使用乙丙嗪和BW 284C51作为来自不同物种的胆碱酯酶的选择性抑制剂。

Use of ethopropazine and BW 284C51 as selective inhibitors for cholinesterases from various species.

作者信息

Mikalsen A, Andersen R A, Alexander J

出版信息

Comp Biochem Physiol C Comp Pharmacol Toxicol. 1986;83(2):447-9. doi: 10.1016/0742-8413(86)90152-0.

PMID:2872013

Abstract

Both inhibitors tested were still able to depress the cholinesterase (ChE) for which it is not selective (BW 284C51 for pseudo ChE, ethopropazine for the true ChE) provided the concentration was high (greater than 10(-2) M). BW 284C51 totally depressed the true ChE activity from bovine erythrocytes at a concentration of 10(-6) M. This inhibitor concentration gave no depression of pseudo ChE activity from horse serum. Ethopropazine totally depressed the pseudo ChE activity from horse serum at a concentration of 5 X 10(-5) M. The true ChE was not inhibited at this concentration. For true ChE from bovine erythrocytes and pseudo ChE from horse serum BW 284C51 and ethopropazine therefore certainly have a potential as selective ChE inhibitors. Ethopropazine at a concentration of 5 X 10(-6) M completely inhibited the pseudo ChE activity in rat plasma and cortex without affecting true ChE activity. BW 284C51 at a concentration of 10(-6) M gave a total depression of the true ChE activity in these preparations. In rat plasma, however, a considerable part of the pseudo ChE activity was depressed at this concentration.

摘要

所测试的两种抑制剂在高浓度（大于10⁻² M）时，仍能够抑制其并非选择性作用的胆碱酯酶（ChE）（BW 284C51作用于拟胆碱酯酶，乙磺丙嗪作用于真性胆碱酯酶）。BW 284C51在浓度为10⁻⁶ M时可完全抑制牛红细胞中的真性胆碱酯酶活性。此抑制剂浓度对马血清中的拟胆碱酯酶活性无抑制作用。乙磺丙嗪在浓度为5×10⁻⁵ M时可完全抑制马血清中的拟胆碱酯酶活性。在此浓度下，真性胆碱酯酶未受抑制。因此，对于牛红细胞中的真性胆碱酯酶和马血清中的拟胆碱酯酶而言，BW 284C51和乙磺丙嗪无疑具有作为选择性胆碱酯酶抑制剂的潜力。乙磺丙嗪在浓度为5×10⁻⁶ M时可完全抑制大鼠血浆和皮质中的拟胆碱酯酶活性，而不影响真性胆碱酯酶活性。BW 284C51在浓度为10⁻⁶ M时可使这些制剂中的真性胆碱酯酶活性完全受到抑制。然而，在大鼠血浆中，此浓度下相当一部分拟胆碱酯酶活性也受到了抑制。