Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors
Biochemical pharmacology, 1995•Elsevier
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 …
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 …
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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