吗氯贝胺和2-氨基乙基甲酰胺衍生物对单胺氧化酶的抑制作用：作用方式和动力学特征。

Monoamine oxidase inhibition by moclobemide and 2-amino-ethyl carboxamide derivatives: mode of action and kinetic characteristics.

作者信息

Cesura A M, Muggli-Maniglio D, Lang G, Imhof R, Da Prada M

机构信息

Pharmaceutical Research Department, F. Hoffmann-La Roche Ltd, Basel, Switzerland.

出版信息

J Neural Transm Suppl. 1990;32:165-70. doi: 10.1007/978-3-7091-9113-2_24.

DOI:10.1007/978-3-7091-9113-2_24

PMID:2089085

Abstract

The selective, reversible inhibitors of monoamine oxidase (MAO) moclobemide and Ro 41-1049 (selective for MAO-A), as well as of Ro 16-6491 and Ro 19-6327 (selective for MAO-B) inhibited the enzyme with an initial competitive phase, followed by a time-dependent inhibition of MAO. Ro 41-1049, Ro 16-6491 and Ro 19-6327, being activated by MAO into reversible adducts, fit into the classification as mechanism-based inhibitors. Conversely, since no product formation was observed after incubation of tissue homogenates with moclobemide, this drug probably belongs to the class of the "slow-binding" MAO inhibitors.

摘要

单胺氧化酶（MAO）的选择性、可逆抑制剂吗氯贝胺和Ro 41 - 1049（对MAO - A有选择性），以及Ro 16 - 6491和Ro 19 - 6327（对MAO - B有选择性）以初始竞争阶段抑制该酶，随后是对MAO的时间依赖性抑制。Ro 41 - 1049、Ro 16 - 6491和Ro 19 - 6327被MAO激活形成可逆加合物，属于基于机制的抑制剂类别。相反，由于用吗氯贝胺孵育组织匀浆后未观察到产物形成，该药物可能属于“慢结合”MAO抑制剂类别。