Sarizotan
| 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 |
| 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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