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Bioorg Khim ; 11(10): 1348-52, 1985 Oct.
Artigo em Russo | MEDLINE | ID: mdl-4074397

RESUMO

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.


Assuntos
Aziridinas/síntese química , Azirinas/síntese química , Inibidores da Colinesterase/síntese química , Acetilcolinesterase/metabolismo , Aziridinas/metabolismo , Aziridinas/farmacologia , Sítios de Ligação , Fenômenos Químicos , Química , Inibidores da Colinesterase/metabolismo , Proteínas Neurotóxicas de Elapídeos , Cinética , Peso Molecular , Trítio
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