中文名 | Zatosetron (maleate) |
英文名 | Zatosetron (maleate) |
别名 | 扎托司琼马来酸盐 化合物 T17285 |
英文别名 | LY 277359 maleate Zatosetron Maleate 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 |
CAS | 123482-23-5 |
化学式 | C23H29ClN2O6 |
分子量 | 464.93916 |
熔点 | 184-186 °C |
溶解度 | DMSO |
存储条件 | -20℃ |
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. |
上游原料 | 3-氯-2-甲基丙烯 氯化亚砜 5-氯-2-羟基苯甲酸甲酯 氫)-1/氫氧化鈉/氫氧化鉀 N-甲基吡咯烷酮 |
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