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扎托司琼马来酸盐  

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包装规格：100mg in glass bottle
产品描述：基本信息 产品编号： Z10058 产品名称： Zatosetron maleate CAS: 123482-23-5   储存条件 粉末 -20℃ 四年     分子式： C20H24ClN 溶于液体     分子量 313.86     化学名：  5-Chloro-2,3-dihydro-2,2-dimethyl-N-1alphaH,5alphaH-tropan-3alpha-yl-7-benzofurancarboxamide maleate (1:1) Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   生物活性 产品描述 一种血清素再摄取转运体 (SERT) 和去甲肾上腺素再摄取转运体 (NET) 抑制剂，对人的 SERT 和 NET 作用的 Ki 值分别为 3.45nM 和 13.3nM。Amitriptyline hydrochloride 还与多巴胺再摄取转运体 (DAT) 结合，其 Ki 为 2.58μM。 靶点 5-HT3 Receptor 体内研究 Acute administration of 0.1 (n=21) and 0.3 (n=5) mg/kg Zatosetron maleate (Zatosetron) in male rats, but not 0.01, 0.05, 1.0 or 10 mg/kg (n=5, 3, 6 and 4, respectively) Zatosetron maleate or saline (n=5), leads to a significant reduction in the number of spontaneously active A10 dopamine cells. The number of spontaneously active A10 dopamine cells is not significantly different from 30 to 60 min post i.p. Zatosetron maleate (0.1 mg/kg) administration, shows a significant decrease by 60 to 90 min (0.65±0.11, P=0.03, n=5), a larger decrease by 90 to120 min (0.53±0.08, P=0.004, n=5) and remains at this significantly decreased level from 2 to 3 h (0.50+0.05, P=0.0004, n=5). Single-unit recordings show that Zatosetron maleate inhibits the activity of A10 dopamine cells following i.v. administration (ED50=0.12 mg/kg, n=8). Chronic administration of 0.1 mg/kg (n=16) Zatosetron maleate, but not 0.01, 1.0 or 10 mg/kg (n=4, 8 and 7, respectively) Zatosetron maleate or saline (n=5), leads to a significant reduction in the number of spontaneously active A10 dopamine cells .   推荐实验方法(仅供参考) Animal Administration Male rats are used and Zatosetron maleate (Zatosetron) is prepared as an aqueous solution. Acutely treated animals receive i.p. injections of Zatosetron maleate or saline 2 h before electrophysiological recordings; Chronically treated animals receive injections (i.p.) of Zatosetron maleate or saline once daily for 21 days, and receive their last injection 2h before electrophysiological recordings. After completion of nine tracks, some animals are administered either apomorphine HCI (0.14 or 0.01 mg/kg i.v.) or haloperidol (0.1 mg/kg i.v.) and the number of dopamine cells is then counted in three additional tracks.
保存条件：-20℃

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