The DOI matches its Crossref record; 16 of the 16 references it cites were found in a registry or an index.
The Biodisposition and Metabolism of Anandamide in Mice
Abstract
The endogenous cannabinoid anandamide (AN) has been reported to produce pharmacological effects similar to those of delta9-tetrahydrocannabinol but with a shorter duration of action. Also, AN is known to be metabolized to arachidonic acid. The purpose of this study was to examine the time course of distribution and metabolism of AN. Male mice were each administered 20 microCi 3H-AN and 50 mg/kg AN (i.v.). At 1, 5, 15 and 30 min after administration, the animals were sacrificed, and various tissues were removed, solubilized and counted to determine the distribution of 3H. Also, samples from brain, adrenal gland and plasma were extracted with ethyl acetate and analyzed by HPLC to separate 3H-labeled AN, arachidonic acid and other metabolites. AN was detectable in brain by 1 min after injection. At 1 min after injection, the rank order of radioactivity per milligram or microliter of tissue was adrenal > lung > kidney > plasma > heart > liver > diaphragm > brain > fat. Although the 1 and 5 min metabolic profiles of brain 3H showed that AN was clearly present, most AN had already been transformed to arachidonic acid and other polar metabolites, and there were almost no detectable brain levels of AN at 15 and 30 min. In plasma and adrenal gland, AN was the predominant form at 1 and 5 min. Our experiments confirm that AN quickly reaches the brain and suggest that rapid metabolism of AN plays a key role in the time course of the pharmacological activity of this naturally occurring cannabinoid receptor ligand.
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“eCBs and their structural analogs are able to cross the blood brain barrier (Willoughby et al, 1997;Glaser et al, 2006).”
From Acute stress increases circulating anandamide and other N-acylethanolamines in healthy humans (2012) · cites this paper as Willoughby et al, 1997
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Self-citationEndocannabinoids: endogenous cannabinoid receptor ligands with neuromodulatory action
Marzo, V. D., Melck, D. J., Bisogno, T., & PETROCELLIS, L. D. (1998) · Trends in Neurosciences · doi:10.1016/s0166-2236(98)01283-1 · Cited by 722
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Metadata
- Authors
- Willoughby, K. A., Moore, S. F., Martin, B. R., & Ellis, E. F.
- Affiliations
- Virginia Commonwealth University (US)
- Corresponding author
- Ellis, Earl F.
- Venue
- The Journal of Pharmacology and Experimental Therapeutics
- Publisher
- Elsevier BV
- Published
- 1997-07
- Volume
- 282
- Issue
- 1
- Pages
- 243-247
- ISSN
- 0022-3565 (ISSN-L)
- OpenAlex
- W2259059236
- Cited by
- 159
- References
- 16
- Citations by year
- 2026: 2 · 2025: 1 · 2024: 2 · 2023: 4 · 2022: 5 · 2021: 4 · 2020: 3 · 2019: 5 · 2017: 5 · 2016: 3 · 2015: 3 · 2014: 4 · 2013: 6 · 2012: 8
- FWCI
- 6.19
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Pharmacology and Experimental Therapeutics (publishedVersion)
- PubMed (publishedVersion)
- PubMed
- Funders
- National Institutes of Health (5r01da008677-03)
- National Institute on Drug Abuse (DA-08677)
- Topics
- Health Sciences › Medicine › Pharmacology (medical) › Cannabis and Cannabinoid Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Eicosanoids and Hypertension Pharmacology
- Health Sciences › Nursing › Nutrition and Dietetics › Fatty Acid Research and Health
- Keywords
- anandamide, endocannabinoids, tissue distribution, metabolism, arachidonic acid, brain, adrenal gland, plasma, polar metabolites, cannabinoid receptor ligands, pharmacokinetics
- MeSH terms
- Animals, Arachidonic Acids, Brain, Cannabinoids, Male, Mice, Inbred ICR, Motor Activity, Tissue Distribution, Mice, Polyunsaturated Alkamides, Endocannabinoids
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