Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors.
摘要：
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.
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关键词：
Animals Mice, Inbred ICR Dogs Mice Cell Line Arachidonic Acids Glycerides Receptors, Cannabinoid Molecular Structure Gas Chromatography-Mass Spectrometry
DOI：
10.1016/0006-2952(95)00109-D
被引量：
年份：
1995
Elsevier
Taylor & Francis
BMJ
万方医学
Ingenta
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