The DOI matches its Crossref record; 49 of the 49 references it cites were found in a registry or an index.
The Activity of Anandamide at Vanilloid VR1 Receptors Requires Facilitated Transport across the Cell Membrane and Is Limited by Intracellular Metabolism
Open accessAbstract
The endogenous ligand of CB(1) cannabinoid receptors, anandamide, is also a full agonist at vanilloid VR1 receptors for capsaicin and resiniferatoxin, thereby causing an increase in cytosolic Ca(2+) concentration in human VR1-overexpressing (hVR1-HEK) cells. Two selective inhibitors of anandamide facilitated transport into cells, VDM11 and VDM13, and two inhibitors of anandamide enzymatic hydrolysis, phenylmethylsulfonyl fluoride and methylarachidonoyl fluorophosphonate, inhibited and enhanced, respectively, the VR1-mediated effect of anandamide, but not of resiniferatoxin or capsaicin. The nitric oxide donor, sodium nitroprusside, known to stimulate anandamide transport, enhanced anandamide effect on the cytosolic Ca(2+) concentration. Accordingly, hVR1-HEK cells contain an anandamide membrane transporter inhibited by VDM11 and VDM13 and activated by sodium nitroprusside, and an anandamide hydrolase activity sensitive to phenylmethylsulfonyl fluoride and methylarachidonoyl fluorophosphonate, and a fatty acid amide hydrolase transcript. These findings suggest the following. (i) Anandamide activates VR1 receptors by acting at an intracellular site. (ii) Degradation by fatty acid amide hydrolase limits anandamide activity on VR1; and (iii) the anandamide membrane transporter inhibitors can be used to distinguish between CB(1) or VR1 receptor-mediated actions of anandamide. By contrast, the CB(1) receptor antagonist SR141716A inhibited also the VR1-mediated effect of anandamide and capsaicin on cytosolic Ca(2+) concentration, although at concentrations higher than those required for CB(1) antagonism.
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Cites
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Isolation and Structure of a Brain Constituent That Binds to the Cannabinoid Receptor
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Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide
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Vanilloid (Capsaicin) Receptors and Mechanisms
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SR141716A, a potent and selective antagonist of the brain cannabinoid receptor
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Self-citationPharmacology of cannabinoid CB1 and CB2 receptors
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Functional Role of High-Affinity Anandamide Transport, as Revealed by Selective Inhibition
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Cited by
Huang, S. M., Bisogno, T., Trevisani, M., Al-Hayani, A., De Petrocellis, L., Fezza, F., Tognetto, M., Petros, T. J., Krey, J. F., Chu, C. J., et al. (2002) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.122196999 · Cited by 964
Self-citationCannabinoid Ligands Targeting TRP Channels
Muller, C., Morales, P., & Reggio, P. H. (2019) · Frontiers in Molecular Neuroscience · doi:10.3389/fnmol.2018.00487 · Cited by 567
Cannabinoid receptors and their ligands
Pertwee, R. G., & Ross, R. A. (2002) · Prostaglandins, Leukotrienes and Essential Fatty Acids (PLEFA) · doi:10.1054/plef.2001.0341 · Cited by 561
Melis, M., Pistis, M., Perra, S., Muntoni, A. L., Pillolla, G., & Gessa, G. L. (2004) · The Journal of Neuroscience · doi:10.1523/jneurosci.4503-03.2004 · Cited by 478
Inverse agonism and neutral antagonism at cannabinoid CB1 receptors
Pertwee, R. G. (2005) · Life Sciences · doi:10.1016/j.lfs.2004.10.025 · Cited by 444
Metadata
- Authors
- De Petrocellis, L., Bisogno, T., Maccarrone, M., Davis, J. B., Finazzi-Agrò, A., & Di Marzo, V.
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 2001-04
- Volume
- 276
- Issue
- 16
- Pages
- 12856-12863
- ISSN
- 0021-9258 (ISSN-L)
- OpenAlex
- W2161954110
- Cited by
- 355
- References
- 49
- FWCI
- 20.16
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- De Petrocellis, L., Bisogno, T., Maccarrone, M., Davis, J. B., Finazzi-Agrò, A., & Di Marzo, V. (2001). The Activity of Anandamide at Vanilloid VR1 Receptors Requires Facilitated Transport across the Cell Membrane and Is Limited by Intracellular Metabolism. Journal of Biological Chemistry. https://doi.org/10.1074/jbc.m008555200
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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