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Unsaturated Free Fatty Acids Increase Benzodiazepine Receptor Agonist Binding Depending on the Subunit Composition of the GABA~A~ Receptor Complex by M. R. Witt; S. E. Westh-Hansen; P. Baad Rasmussen; S. Hastrup; M. Nielsen is a Neuroscience article available to read on EtoBox.

What is Unsaturated Free Fatty Acids Increase Benzodiazepine Receptor Agonist Binding Depending on the Subunit Composition of the GABA~A~ Receptor Complex about?

Abstract: It has been shown previously that unsaturated free fatty acids (FFAs) strongly enhance the binding of agonist benzodiazepine receptor ligands and GABA~A~ receptor ligands in the CNS in vitro. To investigate the selectivity of this effect, recombinant human GABA~A~/benzodiazepine receptor complexes formed by different subunit compositions (α~x~β~y~γ~2~, __x__ = 1, 2, 3, and 5; __y__ = 1, 2, and 3) were expressed using the baculovirus‐transfected Sf9 insect cell system. At 10^−4^__M__, unsaturated FFAs, particularly arachidonic (20:4) and docosahexaenoic (22:6) acids, strongly stimulated (>200% of control values) the binding of [^3^H]flunitrazepam ([^3^H]FNM) to the α~3~β~2~γ~2~ receptor combination in whole cell preparations. No effect or small increases in levels of unsaturated FFAs on [^3^H]FNM binding to α~1~β~x~γ~2~ and α~2~β~x~γ~2~ receptor combinations were observed, and weak effects (130% of control values) were detected using the α~5~β~2~γ~2~ receptor combination. The saturated FFAs, stearic and palmitic acids, were without effect on [^3^H]FNM binding to any combination of receptor complexes. The hydroxylated unsaturated FFAs, ricinoleic and ricinelaidic acids, wer

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Author

M. R. Witt; S. E. Westh-Hansen; P. Baad Rasmussen; S. Hastrup; M. Nielsen

Publisher

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

Published

1996

Language

EN

Field

Neuroscience (Life Sciences)