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Benzodiazepine Treatment Causes Uncoupling of Recombinant GABA~A~ Receptors Expressed in Stably Transfected Cells by Ronald L. Klein; Paul J. Whiting; R. Adron Harris is a Neuroscience article available to read on EtoBox.

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Abstract: GABA~A~ and benzodiazepine receptors are allosterically coupled, and occupation of either receptor site increases the affinity of the other. Chronic exposure of primary neuronal cultures to benzodiazepine agonists reduces these allosteric interactions. Neurons express multiple GABA~A~ receptor subunits, and it has been suggested that uncoupling is due to changes in the subunit composition of the receptor. To determine if uncoupling could be observed with expression of defined subunits, mouse Ltk^−^ cells stably transfected with GABA~A~ receptors (bovine α1, β1, and γ2L subunits) were treated with flunitrazepam (Flu) or clonazepam. The increase in [^3^H]Flu binding affinity caused by GABA (GABA shift or coupling) was significantly reduced in cells treated chronically with the benzodiazepines, whereas the __K__~D~ and __B__~max~ of [^3^H]Flu binding were unaffected. The uncoupling caused by clonazepam treatment occurred rapidly with a __t__~1/2~ of ∼30 min. The EC~50~ for clonazepam treatment was ∼0.3 μ__M__, and cotreatment with the benzodiazepine antagonist Ro 15‐1788 (5.6 μ__M__) prevented the effect of clonazepam. The uncoupling observed in this system was not accompani

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Author

Ronald L. Klein; Paul J. Whiting; R. Adron Harris

Publisher

John Wiley and Sons; Wiley (Blackwell Publishing); Blackwell Publishing Inc.; Wiley (ISSN 0022-3042)

Published

1994

Language

EN

Field

Neuroscience (Life Sciences)