Transient Expression Shows Ligand Gating and Allosteric Potentiation of GABAA Receptor Subunits
Abstract
Human (GABAA) receptor subunits were expressed transiently in cultured mammalian cells. This expression system allows the simultaneous characterization of ligand-gated ion channels by electrophysiology and by pharmacology. Thus, coexpression of the α and β subunits of the GABAA receptor generated GABA-gated chloride channels and binding sites for GABAA receptor ligands. Channels consisting of only α or β subunits could also be detected. These homomeric channels formed with reduced efficiencies compared to the heteromeric receptors. Both of these homomeric GABA-responsive channels were potentiated by barbiturate, indicating that sites for both ligand-gating and allosteric potentiation are present on receptors assembled from either subunit.
- Publication:
-
Science
- Pub Date:
- December 1988
- DOI:
- 10.1126/science.2848320
- Bibcode:
- 1988Sci...242.1306P