Sarizotan

  • 化学数据
CAS号 351862-32-3 货号 BCP24751
中文名 Sarizotan
英文名 Sarizotan
中文别名
英文别名 EMD-128130; EMD128130; EMD 128130; EMD-77697; EMD-77697; EMD-77697;
分子式 C22H21FN2O 分子量 348.41
  • 用途
生物活性 Sarizotan is a Dopamine D2 receptor partial agonist and Serotonin 1A receptor agonist. Sarizotan exhibits affinity at serotonin and dopamine receptors. Sarizotan effectively suppresses levodopa-induced dyskinesia in primate and rodent models of Parkinson's disease, and tardive dyskinesia in a rodent model. Sarizotan is a full agonist at D3 and D4.4 receptors (EC50=5.6 and 5.4 nM, respectively) but a partial agonist at D2S, D2L and D4.2 receptors (EC50=29, 23 and 4.5 nM, respectively). Sarizotan is an antagonist at D2S and D2L receptors (IC50=52 and 121 nM, respectively). Sarizotan is a full agonist at D2L, D3, D4.2 and D4.4 receptors (EC50=0.51, 0.47, 0.48 and 0.23 nM, respectively) but a partial agonist at D2S receptors (EC50=0.6 nM).
信号通路 Neuro Signaling Pathway GPCR/G Protein 
靶 点 5 HT Receptor/Serotonin Receptor 

结构式

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