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卡他唑酯(SQ 65,396)在猴体内的生物转化,卡他唑酯是一种具有抗焦虑活性的取代吡唑并吡啶。

Biotransformation in the monkey of cartazolate (SQ 65,396), a substituted pyrazolopyridine having anxiolytic activity.

作者信息

Kripalani K J, Dreyfuss J, Nemec J, Cohen A I, Meeker F, Egli P

出版信息

Xenobiotica. 1981 Jul;11(7):481-8. doi: 10.3109/00498258109045858.

DOI:10.3109/00498258109045858
PMID:6117154
Abstract
  1. The metabolism of cartazolate (SQ 65,396), an anxiolytic agent, was studied in four male rhesus monkeys after oral administration. 2. Seven metabolites were identified in the pooled urine of the four monkeys. These resulted from a combination of (1) hydrolysis of the 5-carboxylic acid ethyl ester; (2) N-de-ethylation of the pyrazole ring; (3) gamma-hydroxylation of the n-butylamino side-chain; (4) removal of the n-butyl group; and (5) conjugation with beta-glucuronic acid.
摘要
  1. 对4只雄性恒河猴口服抗焦虑药卡他唑酯(SQ 65,396)后的代谢情况进行了研究。2. 在4只猴子的混合尿液中鉴定出了7种代谢物。这些代谢物是由以下几种情况组合而成的:(1)5-羧酸乙酯的水解;(2)吡唑环的N-脱乙基化;(3)正丁基氨基侧链的γ-羟基化;(4)正丁基的去除;以及(5)与β-葡萄糖醛酸的结合。

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Biotransformation in the monkey of cartazolate (SQ 65,396), a substituted pyrazolopyridine having anxiolytic activity.卡他唑酯(SQ 65,396)在猴体内的生物转化,卡他唑酯是一种具有抗焦虑活性的取代吡唑并吡啶。
Xenobiotica. 1981 Jul;11(7):481-8. doi: 10.3109/00498258109045858.
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