Holt A, Callingham B A
Department of Pharmacology, University of Cambridge, United Kingdom.
J Neural Transm Suppl. 1994;41:439-43. doi: 10.1007/978-3-7091-9324-2_59.
Monoamine oxidase (MAO) and semicarbazide-sensitive amine oxidase (SSAO) activities were examined in homogenates of various rat tissues following i.p. administration of procarbazine or methylhydrazine. Both compounds inhibited SSAO in a dose-dependent manner in all tissues examined, with methylhydrazine the more potent agent in this respect. Little inhibition of MAO could be detected in most cases. However, hepatic MAO-B activity was potentiated significantly in rats receiving methylhydrazine and both drugs caused a dose-dependent potentiation of MAO-A in homogenates of brown adipose tissue. The potential use of these compounds in vivo as selective SSAO inhibitors is discussed.
腹腔注射丙卡巴肼或甲基肼后,检测了各种大鼠组织匀浆中的单胺氧化酶(MAO)和氨基脲敏感性胺氧化酶(SSAO)活性。两种化合物在所有检测组织中均以剂量依赖性方式抑制SSAO,在这方面甲基肼是更有效的药物。在大多数情况下,几乎检测不到对MAO的抑制作用。然而,接受甲基肼的大鼠肝脏MAO-B活性显著增强,两种药物均导致棕色脂肪组织匀浆中MAO-A呈剂量依赖性增强。讨论了这些化合物在体内作为选择性SSAO抑制剂的潜在用途。