Structural and functional characterization of the gamma 1 subunit of GABAA/benzodiazepine receptors.

摘要: The GABAA receptor gamma 1 subunit of human, rat and bovine origin was molecularly cloned compared with the 2 in structure function. Both variants share 74% sequence similarity are prominently synthesized often distinct areas central nervous system as documented by situ hybridization. When co-expressed alpha beta subunits Xenopus oocytes mammalian cells, mediate potentiation GABA evoked currents benzodiazepines help generate high-affinity binding sites for these drugs. However, show disparate pharmacological properties which, receptors assembled from 1, subunits, characterized conspicuous loss affinity neutral antagonists (e.g. flumazenil) negative modulators DMCM). These findings reveal a pronounced effect on GABAA/benzodiazepine pharmacology.