取代色胺类似物、单胺氧化酶抑制剂与细胞色素P-450之间的相互作用。

Interactions between substituted tryptamine analogues, MAO inhibitors and cytochrome P-450.

作者信息

Valoti M, Costanzo M, Perez V, Unzeta M, Sgaragli G P

机构信息

Department de Bioquimica i Biologia Molecular, Universidad Autonoma de Barcelona, Spain.

出版信息

J Neural Transm Suppl. 1994;41:291-3. doi: 10.1007/978-3-7091-9324-2_38.

DOI:10.1007/978-3-7091-9324-2_38

PMID:7931240

Abstract

The effects of some MAO inhibitors, N-acetylenic analogues of tryptamine, on rat liver microsomal cytochrome P-450 (cyt P-450) have been investigated. All the compounds tested interacted with cyt P-450 with Ks values ranging between 14 and 358 microM (clorgyline Ks = 10.5 microM). Compounds with a tertiary amine and those possessing a secondary amine group in the acetylenic side chain exhibited type I and type II difference spectra, respectively. Aniline hydroxylase activity was inhibited irreversibly and in a time-dependent fashion by all compounds tested with IC50 ranging between 7 x 10(-5) and 7 x 10(-3) M (clorgyline 10(-4) M).

摘要

已经研究了一些单胺氧化酶抑制剂，即色胺的N-炔类类似物对大鼠肝脏微粒体细胞色素P-450（细胞色素P-450）的影响。所有测试的化合物都与细胞色素P-450相互作用，其Ks值在14至358微摩尔之间（氯吉兰的Ks = 10.5微摩尔）。在炔侧链中含有叔胺的化合物和含有仲胺基团的化合物分别表现出I型和II型差异光谱。所有测试的化合物均以不可逆且时间依赖性的方式抑制苯胺羟化酶活性，其IC50在7×10^(-5)至7×10^(-3)摩尔之间（氯吉兰为10^(-4)摩尔）。