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123482-23-5

中文名称 123482-23-5
英文名称 Zatosetron Maleate
CAS 123482-23-5
分子式 C23H29ClN2O6
分子量 464.939
MOL 文件 123482-23-5.mol
123482-23-5 结构式 123482-23-5 结构式

基本信息

中文别名
扎托司琼马来酸盐
英文别名
Zatosetron Maleate
5-Chloro-2,3-dihydro-2,2-dimethyl-N-[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octane-3α-yl]benzofuran-7-carboxamide·maleic acid

物理化学性质

熔点184-186 °C
储存条件-20°C储存
溶解度溶于二甲基亚砜

常见问题列表

生物活性
Zatosetron maleate 是一个有效且有选择性的 5HT3 受体拮抗剂。
靶点

5-HT 3 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 (ED 50 =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.

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