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Updated: Aug 11, 2026

Using an α-Bungarotoxin Binding Site Tag to Study GABA A Receptor Membrane Localization and Trafficking
Published on: March 28, 2014
GABA(B) auto- versus hetero-receptor sensitivity: implications for novel pharmacotherapy
B Yu1, K Yamada, J P Gallagher
1Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston 77555-1031, USA.
Abstract:
After uncoupling G-protein dependent post-synaptic GABA(B) receptors--without altering GABA(B) nerve terminal receptors--we demonstrate that the GABA(B) agonist, CGP44533, exhibits less efficacy and potency at GABA(B) auto- versus hetero-receptors. CGP44533 (1 and 10 microM) depressed monosynaptic GABA(A)-mediated transmission by 2 and 35%, but depressed glutamate mediated transmission by 41 and 78%, respectively. These data suggest a differential pharmacological sensitivity for CGP44533 at glutamate versus GABA releasing neurons.
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