁症的研究[1][2][3][4]。

SKF 83959 hydrobromide名称

• 英文名: 6-Chloro-3-methyl-1-(3-methylphenyl)-2,3,4,5-tetrahydro-1H-3-benz azepine-7,8-diol hydrobromide (1:1)

SKF 83959 hydrobromide生物活性

• 描述: SKF83959氢溴酸盐是一种有效的选择性多巴胺D1样受体部分激动剂。大鼠D1、D5、D2和D3受体的SKF83959氢溴酸钾Ki值分别为1.18、7.56、920和399 nM。SKF83959氢溴酸盐是西格玛(σ)-1受体的有效变构调节剂。氢溴酸SKF83959属于苯扎地平家族,对认知功能障碍有改善作用。SKF83959氢溴酸盐可用于阿尔茨海默病和抑郁症的研究[1][2][3][4]。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体
  信号通路 >> 神经信号通路 >> 多巴胺受体
  研究领域 >> 神经疾病
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> Sigma Receptor
• 靶点实验:

  D1 Receptor:1.18 nM (Ki)

  D5 Receptor:7.56 nM (Ki)

  D2 Receptor:920 nM (Ki)

  D3 Receptor:399 nM (Ki)

  sigma (σ)-1

• 体外研究: SKF83959氢溴酸盐(10~250μM)刺激膜中PIP2水解。SKF83959氢溴酸盐(0.1~10μM；PC12细胞)将对照组织中SKF81297的EC50值从0.5 nM改变为31.6 nM、251.2 nM和631.0 nM[2]。
• 体内研究: SKF83959氢溴酸钾(0.5和1 mg/kg；i、 p。；1小时)逆转被动回避任务和Y-迷宫测试中东莨菪碱引起的认知损害[1]。SKF83959氢溴酸钾(1 mg/kg；i、 p。；脑源性神经营养因子系统阻断可阻止诱导的记忆增强效应[1]。氢溴酸SKF83959具有抗健忘症活性,可恢复小鼠海马中东莨菪碱减少的BDNF信号通路[1]。动物模型：雄性ICR雄性小鼠(8周)[1]剂量：0.5和1mg/kg给药：腹腔注射。；1小时结果：在被动回避任务和Y-迷宫测试中逆转东莨菪碱诱导的认知损害。动物模型：雄性ICR雄性小鼠(8周)[1]剂量：1mg/kg给药：腹腔注射。；结果：脑源性神经营养因子(BDNF)系统阻断可抑制记忆增强效应。
• 参考文献:

  [1]. Sheng G, et al. SKF83959 Has Protective Effects in the Scopolamine Model of Dementia. Biol Pharm Bull. 2018;41(3):427-434.

  [2]. Jin LQ, et al. SKF83959 selectively regulates phosphatidylinositol-linked D1 dopamine receptors in rat brain. J Neurochem. 2003;85(2):378-386.

  [3]. Neumeyer JL, et al. Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines. Eur J Pharmacol. 2003;474(2-3):137-140.

  [4]. Guo L, et al. SKF83959 is a potent allosteric modulator of sigma-1 receptor. Mol Pharmacol. 2013;83(3):577-586.

SKF 83959 hydrobromide物理化学性质

• 分子式: C₁₈H₂₁BrClNO₂
• 分子量: 398.72200
• 精确质量: 397.04400
• PSA: 43.70000
• LogP: 4.57540
• InChIKey: FHYWNBUFNGHNCP-UHFFFAOYSA-N
• SMILES: Br.Cc1cccc(C2CN(C)CCc3c2cc(O)c(O)c3Cl)c1

SKF 83959 hydrobromide安全信息

• WGK德国: 3

SKF 83959 hydrobromide靶点实验

查看更多实验

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SKF 83959 hydrobromide英文别名

• 6-chloro-9H-purine-2-sulfonyl fluoride
• 2-fluorosulfonyl-6-chloropurine
• 6-chloranyl-7H-purine-2-sulfonyl fluoride
• 6-Chlor-purin-2-sulfonylfluorid
• 6-Chloro-1H-Purine-2-sulfonyl fluoride