Extrasynaptic GABAA receptor pharmacology and structure-activity relationship.docVIP

 PAGE \* MERGEFORMAT 16 Extrasynaptic GABAA receptor pharmacology and structure-activity relationship [Abstract] GABA (-aminobutyric acid in the vertebrate central nervous system, an important inhibitory neurotransmitter, mainly by acting on GABAA, GABAB and GABAC physiological effects of three subtypes of receptors. GABAA synapse receptor-mediated inhibitory postsynaptic currents mediated by GABAA receptors in the theoretical basis of inhibitory effect, but recently, scientists have described a new type of GABAA receptor-mediated inhibition of the sustained inhibition. is due to low concentration The activation of extrasynaptic GABAA receptors in GABA induced physiological effects. extrasynaptic GABAA receptors in the biophysical properties can stably inherited to the next generation of the subunits in the pharmacological and functional receptors are also different from the synapse analogue. This review will be more comprehensive exposition of the specific nature of recombinant, natural extrasynaptic GABAA receptors and their associated reagents. and further from the physiology and pathology of the central nervous system extrasynaptic GABAA receptors GABA can inhibit the important role of the current process. [Keywords:] GABAA receptor pharmacology function 1 Introduction It was originally found in cerebellar granule cells, some neurons in the presence of a dependent on extrasynaptic GABAA receptor signaling. Later, back in the other parts such as brain, hippocampus, cerebral cortex, thalamus, striatum, hypothalamus, This phenomenon is also found in the spinal cord. GABA (-aminobutyric acid overflow from the synaptic cleft, or the activation of extrasynaptic GABAA receptors in the presynaptic membrane, resulting in a continual GABA currents, which play with the classic conflict Aftertouch stage GABAA receptor-mediated slow but transient phase lasting inhibition of different persistent inhibition. this inhibition also exists in humans. It is not a