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GABAergic hypotheses of anxiety and depression: focus on GABA-B receptors.

机译：焦虑和抑郁的GABA能假说：关注GABA-B受体。

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Depression and anxiety are psychiatric disorders with high morbidity and comorbidity. Because of multiple adverse effects of existing drugs and a low efficacy, therapy for a substantial number of patients is unsatisfactory. It is widely accepted that gamma-aminobutyric acid (GABA) is the primary inhibitory transmitter substance in the mammalian central nervous system. Data are accumulating that the recently cloned GABAB receptors might become a target for the development of new antidepressant and/or anxiolytic drugs. The existing data support the hypothesis that agonists and particularly positive modulators of GABAB receptors (but not GABAB receptor antagonists) may be anxiolytic drugs in the future. The experiments demonstrate that the most consistent finding following chronic administration of antidepressants is an increase in GABAB receptor function, with or without a change in receptor binding or subunit expression. Data are accumulating in preclinical studies that show that antagonists (but not agonists) of GABAB receptors may have antidepressant effects.
机译：抑郁和焦虑是高发病率和合并症的精神病。由于现有药物的多种不良反应和疗效低下，因此无法满足大量患者的治疗需求。 γ-氨基丁酸（GABA）是哺乳动物中枢神经系统中的主要抑制性递质，这一点已被广泛接受。越来越多的数据表明，最近克隆的GABA B受体可能成为开发新的抗抑郁药和/或抗焦虑药的目标。现有数据支持这样的假设，即激动剂，尤其是GABA B受体的正调节剂（但不是GABA B受体拮抗剂）将来可能是抗焦虑药。实验表明，长期服用抗抑郁药后，最一致的发现是GABA B受体功能的增强，无论受体结合或亚基表达是否发生变化。临床前研究中积累的数据表明，GABA B受体的拮抗剂（而非激动剂）可能具有抗抑郁作用。

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