尼古丁对映体对豚鼠肺芳香氮杂环N-甲基转移酶具有显著的底物抑制特性。

Remarkable substrate-inhibitor properties of nicotine enantiomers towards a guinea pig lung aromatic azaheterocycle N-methyltransferase.

作者信息

Cundy K C, Crooks P A, Godin C S

出版信息

Biochem Biophys Res Commun. 1985 Apr 16;128(1):312-6. doi: 10.1016/0006-291x(85)91680-8.

Abstract

The kinetics of nicotine methylation by guinea pig lung homogenates has been investigated. An interesting stereospecificity has been observed for nicotine enantiomers. R-(+)-Nicotine is a substrate Km = 1.42 X 10(-5)M for an SAM-dependent guinea pig lung aromatic azaheterocycle N-methyltransferase, whereas S-(-)-nicotine acts as a competitive inhibitor (Ki = 6.25 X 10(-5)M) of the N-methylation of its antipode.

摘要

对豚鼠肺匀浆中尼古丁甲基化的动力学进行了研究。已观察到尼古丁对映体存在有趣的立体特异性。R-(+)-尼古丁是一种底物，对于依赖S-腺苷甲硫氨酸（SAM）的豚鼠肺芳香氮杂环N-甲基转移酶，其Km = 1.42×10⁻⁵M，而S-(-)-尼古丁作为其对映体N-甲基化的竞争性抑制剂（Ki = 6.25×10⁻⁵M）。