Abstract

In this study, we report the isolation from canine intestines of 2-arachidonyl glycerol (2-Ara-Gl). Its structure was determined by mass spectrometry and by direct comparison with a synthetic sample. 2-Ara-Gl bound to membranes from cells transiently transfected with expression plasmids carrying DNA of either CB1 or CB2—the two cannabinoid receptors identified thus far—with Ki values of 472 ± 55 and 1400 ± 172 nM, respectively. In the presence of forskolin, 2-Ara-Gl inhibited adenylate cyclase in isolated mouse spleen cells, at the potency level of Δ9-tetrahydrocannabinol (Δ9-THC). Upon intravenous administration to mice, 2-Ara-Gl caused the typical tetrad of effects produced by THC: antinociception, immobility, reduction of spontaneous activity, and lowering of the rectal temperature. 2-Ara-Gl also shares the ability of Δ9-THC to inhibit electrically evoked contractions of mouse isolated vasa deferentia; however, it was less potent than Δ9-THC.

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Anandamide

Authors
Raphael Mechoulam, Shimon Ben-Shabat, Lumir Hanus, Moshe Ligumsky, Norbert E Kaminski, Anthony R Schatz, Asher Gopher, Shlomo Almog, Billy R Martin, David R Compton, Roger G Pertwee, Graeme Griffin, Michael Bayewitch, Jacob Barg, ZVI Vogel 29 Jun 1995 Biochemical pharmacology 50 1 83-90 Elsevier
Publication date
29 June, 1995
Journal
Biochemical pharmacology
Volume
50
Issue
1
Pages
83-90
Publisher
Elsevier

Keywords