Two new unsaturated fatty acid ethanolamides in brain that bind to the cannabinoid receptor

Journal of Medicinal Chemistry
1993.0

Abstract

Arachidonic acid ethanolamide (anandamide) was previously identified as an endogenous cannabinoid receptor ligand. Given that many arachidonic acid-derived mediators exist as families, we hypothesized additional unsaturated fatty acid ethanolamides might bind the cannabinoid receptor. We synthesized linoleylethanolamide, linolenylethanolamide, homo-γ-linolenylethanolamide (5), and 7,10,13,16-docosatetraenylethanolamide (6), then used TLC and GC-MS to compare with porcine brain extracts. Compounds 5 and 6 were identified in brain. Both are oily, with NMR spectra similar to anandamide but differing in vinyl/doubly allylic protons. GC-MS showed they form parent/dehydrated (2-oxazoline) peak pairs, with retention times distinct from anandamide. EI/CI spectra of brain-derived and synthetic 5/6 were identical. In ligand binding assays, 5 and 6 competitively displaced [³H]HU-243 from rat synaptosomal membranes, with Ki values (53.4±5.5 nM and 34.4±3.2 nM) similar to anandamide (52±1.8 nM) and Δ⁹-THC (46±3 nM). This identifies two new brain-derived cannabinoid receptor-binding ethanolamides, showing anandamide is not the sole member of this mediator class; further study is needed on their biological activity differences.

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