出版社：International Medical Journal Management and Indexing System
摘要：ABSTRACT The gamma-aminobutyric acid type A receptors (GABAARs), belonging to the superfamily of Cys-loop receptors, responsible for the inhibitory transmission in the vertebrate central nervous system. Encoded by 19 distinct genes, the subunit assembly of heteropentameric GABAARs impact on receptors location in the cell membrane, i.e., synaptic or extrasynaptic. g2 containing GABAARs (g2-GABAARs) are clustered in the synapses and mediate classical fast synaptic inhibition called phasic inhibition. d subunit containing GABAARs (d-GABAARs) are located extrasynaptically and mediate a different form of inhibition called tonic inhibition critical for the threshold of action potential generation. Thus, these two different subtypes of GABAARs display distinct physiological roles for the brain function. In the light of new data from recent X-ray crystal structures of vertabrate, invertabrate and prokaryotic Cys-loop receptor members, new opportunities arise for the development of novel drugs targeting specificaly these subtypes of GABAARs for the treatment of various neuropathological conditions.
