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123482-23-5

中文名稱 123482-23-5
英文名稱 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 結(jié)構(gòu)式 123482-23-5 結(jié)構(gòu)式

基本信息

中文別名
扎托司瓊馬來(lái)酸鹽
英文別名
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

物理化學(xué)性質(zhì)

熔點(diǎn)184-186 °C
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜

常見(jiàn)問(wèn)題列表

生物活性
Zatosetron maleate 是一個(gè)有效且有選擇性的 5HT3 受體拮抗劑。
靶點(diǎn)

5-HT 3 Receptor

體內(nèi)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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