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2-Arachidonoylgylcerol: A Possible Endogenous Cannabinoid Receptor Ligand in Brain
Open accessAbstract
The effects of anadamide, 2-arachidonoylglycerol and related compounds on the specific binding of a radiolabeled cannabinoid receptor ligand,[3H]CP55940, to synaptosomal membranes were examined. Anandamide, an endogenous cannabinoid receptor ligand, reduced the specific binding of [3H]CP55940 to synaptosomal membranes in a dose-dependent manner: the Ki value was 89 nM. 2-Arachidonoylglycerol was also shown to bind appreciably to the cannabinoid receptor in competitive inhibition experiments. The apparent binding affinity was markedly increased when the binding assay was carried out in the presence of the esterase inhibitor DFP or at 0 degrees C. Free arachidonic acid and N-palmitoylethanolamine were almost inactive in terms of binding to the cannabinoid receptor in synaptosomal membranes. 2-Arachidonoylglycerol may be an endogenous cannabinoid receptor ligand in the brain.
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“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 Sugiura et al, 1995
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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
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
Pertwee, R. G. (2007) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0707442 · Cited by 2,047
Pertwee, R. G., Howlett, A. C., Abood, M. E., Alexander, S. P. H., Marzo, V. D., Elphick, M. R., Greasley, P. J., Hansen, H. S., Kunos, G., Mackie, K., et al. (2010) · Pharmacological Reviews · doi:10.1124/pr.110.003004 · Cited by 1,666
Metadata
- Authors
- Sugiura, T., Kondo, S., Sukagawa, A., Nakane, S., Shinoda, A., Itoh, K., Yamashita, A., & Waku, K.
- Affiliations
- Teikyo University (JP)
- ORCID
- Yamashita, A.
- Venue
- Biochemical and Biophysical Research Communications
- Publisher
- Elsevier BV
- Published
- 1995-10
- Volume
- 215
- Issue
- 1
- Pages
- 89-97
- ISSN
- 0006-291X (ISSN-L)
- OpenAlex
- W2085741941
- Cited by
- 2,196
- References
- 0
- Citations by year
- 2026: 22 · 2025: 61 · 2024: 68 · 2023: 63 · 2022: 59 · 2021: 113 · 2020: 97 · 2019: 68 · 2018: 77 · 2017: 74 · 2016: 79 · 2015: 84 · 2014: 87 · 2013: 82 · 2012: 95
- FWCI
- 14.31
- Type
- journal article
- Language
- en
- Open access
- Licence
- cc-by-nc-nd
- www.elsevier.com/tdm/userlicense/1.0/ (tdm)
- Locations
- Biochemical and Biophysical Research Communications (publishedVersion)
- PubMed (publishedVersion)
- Institutional Repositories DataBase (IRDB) (submittedVersion, cc-by-nc-nd)
- Topics
- Health Sciences › Medicine › Pharmacology (medical) › Cannabis and Cannabinoid Research
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Keywords
- 2-arachidonoylglycerol, anandamide, endocannabinoid system, cannabinoid receptors, synaptosomal membranes, competitive inhibition, esterase inhibition, DFP, arachidonic acid, N-palmitoylethanolamine, brain
- MeSH terms
- Animals, Arachidonic Acids, Binding, Competitive, Brain, Cannabinoids, Cyclohexanols, Dose-Response Relationship, Drug, Glycerides, Lipase, Male, Receptors, Drug, Synaptic Membranes, Tritium, Rats, Wistar, Receptors, Cannabinoid, Rats, Polyunsaturated Alkamides, Endocannabinoids
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