TY - JOUR
T1 - Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors
AU - Mechoulam, Raphael
AU - Ben-Shabat, Shimon
AU - Hanus, Lumir
AU - Ligumsky, Moshe
AU - Kaminski, Norbert E.
AU - Schatz, Anthony R.
AU - Gopher, Asher
AU - Almog, Shlomo
AU - Martin, Billy R.
AU - Compton, David R.
AU - Pertwee, Roger G.
AU - Griffin, Graeme
AU - Bayewitch, Michael
AU - Barg, Jacob
AU - Vogel, Zvi
PY - 1995/6/29
Y1 - 1995/6/29
N2 - 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.
AB - 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.
KW - 2-arachidonyl glycerol
KW - adenylate cyclase inhibition
KW - anandamide
KW - arachidonylethanolamide
KW - immune system
KW - mouse behavior
KW - tetrahydrocannabinol
KW - transfection
UR - https://www.scopus.com/pages/publications/0029012014
U2 - 10.1016/0006-2952(95)00109-D
DO - 10.1016/0006-2952(95)00109-D
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C2 - 7605349
AN - SCOPUS:0029012014
SN - 0006-2952
VL - 50
SP - 83
EP - 90
JO - Biochemical Pharmacology
JF - Biochemical Pharmacology
IS - 1
ER -