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[Synthesis of tritium-labeled N,N-dimethyl-2-phenylaziridinium and its reaction with acetylcholinesterase].

作者信息

Palumaa P Ia, Raĭdaru G I, Iarv Ia L, Shevchenko V P, Miasoedov N F

出版信息

Bioorg Khim. 1985 Oct;11(10):1348-52.

PMID:4074397
Abstract

The synthesis of tritium-labeled N,N-demethyl-2-phenylaziridinium has been described. The specific radioactivity of the product obtained was 1,06 TBq/mmole. Kinetics of incorporation of this radioactive label into acetylcholinesterase of cobra venom (Naja naja oxiana) has been studied at 1,05 mM ligand concentration (25 degrees C, pH 7,50. 0,15 M phosphate buffer). Under these conditions two molecules of the radioactive label have been found to react with the enzyme. One molecule incorporates fast with half-life of 4,8 min, not affecting the enzymatic activity. Incorporation of the second label is a slow reaction with half-life of 6 hr and leads to complete inactivation of acetylcholinesterase. Molecular mass of the modified enzyme is 63 +/- 4 kDa and coincides with that of native one.

摘要

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