士的宁在大鼠体内的代谢命运。

Metabolic fate of strychnine in rats.

Oguri K, Tanimoto Y, Mishima M, Yoshimura H

Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.

Xenobiotica. 1989 Feb;19(2):171-8. doi: 10.3109/00498258909034689.

Abstract

The urinary and faecal excretions of radioactivity, in rats dosed with 3H-strychnine at 0.5 mg/kg subcutaneously, were approx. 30% and 65% of the dose in 7 days, respectively. The radioactivity was mostly excreted within 24 h. 2. Approx. 6% and 3% dose was excreted into urine and faeces, respectively, as unchanged strychnine. 3. Urinary metabolites were extracted from rat urine and purified by silica gel column, t.l.c. and h.p.l.c. Six urinary metabolites, namely, strychnine N-oxide, 21 alpha,22 alpha-dihydroxy-22-hydrostrychnine, 21 alpha,22 beta-dihydroxy-22-hydrostrychnine, 2-hydroxy-strychnine, strychnine 21,22-epoxide and 16-hydroxystrychnine, were identified by comparison with authentic samples by g.l.c.-mass spectrometry. The major metabolites of strychnine in vivo was strychnine 21,22-epoxide.

摘要

给大鼠皮下注射0.5mg/kg的3H-士的宁后，7天内放射性物质经尿液和粪便的排泄量分别约为给药剂量的30%和65%。放射性物质大多在24小时内排出。2. 分别约有6%和3%的给药剂量以未变化的士的宁形式经尿液和粪便排出。3. 从大鼠尿液中提取尿代谢物，并通过硅胶柱、薄层层析和高效液相色谱进行纯化。通过气相色谱-质谱联用与标准品比较，鉴定出六种尿代谢物，即士的宁N-氧化物、21α,22α-二羟基-22-氢化士的宁、21α,22β-二羟基-22-氢化士的宁、2-羟基-士的宁、士的宁21,22-环氧化物和16-羟基士的宁。士的宁在体内的主要代谢物是士的宁21,22-环氧化物。