人体中的药理学“脑啡肽酶”抑制作用。

Pharmacological "enkephalinase" inhibition in man.

作者信息

Marcello F, Grazia S M, Sergio M, Federigo S

出版信息

Adv Exp Med Biol. 1986;198 Pt B:153-60. doi: 10.1007/978-1-4757-0154-8_19.

Abstract

"Enkephalinase", a peptidase capable of degradating enkephalins, has been recently characterized in man, in both plasma and cerebro-spinal fluid (CSF). This study was designed to evaluate the ability of putative "enkephalinase" inhibitors, D-phenylalanine, captopril and thiorphan to decrease "enkephalinase" activity (EKA) in plasma and CSF in human sufferers. All drugs studied decreased plasma EKA. Captopril and thiorphan also decreased CSF EKA. Of the three drugs tested thiorphan proved to be the most potent "enkephalinase" inhibitor in both plasma and CSF. These results show the usefulness of EKA assessment as a procedure for evaluating the potency and specificity of putative "enkephalinase" inhibitors in man.

摘要

“脑啡肽酶”是一种能够降解脑啡肽的肽酶，最近已在人体的血浆和脑脊液（CSF）中得到鉴定。本研究旨在评估三种假定的“脑啡肽酶”抑制剂——D-苯丙氨酸、卡托普利和硫氧还蛋白降低人类患者血浆和脑脊液中“脑啡肽酶”活性（EKA）的能力。所有研究的药物均降低了血浆EKA。卡托普利和硫氧还蛋白也降低了脑脊液EKA。在所测试的三种药物中，硫氧还蛋白在血浆和脑脊液中均被证明是最有效的“脑啡肽酶”抑制剂。这些结果表明，EKA评估作为一种评估人体中假定的“脑啡肽酶”抑制剂效力和特异性的方法是有用的。