GABA -gated chloride channel

The GABA-gated chloride ion channel is modulated by several classes of drugs that bind to allosteric sites on the receptor complex the benzodiazepines, barbiturates and related intravenous general anesthetics such as etomidate and propofol, as well as anesthetic steroids and endogenous neurosteroids. It appears that some types of GABAa receptor are directly enhanced by ethanol and volatile general anesthetics (Fig. 16-2) [7,8,20]. 

Schwartz-Bloom RD, CookTA, Yu X. (1996). Inhibition of GABA-gated chloride channels in brain by the arachidonic acid metabolite, thromboxane A2. Neuropharmacology. 35(9-10) 1347-53. 

In the retina, homomeric receptors consisting of the p-subunit represent a particular class of GABA-gated chloride channels. Their GABA site is insensitive to bicuculline and baclofen and they are not modulated by barbiturates or benzodiazepines. Due to these distinctive features, the receptors are sometimes termed GABAc receptors (Bormann 2000), although they are be considered a homomeric class of GABAa receptors (Barnard et al. 1998). 

Barbiturates also facilitate the actions of GABA at multiple sites in the central nervous system, but—in contrast to benzodiazepines—they appear to increase the duration of the GABA-gated chloride channel openings. At high... 

There is little doubt that milbemycins and avermectins act on chloride channels associated with GABA receptors and amplify GABA functions in the mammalian central nervous system. In the free-living nematode, C elegans, however, avermectin was found to interact with glutamate-gated... 

The GABAa receptor is a ligand-gated chloride channel that underlies synaptic inhibition in the brain. When the endogenous neurotransmitter, GABA, binds to the... 

Insecticides Interfering with GABA-Gated Chloride Channels... 

The insect GABA receptor-chloride ionophore complex is found in the CNS and also at peripheral neuromuscular sites. GABA receptors belong to a superfamily of ligand-gated ion channels known as Cys-loop receptors that include nicotinic acetylcholine receptors and glutamate-gated chloride channels (Lester, 2004). Cys-loop receptors are so named because... 

GABA-gated chloride channels Cyclodienes, lindane, phenylpyrazoles, Avermectins, emamectin benzoate, milbemectin Antagonism Chloride channel activators... 

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