取代色胺类似物对单胺氧化酶的抑制作用。

Inhibition of MAO by substituted tryptamine analogues.

作者信息

Balsa D, Fernandez-Alvarez E, Tipton K F, Unzeta M

机构信息

Departament de Bioquímica i Biología Molecular, Facultat de Medicina, Universitát Autónoma de Barcelona, Spain.

出版信息

J Neural Transm Suppl. 1990;32:103-5. doi: 10.1007/978-3-7091-9113-2_13.

DOI:10.1007/978-3-7091-9113-2_13

PMID:2089079

Abstract

Three different acetylenic analogues of tryptamine, in which the side chain is attached at the 2 position of the heterocyclic ring, were studied as inhibitors of MAO-A and MAO-B. IC50 values were determined after 30 min preincubation of the enzyme and inhibitor, at 37 degrees C before assay. Irreversibility and time-dependence of the inhibition were also established in each case. The kinetic parameters defining non-covalent complex formation and covalent adduct formation were calculated for the mechanism-based inhibition of both MAO-A and MAO-B by these compounds.

摘要

研究了三种不同的色胺乙炔类似物，其侧链连接在杂环的2位，作为单胺氧化酶A（MAO-A）和单胺氧化酶B（MAO-B）的抑制剂。在测定前于37℃对酶和抑制剂进行30分钟预温育后，测定半数抑制浓度（IC50）值。还在每种情况下确定了抑制作用的不可逆性和时间依赖性。计算了这些化合物对MAO-A和MAO-B基于机制抑制作用的定义非共价复合物形成和共价加合物形成的动力学参数。