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精神药物在中枢神经系统的生化效应(作者译)

[Biochemical effects of psychotropic drugs in central nervous system (author's transl)].

作者信息

Karobath M

出版信息

Klin Wochenschr. 1979 Jun 15;57(12):599-605. doi: 10.1007/BF01477626.

Abstract

Studies on the biochemical effects of clinically used psychotropic drugs in brain have shown that they all exert their action by a direct or indirect interference with synaptic transmission. Thus, animal studies in vivo and in vitro have shown that the clinical efficacy of antipsychotic drugs correlates with their inhibitory action on dopamine receptors. In vivo these compounds enhance dopamine turnover in the brain and in vitro they inhibit the dopamine sensitive adenylate cyclase and the binding of dopamine to its receptor at neuronal membranes. Tricyclic antidepressants are drugs which have effects on many transmitter systems. No specific biochemical action has been found which is closely correlated with their clinical potency. However, it appears that a stimulation of the function of the noradrenergic system might have some clinical relevance. Benzodiazepines exert their pharmacological activity in the CNS by interacting with a brain specific receptor. This receptor appears to be part of a larger complex including a GABA receptor and the chloride conductance mechanism associated with the GABA receptor. By binding to their receptor, benzodiazepines appear to enhance the sensitivity of the GABA receptor, thus indirectly potentiating GABA-ergic neurotransmission in the brain.

摘要

对临床上使用的精神药物在大脑中的生化作用的研究表明,它们都是通过直接或间接干扰突触传递来发挥作用的。因此,体内和体外的动物研究表明,抗精神病药物的临床疗效与其对多巴胺受体的抑制作用相关。在体内,这些化合物会增强大脑中的多巴胺周转,在体外,它们会抑制多巴胺敏感的腺苷酸环化酶以及多巴胺与神经元膜上其受体的结合。三环类抗抑郁药是对许多递质系统都有作用的药物。尚未发现与其临床效力密切相关的特异性生化作用。然而,似乎去甲肾上腺素能系统功能的刺激可能具有一定的临床相关性。苯二氮䓬类药物通过与大脑特异性受体相互作用在中枢神经系统发挥其药理活性。该受体似乎是一个更大复合物的一部分,该复合物包括一个GABA受体以及与GABA受体相关的氯电导机制。通过与它们的受体结合,苯二氮䓬类药物似乎增强了GABA受体的敏感性,从而间接增强了大脑中的GABA能神经传递。

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