Differential pharmacology of GABAA and GABAC receptors on rat retinal bipolar cells

European Journal of Pharmacology
A Feigenspan, J Bormann

Abstract

GABAA and GABAC receptors were studied on cultured or freshly isolated rat retinal bipolar cells. The cells displayed GABA-induced whole-cell currents, which were only partially blocked by high concentrations (100 microM) of the GABAA receptor antagonist bicuculline. The bicuculline-resistant (GABAC) component was insensitive to the GABAA receptor modulators flunitrazepam (1 microM) and pentobarbital (50 microM). The bicuculline-sensitive portion of the current was strongly augmented by both drugs, indicating that it was mediated by conventional GABAA receptors. The GABAC and GABAA receptor subtypes displayed a 7-fold difference in their binding affinity for GABA, the EC50 values being 4.2 microM and 27.1 microM, respectively. The Hill coefficient was approximately 2 for both receptors. The bicuculline-insensitive GABAC receptors were markedly blocked by 100 microM picrotoxinin, 2-(3-carboxypropyl)-3-amino-6-(4-methoxyphenyl)pyridazinium bromide (SR-95531) and gamma-hexachlorocyclohexane, drugs known to be antagonists of GABAA receptors. Examination of single-channel currents indicated main-state conductances of 7.9 pS and 29.6 pS for GABAC and GABAA receptors, respectively. The pore diameter of open GABAC receptor channels was...Continue Reading

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Citations

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Aug 7, 2010·Psychopharmacology·Candy Flores-GraciaMiguel Pérez de la Mora
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