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  • Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors.

Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors.

Biochemical pharmacology (1995-06-29)
R Mechoulam, S Ben-Shabat, L Hanus, M Ligumsky, N E Kaminski, A R Schatz, A Gopher, S Almog, B R Martin, D R Compton
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 delta 9-tetrahydrocannabinol (delta 9-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 delta 9-THC to inhibit electrically evoked contractions of mouse isolated vasa deferentia; however, it was less potent than delta 9-THC.

MATERIALS
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Supelco
N,O-Bis(trimethylsilyl)trifluoroacetamide, for GC derivatization, LiChropur, ≥99.0%