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腺苷酸环化酶的双重调节导致了麻醉药物依赖和耐受性。

Dual regulation of adenylate cyclase accounts for narcotic dependence and tolerance.

作者信息

Sharma S K, Klee W A, Nirenberg M

出版信息

Proc Natl Acad Sci U S A. 1975 Aug;72(8):3092-6. doi: 10.1073/pnas.72.8.3092.

Abstract

Narcotics affect adenylate cyclase [ATP pyrophosphate-lyase (cyclizing), EC 4.6.1.1] in two opposing ways, both mediated by the opiate receptor. The first process is the readily reversible inhibition of the enzyme by narcotics; the second is a compensatory increase in enzyme activity which is delayed in onset and relatively stable. Late positive regulation of the enzyme counteracts the inhibitory influence of morphine and is responsible for narcotic dependence and tolerance. The coupled inhibitory and positive regulatory mechanisms for adenylate cyclase provide a means of activating and deactivating neural circuits hours after the initial event and thus may play a role in a memory process.

摘要

麻醉药以两种相反的方式影响腺苷酸环化酶[ATP焦磷酸裂解酶(环化),EC 4.6.1.1],这两种方式均由阿片受体介导。第一个过程是麻醉药对该酶的快速可逆抑制;第二个过程是酶活性的代偿性增加,其起效延迟且相对稳定。该酶的晚期正向调节抵消了吗啡的抑制作用,并导致麻醉药依赖和耐受性。腺苷酸环化酶的耦合抑制和正向调节机制提供了一种在初始事件数小时后激活和失活神经回路的方法,因此可能在记忆过程中发挥作用。

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