The DOI matches its Crossref record; 4 of the 4 references it cites were found in a registry or an index.
Cannabinol Derivatives: Binding to Cannabinoid Receptors and Inhibition of Adenylylcyclase
Open accessAbstract
Several derivatives of cannabinol and the 1,1-dimethylheptyl homolog (DMH) of cannabinol were prepared and assayed for binding to the brain and the peripheral cannabinoid receptors (CB1 and CB2), as well as for activation of CB1- and CB2-mediated inhibition of adenylylcyclase. The DMH derivatives were much more potent than the pentyl (i.e., cannabinol) derivatives. 11-Hydroxycannabinol (4a) was found to bind potently to both CB1 and CB2 (Ki values of 38.0 +/- 7.2 and 26.6 +/- 5.5 nM, respectively) and to inhibit CB1-mediated adenylylcyclase with an EC50 of 58.1 +/- 6.2 nM but to cause only 20% inhibition of CB2-mediated adenylylcyclase at 10 microM. It behaves as a specific, though not potent, CB2 antagonist. 11-Hydroxycannabinol-DMH (4b) is a very potent agonist for both CB1 and CB2 (Ki values of 100 +/- 50 and 200 +/- 40 pM; EC50 of adenylylcyclase inhibition 56.2 +/- 4.2 and 207.5 +/- 27.8 pM, respectively).
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Citations
Cites
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International Union of Pharmacology. XXVII. Classification of Cannabinoid Receptors
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Self-citationThe Endocannabinoid System as an Emerging Target of Pharmacotherapy
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Metadata
- Authors
- Rhee, M.-H., Vogel, Z., Barg, J., Bayewitch, M., Levy, R., Hanuš, L., Breuer, A., & Mechoulam, R.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 1997-09-01
- Volume
- 40
- Issue
- 20
- Pages
- 3228-3233
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1999428457
- Cited by
- 191
- References
- 4
- FWCI
- 2.92
- Type
- journal article
- Language
- en
- Open access
- green
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