Department of Bioorganic Chemistry, Wrocław University of Technology, Wrocław, Poland.
Curr Med Chem. 2010;17(22):2338-47. doi: 10.2174/092986710791698549.
gamma-Amino butyric acid is an extremely important inhibitory neurotransmitter in the mammalian central nervous system and is essential for the overall balance between neuronal excitation and inhibition. It is well documented that GABA deficiency is associated with several important neurological disorders such as Huntington's chorea, Parkinson's and Alzheimer's disease and other psychiatric disorders, like anxiety, depression, pain, panic, or mania. Although, it is known that increasing the brain concentration of GABA prevents convulsions, the high polarity and flexible structure of this compound are probably responsible for its inefficiency as an anticonvulsant when administered orally or intravenously. To resolve this problem, GABA analogues are being designed. Over recent years, there has been increasing interest in the synthesis and pharmacological effect of new GABA derivatives, which can be considered as potent drugs in the treatment of neurodegenerative disorders.
γ-氨基丁酸是哺乳动物中枢神经系统中一种极其重要的抑制性神经递质,对于神经元兴奋和抑制之间的整体平衡至关重要。有充分的文献记载表明,GABA 缺乏与几种重要的神经疾病有关,如亨廷顿舞蹈病、帕金森病和阿尔茨海默病,以及其他精神疾病,如焦虑、抑郁、疼痛、恐慌或躁狂。尽管人们知道增加大脑中 GABA 的浓度可以预防惊厥,但这种化合物的高极性和灵活结构可能是其口服或静脉注射时作为抗惊厥药物效率低下的原因。为了解决这个问题,正在设计 GABA 类似物。近年来,人们对新型 GABA 衍生物的合成和药理学作用越来越感兴趣,这些衍生物可以被认为是治疗神经退行性疾病的有效药物。