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新型氨基甲酸酯类化合物庚基毒扁豆碱的抗胆碱酯酶活性及其在阿尔茨海默病型痴呆患者中的应用前景

Anticholinesterase activity of a new carbamate, heptylphysostigmine, in view of its use in patients with Alzheimer-type dementia.

作者信息

Brufani M, Marta M, Pomponi M

出版信息

Eur J Biochem. 1986 May 15;157(1):115-20. doi: 10.1111/j.1432-1033.1986.tb09646.x.

DOI:10.1111/j.1432-1033.1986.tb09646.x
PMID:3709528
Abstract

The anticholinesterase activity of a new carbamate, heptylphysostigmine, was studied in vitro. This compound is a competitive inhibitor of acetylcholinesterase (or true cholinesterase) having Ki = (1 +/- 0.5) X 10(-7) M. The inhibition was instantaneous at the onset and did not diminish with prolonged incubation of the drug and enzyme.

摘要

在体外研究了一种新型氨基甲酸酯——庚基毒扁豆碱的抗胆碱酯酶活性。该化合物是乙酰胆碱酯酶(或真性胆碱酯酶)的竞争性抑制剂,其抑制常数Ki = (1 ± 0.5)×10⁻⁷M。抑制作用在开始时是瞬间发生的,并且不会随着药物和酶的长时间孵育而减弱。

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