Unsaturated Analogues of the Neurotransmitter GABA: trans-4-Aminocrotonic, cis-4-Aminocrotonic and 4-Aminotetrolic Acids
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- 作者：Graham A. R. Johnston
- 关键词：GABA ; trans ; 4 ; Aminocrotonic acid ; cis ; 4 ; Aminocrotonic acid ; 4 ; Aminotetrolic acid ; GABAA receptors ; GABAC receptors
- 刊名：Neurochemical Research
- 出版年：2016
- 出版时间：March 2016
- 年：2016
- 卷：41
- 期：3
- 页码：476-480
- 全文大小：458 KB
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1. Pharmacology, Faculty of Medicine, School of Medical Sciences, The University of Sydney, Sydney, NSW, 2006, Australia - 刊物类别：Biomedical and Life Sciences
- 刊物主题：Biomedicine
Neurosciences
Biochemistry
Neurology - 出版者：Springer Netherlands
- ISSN：1573-6903
文摘
Analogues of the neurotransmitter GABA containing unsaturated bonds are restricted in the conformations they can attain. This review traces three such analogues from their synthesis to their use as neurochemicals. trans-4-Aminocrotonic acid was the first conformationally restricted analogue to be extensively studied. It acts like GABA across a range of macromolecules from receptors to transporters. It acts similarly to GABA on ionotropic receptors. cis-4-Aminocrotonic acid selectively activates bicuculline-insensitive GABAC receptors. 4-Aminotetrolic acid, containing a triple bond, activates bicuculline-sensitive GABAA receptors. These findings indicate that GABA activates GABAA receptors in extended conformations and GABAC receptors in folded conformations. These and related analogues are important for the molecular modelling of ionotropic GABA receptors and to the development of new agents acting selectively on these receptors.