The DOI matches its Crossref record; 42 of the 42 references it cites were found in a registry or an index.
Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors
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.
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In the citing paper
“The most studied endogenous ligands that bind cannabinoid receptors are AEA (Devane et al, 1992) and 2arachidonoylglycerol (2-AG) (Mechoulam et al, 1995;Sugiura et al, 1995).”
From The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain (2018) · cites this paper as Mechoulam et al, 1995
In the citing paper
“Enriching the picture further, the actions of AEA are not restricted to CB1R, given that ECBs also act, sometimes in a non-retrograde manner, at CB2R [30], GPR55 [31], and TRPV1 (transient receptor potential vanilloid type 1) channels [32–34], as well as other G protein subtypes such as Gs and/or Gq11 [35,36].”
From Amygdala FAAH and anandamide: mediating protection and recovery from stress (2013) · cites this paper as [30]
Citations
Cites
Isolation and Structure of a Brain Constituent That Binds to the Cannabinoid Receptor
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Self-citationMolecular characterization of a peripheral receptor for cannabinoids
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Determination and characterization of a cannabinoid receptor in rat brain
Devane, W. A., Dysarz, F. A., Johnson, M. R., Melvin, L. S., & Howlett, A. C. (1988) · Molecular Pharmacology · doi:10.1016/s0026-895x(25)09876-1 · Cited by 2,443
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(1988) · International Journal of Biochemistry · doi:10.1016/0020-711x(88)90084-5 · Cited by 1,458
Enzymatic synthesis and degradation of anandamide, a cannabinoid receptor agonist
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Research works printed but not linked: 1
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International Union of Pharmacology. XXVII. Classification of Cannabinoid Receptors
Howlett, A. C., Barth, F., Bonner, T. I., Cabral, G., Casellas, P., Devane, W. A., Felder, C. C., Herkenham, M., Mackie, K., Martin, B. R., et al. (2002) · Pharmacological Reviews · doi:10.1124/pr.54.2.161 · Cited by 2,819
Self-citationGut microbiome and health: mechanistic insights
de Vos, W. M., Tilg, H., Van Hul, M., & Cani, P. D. (2022) · Gut · doi:10.1136/gutjnl-2021-326789 · Cited by 2,388
The Endocannabinoid System as an Emerging Target of Pharmacotherapy
Pacher, P., Bátkai, S., & Kunos, G. (2006) · Pharmacological Reviews · doi:10.1124/pr.58.3.2 · Cited by 2,077
The molecular logic of endocannabinoid signalling
Piomelli, D. (2003) · Nature Reviews Neuroscience · doi:10.1038/nrn1247 · Cited by 1,957
A second endogenous cannabinoid that modulates long-term potentiation
Stella, N., Schweitzer, P., & Piomelli, D. (1997) · Nature · doi:10.1038/42015 · Cited by 1,496
Metadata
- Authors
- Mechoulam, R., Ben-Shabat, S., Hanus, L., Ligumsky, M., Kaminski, N. E., Schatz, A. R., Gopher, A., Almog, S., Martin, B. R., Compton, D. R., Pertwee, R. G., Griffin, G., Bayewitch, M., Barg, J., & Vogel, Z.
- Affiliations
- Hebrew University of Jerusalem (IL)
- Michigan State University (US)
- Virginia Commonwealth University (US)
- Sheba Medical Center (IL)
- University of Aberdeen (GB)
- Weizmann Institute of Science (IL)
- Corresponding author
- Mechoulam, Raphael
- Venue
- Biochemical Pharmacology
- Publisher
- Elsevier BV
- Published
- 1995-06
- Volume
- 50
- Issue
- 1
- Pages
- 83-90
- ISSN
- 0006-2952 (ISSN-L)
- OpenAlex
- W2024653583
- Cited by
- 2,913
- References
- 42
- Citations by year
- 2026: 27 · 2025: 69 · 2024: 89 · 2023: 84 · 2022: 103 · 2021: 125 · 2020: 118 · 2019: 110 · 2018: 89 · 2017: 105 · 2016: 112 · 2015: 109 · 2014: 98 · 2013: 104 · 2012: 137
- FWCI
- 22.43
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Biochemical Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Wellcome Trust
- National Institutes of Health (5r01da008169-02)
- U.S. Public Health Service
- National Institute on Drug Abuse (DA 8169, DA-3672)
- Topics
- Health Sciences › Medicine › Pharmacology (medical) › Cannabis and Cannabinoid Research
- Health Sciences › Nursing › Nutrition and Dietetics › Fatty Acid Research and Health
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Eicosanoids and Hypertension Pharmacology
- Keywords
- 2-arachidonoylglycerol, endocannabinoids, cannabinoid receptors, CB1 receptor, CB2 receptor, canine intestine, adenylate cyclase inhibition, forskolin, delta-9-tetrahydrocannabinol, antinociception, immobility, hypothermia, vas deferens contraction, structure elucidation
- MeSH terms
- Animals, Arachidonic Acids, Cannabinoids, Cell Line, Dogs, Glycerides, Intestines, Male, Gas Chromatography-Mass Spectrometry, Mice, Inbred ICR, Receptors, Drug, Molecular Structure, Receptors, Cannabinoid, Mice, Endocannabinoids
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