Arachidonylethanolamide (anandamide) binds with low affinity to dihydropyridine binding sites in brain membranes

Prostaglandins, Leukotrienes, and Essential Fatty Acids
A Jarrahian, C J Hillard

Abstract

The purpose of this study was to explore the hypothesis that the dihydropyridine (DHP) binding site of the L-type calcium channel is a high affinity binding site for the cannabimimetic arachidonylethanolamide (AEA). Binding affinities were determined from competition isotherms using the DHP analog [3H]PN-200. AEA competed for [3H]PN-200 binding with a K(I) of 40 +/- 4 microM. Inclusion of phenylmethylsulfonyl fluoride to inhibit an amidohydrolase that converts AEA to arachidonic acid had little effect on the K(I) of AEA (48 +/- 6 microM). Arachidonic acid had a slightly higher K(I) (120 +/- 11 microM) and other N-acylethanolamides examined (linolenylethanolamide, dihomo-gamma-linolenylethanolamide, docosatetraenylethanolamide, and palmitoylethanolamide) had no effect on [3H]PN-200 binding at concentrations as high as 10 microM. Our conclusions are that AEA binds to the DHP binding site with relatively low affinity and its conversion to arachidonic acid is not required for binding.

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Citations

Dec 7, 2000·Chemistry and Physics of Lipids·A C Howlett, S Mukhopadhyay
Oct 21, 2000·European Journal of Pharmacology·V Di MarzoB R Martin
Nov 27, 1998·European Journal of Pharmacology·R MechoulamV Di Marzo
Aug 1, 2002·Life Sciences·Osama M H HabayebJustin C Konje
Mar 4, 2000·The Biochemical Journal·J LiuG Kunos
Apr 1, 2009·The Journal of General Physiology·Mandy L Roberts-Crowley, Ann R Rittenhouse
Feb 6, 2014·The European Journal of Neuroscience·João Sousa-ValenteIstvan Nagy
May 8, 2009·Cell Calcium·Mandy L Roberts-CrowleyAnn R Rittenhouse
Jun 8, 2002·Prostaglandins, Leukotrienes, and Essential Fatty Acids·Vincenzo Di MarzoT Bisogno
Jun 8, 2002·Prostaglandins, Leukotrienes, and Essential Fatty Acids·T SugiuraK Waku

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