Kinetic Analyses of Alcohol-Induced Potentiation of the Response of GABAA Receptors Composed of .ALPHA.1 and .BETA.1 Subunits.

概要

論文の詳細を見る
To investigate the kinetics of both the potentiation and desensitization of the response of ionotropic GABA receptors (GABAA receptors) in the presence of various compounds, we expressed receptors composed of α1 and β1subunits by injectingcells with the cRNAs synthesized from cloned bovine GABAA receptor cDNAs and measured the elec-trical responses of the cells electrophysiologically with or without the compounds. The potentiation of the GABAA receptor-mediated response was quantitatively analyzed using a simple model with the assumption that thereceptors have two identical binding sites for GABA molecules with a dissociation constant of Kp, and one potentiation site for the compound with a dissociation constant of Kp, and that the binding of the compound to the potentiation site only increases the affinity of the GABA binding sites, changing K1 to K1p.The estimated Kp and K1p were dependent on the functional groups and the chainlength of the compounds. These results could be satisfactorily analyzed using this simple model. The potentiation of the GABAA receptor-mediated response by the components of essential oils used for aromatherapy was also examined. These com-pounds accelerated the decay of the response, possibly due to desensitizationof the receptors, which was also analyzed on the basis of the model.
社団法人日本生化学会の論文