Methodological approaches for the study of GABA(A) receptor pharmacology and functional responses

摘要: Inhibitory GABA(A) receptor ion channels are the target for a wide range of clinically-used therapeutic agents. The complex structural diversity these ligand-gated channels, revealed by molecular cloning studies, together with increasing requirements higher-throughput functional assays in drug discovery, has led to development techniques examine pharmacology and function. In current article we review some methodologies which have contributed expansion knowledge this field. include: approaches, immunoprecipitation, immunopurification study assembly, structure, expression; situ hybridization, immunocytochemistry, autoradiography distribution native tissues; radioligand binding, site-directed mutagenesis, electrophysiology allosteric modulation; patch clamp, flux, microphysiometry, variety novel fluorescence-based technologies ion-channel use gene targetting approaches transgenic mice also provided important insights into role specific subtypes vivo. continuing evolution assay appropriate sensitivity resolution measure subtle modulation will facilitate ongoing investigation physiological functions inhibitory receptors.