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GABA Alters GABAA Receptor mRNAs and Increases Ligand Binding
Authors:Helen Y Kim  Douglas W Sapp  Richard W Olsen  Allan J Tobin
Institution:Department of Pharmacology and Neuroscience Program, University of Colorado Health Sciences Center, Denver, Colorado, U.S.A.;Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Shizuoka-ken, Japan
Abstract:Abstract: Adenosine A2a receptors have been localized to GABAergic striatopallidal neurons, but their functional role is unknown. To address this question, the modulation of endogenous GABA release by adenosine A2a receptors was examined in slices of rat globus pallidus. The selective adenosine A2a receptor agonist CGS-21680 (3.0–10 n M ) significantly increased electrically stimulated release (overflow) of GABA, with 10 n M CGS-21680 resulting in a 44% increase compared with the control. Both the nonselective adenosine receptor antagonist 8-phenyltheophylline (10 μ M ) and the selective A2a receptor antagonist KF-17837 (100 n M ) abolished the CGS-21680-induced increase in GABA overflow. Higher concentrations of CGS-21680 (0.10–1.0 μ M ) decreased GABA overflow by ?25%.8-Phenyltheophylline (10 μ M ) antagonized these effects, whereas KF-17837 (100 n M ) did not, suggesting actions of CGS-21680 on other adenosine receptors at these concentrations. These results demonstrate that activation of adenosine A2a receptors augments electrically stimulated release of GABA from globus pallidus slices and suggest a mechanism by which adenosine may modulate GABAergic output from the striatopallidal efferent system.
Keywords:A2a receptor  GABA release  Globus pallidus  Basal ganglia  CGS-21680  KF-17837  
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