Michels Guido, Moss Stephen J
Department of Neuroscience, University of Pennsylvania, School of Medicine, Philadelphia, PA 19104-6074, USA.
Crit Rev Biochem Mol Biol. 2007 Jan-Feb;42(1):3-14. doi: 10.1080/10409230601146219.
Fast synaptic inhibition in the brain and spinal cord is mediated largely by ionotropic gamma-aminobutyric acid (GABA) receptors. GABAA receptors play a key role in controlling neuronal activity; thus modulating their function will have important consequences for neuronal excitation. GABAA receptors are important therapeutic targets for a range of sedative, anxiolytic, and hypnotic agents and are involved in a number of CNS diseases, including sleep disturbances, anxiety, premenstrual syndrome, alcoholism, muscle spasms, Alzheimer's disease, chronic pain, schizophrenia, bipolar affective disorders, and epilepsy. This review focuses on the functional and pharmacological properties of GABAA receptors and trafficking as an essential mechanism underlying the dynamic regulation of synaptic strength.
大脑和脊髓中的快速突触抑制主要由离子型γ-氨基丁酸（GABA）受体介导。GABAA受体在控制神经元活动中起关键作用；因此，调节其功能将对神经元兴奋产生重要影响。GABAA受体是一系列镇静、抗焦虑和催眠药物的重要治疗靶点，并涉及多种中枢神经系统疾病，包括睡眠障碍、焦虑、经前综合征、酒精中毒、肌肉痉挛、阿尔茨海默病、慢性疼痛、精神分裂症、双相情感障碍和癫痫。本综述重点关注GABAA受体的功能和药理学特性以及转运，转运是突触强度动态调节的重要机制。
