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Functional Domains of GABAA RECEPTORS

Functional domains of GABAA RECEPTORS

G.B. Smith and R. W. Olsen. TIPS 16:162-167.

This review discusses recent advances in the field of gamma aminobutyric acid-A (GABAA) receptors and their pharmacology. The authors summarize all current information on the molecular biology and pharmacology of the structure of GABAA receptors, the GABA binding site, the benzodiazepine binding site and ion channels. A convincing argument is developed for using information gathered on one member of the transmitter-gated ion channel receptors as models for other members of the superfamily. The authors conclude by presenting and justifying a model describing the functional domain of a transmitter-gated ion channel based on data collected for the GABAA receptor.

GABAA receptors mediate the majority of inhibitory synaptic transmissions in the central nervous system (CNS) and are members of the superfamily of transmitter-gated ion channels that include nicotinic acetylcholine receptors and inhibitory glycine receptors. GABAA receptors contain recognition sites that bind with gamma aminobutyric acid (GABA) - the most ubiquitous neurotransmitter in the brain - and many important neuroactive drugs including benzodiazepines, barbiturates, steroids, general anesthetics and possibly alcohol. These binding sites are directly or indirectly involved in mediating the gating properties of integral Cl- channels.

GABAA receptors - and other members of the superfamily - are heteropentameric pseudo-symmetric protein complexes consisting of several homologous transmembrane glycoprotein subunits. The subunits of various members of the superfamily are evolutionarily related and all are characterized by a large N-terminal extracellular domain with a disulphide bridge, four transmembrane domains (TM1, TM2, TM3 and TM4) and a looped intracellular domain between TM3 and TM4 as shown on Figure 1. As such, GABAA receptors are isoreceptors, composed of multiple sub...

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Functional Domains of GABAA RECEPTORS. (1969, December 31). In LotsofEssays.com. Retrieved 11:53, March 28, 2024, from https://www.lotsofessays.com/viewpaper/1682374.html