The Journal of Neurobehavioral Sciences

Yazarlar: Arslan Ayla

Konular:-

DOI:10.5455/JNBS.1432919387

Anahtar Kelimeler:-

Özet: The gamma-aminobutyric acid type A receptors (GABAA Rs), belonging to the superfamily of Cys-loop receptors, responsible for the inhibitory transmission in the vertebrate central nervous system. Assembled from a pool of 19 subunits, the subunit composition of heteropentameric GABA-A Rs impacts on receptor’s function, physiology, cellular and subcellular localization in the cell membrane, i.e., synaptic or extrasynaptic. γ2 containing GABA-A Rs (γ2-GABA-A Rs) are clustered in the synapses and mediate classical fast synaptic inhibition called phasic inhibition. δ subunit containing GABA-A Rs (δ-GABA-A Rs) are located extrasynaptically and mediate a different form of inhibition called tonic inhibition critical for the threshold of action potential generation and neuronal excitability. Thus, distinct physiological roles of synaptic and extrasynaptic GABA-A R subtypes lead to the question to ask about the possibility of subtype selective drugs. In the light of accumulating data from X-ray crystal structures of vertabrate, invertabrate and prokaryotic Cys-loop receptor family members, new opportunities arise for the development of novel drugs targeting specificaly these subtypes of GABA-A Rs for the treatment of various neuropathological conditions.

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