GABA glycine receptors

GABA glycine receptors transducing components (for inhibitory synapses)... 

The receptor-operated Cl -channels of the central nervous system (CNS) are gated by the respective agonists GABA and glycine. Most Cl -channels can be inhibited by disulphonate stilbenes. Muscle Cl -channels can be inhibited by anthracene-9-carboxylate (A9C) and probably by IAA-94. The ICOR Cl -channel is fairly sensitive to NPPB. It should be noted, however, that none of these probes, except for the GABA- and glycine-receptor Cl -channels, is of sufficient affinity and selectivity to permit the channel identification by its use. This dilemma is one of the reasons why the purification of epithelial Cl -channels lags behind that of the CNS Cl -channels. 

Pharmacological modulation of GABA -receptor and glycine-receptor channels... 

Kerchner, G. A., Wang, G. D., Qiu, C. S., Huettner, J. E., and Zhuo, M. (2001) Direct presynaptic regulation of GABA/glycine release by kainate receptors in the dorsal horn an ionotropic mechanism. Neuron 32,477—488. 

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. 

At least two classes of neurotransmitter-controlled receptors with intrinsic ion channel function can be differentiated. One class includes receptors with the specific ligands acetylcholine, y-aminobutyric acid (GABA), glycine and serotonin. 

The receptors for acetylcholine, GABA, glycine and serotonin have a homologous structure and form a superfamily. The best-investigated representative of this superfamUy is the nicotinic acetylcholine receptor, for which extensive biochemical and structural data are available. The nicotinic acetylcholine receptor can be treated as a representative of the other receptors of the superfamUy since it can be assumed that the structure-function principles of this receptor apply to the others. 

GABA and glycine. Glycine receptors are pentameric structures that are selectively permeable to . Strychnine, which is a potent spinal cord convulsant and has been used in some rat poisons, selectively blocks glycine receptors. 

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