GABA receptors ionotropic

Johnston GA, Hanrahan JR, Chebib M, Duke RK, Mewett KN. 2006. Modulation of ionotropic GABA receptors by natural products of plant origin. Adv Pharmacol 54 285-316. 

Ionotropic GABA receptors (GABA(A)-Rs and GABA(C)-Rs) are inhibitory (hyperpolarizing) GABA-gated Cl channels that have sequence homology with nACh-Rs... 

Inhibitory glutamate receptors (iGlu-Rs) are inhibitory, Glu-gated ion channels related to the ionotropic GABA receptors and glycine receptors, the open channel being permeable to Cl- and sometimes to K+. The isoxazole alkaloid ibotenic acid activates iGlu-Rs (Table 3.3). 

Ozoe Y, Akamatsu M, Higata T, Ikeda I, Mochida K, Koike K, Ohmoto T, Nikaido T (1998) Picrodendrin and Related Terpenoid Antagonists Reveal Structural Differences Between Ionotropic GABA Receptors of Mammals and Insects. Bioorg Med Chem 6 481... 

Ju XL, Hao YL, Pei JF, Ozoe Y (2007) Investigation of Structural Requirements for Inhibitory Activity at the Rat and Housefly Picrotoxinin Binding Sites in Ionotropic GABA receptors using DISCOtech and CoMLA. Chemosphere 69 864... 

Nineteen different ionotropic GABA receptor subunits, named ai 6, P 3, 7i 3, S, e, 71 and d and 3, have been cloned from vertebrates. Experiments using recombinant expression and immunoprecipitation indicate that native vertebrate GABAa receptors contain at least a, fi and y subunits, sometimes also with <5, s, K ox 0 subunits, while GABAc receptors are believed to be composed only of p subunits. 

Molecular Neuropharmacology Strategies and Methods is intended to bridge the gap between molecular biology and advanced chemistry. In addition, it attempts to include information about x-ray crystallographic analyses whenever available. This book discusses interdisciplinary interactions for monoamine transporters, amino acid transporters, ionotropic receptors, metabotropic glutamate receptors, GABA receptors, and other G protein-coupled receptors. 

There are two main families of ligand-gated ion channel proteins that act as ionotropic receptors. One family includes the nicotinic acetylcholine receptor, the GABA-A receptor, the glycine receptor, and a class of serotonin receptor. The other family comprises various types of ionotropic glutamate receptors. Since these various ligand gated ion channels are activated by neurotransmitters, the medicinal chemistry of these proteins is presented in detail in chapter 4. 

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