6-磺胺氨基吲唑（6-SAI）诱导的关节炎大鼠的药物代谢

Drug metabolism in rats with arthritis induced by 6-sulfanilamidoindazole (6-SAI).

作者信息

Müller D, Hirschelmann R

出版信息

Agents Actions. 1981 Dec;11(6-7):736-40. doi: 10.1007/BF01978798.

DOI:10.1007/BF01978798

Abstract

Hexobarbital sleeping time was prolonged and ethylmorphine N-demethylation was inhibited after a single dosage or seven administration of 6-SAI to old rats. These effects were independent of the development of arthritis. Changes in cytochrome P-450 concentration after 6-SAI treatment were insignificant and thus not responsible for the decrease in drug metabolism. In vitro 6-SAI inhibited ethylmorphine N-demethylation; the inhibition was of a mixed type. 6-SAI bound to cytochrome P-450 and induced a type II spectrum. The magnitude of hexobarbital-induced type I spectral changes was diminished by 6-SAI. It is concluded that 6-SAI inhibits cytochrome P-450-dependent drug metabolism by binding to cytochrome P-450.

摘要

给老年大鼠单次给药或连续七次给予6 - SAI后，己巴比妥睡眠时间延长，乙基吗啡N - 去甲基化受到抑制。这些作用与关节炎的发展无关。6 - SAI处理后细胞色素P - 450浓度变化不显著，因此不是药物代谢降低的原因。在体外，6 - SAI抑制乙基吗啡N - 去甲基化；这种抑制是混合型的。6 - SAI与细胞色素P - 450结合并诱导出II型光谱。6 - SAI使己巴比妥诱导的I型光谱变化幅度减小。结论是6 - SAI通过与细胞色素P - 450结合抑制细胞色素P - 450依赖性药物代谢。

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