The DOI matches its Crossref record; 33 of the 33 references it cites were found in a registry or an index.
Overlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake with negligible capsaicin‐like activity
Open accessAbstract
Some synthetic agonists of the VR1 vanilloid (capsaicin) receptor also inhibit the facilitated transport into cells of the endogenous cannabinoid anandamide (arachidonoylethanolamide, AEA). Here we tested several AEA derivatives containing various derivatized phenyl groups or different alkyl chains as either inhibitors of the AEA membrane transporter (AMT) in intact cells or functional agonists of the VR1 vanilloid receptor in HEK cells transfected with the human VR1. We found that four known AMT inhibitors, AM404, arvanil, olvanil and linvanil, activate VR1 receptors at concentrations 400–10 000‐fold lower than those necessary to inhibit the AMT. However, we also found three novel AEA derivatives, named VDM11, VDM12 and VDM13, which inhibit the AMT as potently as AM404 but exhibit little or no agonist activity at hVR1. These compounds are weak inhibitors of AEA enzymatic hydrolysis and poor CB 1/CB 2 receptor ligands. We show for the first time that, despite the overlap between the chemical moieties of AMT inhibitors and VR1 agonists, selective inhibitors of AEA uptake that do not activate VR1 (e.g. VDM11) can be developed.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
The source backs part of the claim, not all of it — or backs it for a different population, condition or comparison.
In the citing paper
“TRPV1 (and also cannabinoid CB 1 ) receptors are present in pain and thermoregulatory pathways (66,111,165,209,210,216).”
From Paracetamol: New Vistas of an Old Drug (2006) · cites this paper as [66]
Experimental — accuracy not yet measuredThe source backs part of the claim, not all of it — or backs it for a different population, condition or comparison.
In the citing paper
“N-arachidonoylphenolamine is an agonist at TRPV1 receptors and an inhibitor of cellular anandamide uptake, which leads to increased levels of endogenous cannabinoids”
From Paracetamol: New Vistas of an Old Drug (2006) · cites this paper as [66]
Experimental — accuracy not yet measuredThe source backs part of the claim, not all of it — or backs it for a different population, condition or comparison.
In the citing paper
“At analgesic doses of paracetamol, AM404 that is formed in rat brain regions expressing high levels of FAAH, can indirectly activate CB 1 receptors and directly activate TRPV1 receptors (66,102,235).”
From Paracetamol: New Vistas of an Old Drug (2006) · cites this paper as [66]
Experimental — accuracy not yet measuredThe source backs part of the claim, not all of it — or backs it for a different population, condition or comparison.
In the citing paper
“At this concentration AM404 activates both rat (102,235) and human (66) TRPV1 receptors, while significant COX-1 and COX-2 inhibition and prostaglandin E 2 formation reduction are obtained at micromolar concentrations (102).”
From Paracetamol: New Vistas of an Old Drug (2006) · cites this paper as [66]
Experimental — accuracy not yet measured
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
Cites
The capsaicin receptor: a heat-activated ion channel in the pain pathway
Caterina, M. J., Schumacher, M. A., Tominaga, M., Rosen, T. A., Levine, J. D., & Julius, D. J. (1997) · Nature · doi:10.1038/39807 · Cited by 9,132
Isolation and Structure of a Brain Constituent That Binds to the Cannabinoid Receptor
Devane, W. A., Hanuš, L., Breuer, A., Pertwee, R. G., Stevenson, L. A., Griffin, G., Gibson, D., Mandelbaum, A., Etinger, A., & Mechoulam, R. (1992) · Science · doi:10.1126/science.1470919 · Cited by 5,633
Self-citationCannabinoid receptor localization in brain.
Herkenham, M., Lynn, A. B., Little, M. D., Johnson, M. R., Melvin, L. S., de Costa, B. R., & Rice, K. C. (1990) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.87.5.1932 · Cited by 2,321
Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide
Zygmunt, P. M., Petersson, J., Andersson, D. A., Chuang, H.-H., Sørgård, M., Di Marzo, V., Julius, D., & Högestätt, E. D. (1999) · Nature · doi:10.1038/22761 · Cited by 2,142
Capsaicin: cellular targets, mechanisms of action, and selectivity for thin sensory neurons.
Holzer, P. D. (1991) · Pharmacological Reviews · doi:10.1016/s0031-6997(25)06664-5 · Cited by 1,784
Formation and inactivation of endogenous cannabinoid anandamide in central neurons
Marzo, V. D., Fontana, A., Cadas, H., Schinelli, S., Cimino, G., Schwartz, J.-C., & Piomelli, D. (1994) · Nature · doi:10.1038/372686a0 · Cited by 1,585
Pharmacology of cannabinoid CB1 and CB2 receptors
Pertwee, R. G. (1997) · Pharmacology & Therapeutics · doi:10.1016/s0163-7258(97)82001-3 · Cited by 1,526
Self-citationMezey, É., Tóth, Z. E., Cortright, D. N., Arzubi, M. K., Krause, J. E., Elde, R., Guo, A., Blumberg, P. M., & Szallasi, A. (2000) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.97.7.3655 · Cited by 850
Functional Role of High-Affinity Anandamide Transport, as Revealed by Selective Inhibition
Beltramo, M., Stella, N., Calignano, A., Lin, S. Y., Makriyannis, A., & Piomelli, D. (1997) · Science · doi:10.1126/science.277.5329.1094 · Cited by 813
The endogenous lipid anandamide is a full agonist at the human vanilloid receptor (hVR1)
Smart, D., Gunthorpe, M. J., Jerman, J. C., Nasir, S., Gray, J., Muir, A. I., Chambers, J. K., Randall, A. D., & Davis, J. B. (2000) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0703050 · Cited by 775
Self-citation
Research works printed but not linked: 6
- Ueda N. Puffenbarger R.A. Yamamoto S. and Deutsch D. (2000) Chem. Phys. Lipids in press.
- Holzer P., 1991, Pharmacol. Rev., 43, 143
- Di Marzo V. Breivogel C. Bisogno T. Melck D. Patrick G. Tao Q. Szallasi A. Razdan R.K. and Martin B.R. (2000) Eur. J. Pharmacol. in press.
- Jerman J.C., 2000, Br. J. Pharmacol. (Proc. Suppl.), 129, 73P
- Hayes P. Meadows H.J. Gunthorpe M.J. Harries M.H. et al. (2000) Pain in press.
- Bisogno T. Melck D. Bobrov Y. De Petrocellis L. Gretskaya N.M. Bezuglov V.V. and Di Marzo V. (2000) Biochem. J. in press.
Cited by
Sorted by citations
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-citationThe 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., 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
Self-citationRole of Endogenous Cannabinoids in Synaptic Signaling
Freund, T. F., Katona, I., & Piomelli, D. (2003) · Physiological Reviews · doi:10.1152/physrev.00004.2003 · Cited by 1,616
Metadata
- Authors
- De Petrocellis, L., Bisogno, T., Davis, J. B., Pertwee, R. G., & Di Marzo, V.
- Affiliations
- National Research Council (IT)
- University of Aberdeen (GB)
- Venue
- FEBS Letters
- Publisher
- Wiley
- Published
- 2000-10-09
- Volume
- 483
- Issue
- 1
- Pages
- 52-56
- ISSN
- 0014-5793 (ISSN-L)
- 1873-3468
- OpenAlex
- W2005828463
- Cited by
- 347
- References
- 33
- Citations by year
- 2026: 2 · 2025: 5 · 2024: 2 · 2023: 3 · 2022: 2 · 2021: 8 · 2020: 7 · 2019: 7 · 2018: 6 · 2017: 10 · 2016: 5 · 2015: 11 · 2014: 7 · 2013: 14 · 2012: 14
- FWCI
- 15.12
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- FEBS Letters (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Pharmacology (medical) › Cannabis and Cannabinoid Research
- Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
- Health Sciences › Medicine › Physiology (medical) › Pain Mechanisms and Treatments
- Keywords
- capsaicin receptor, AM404, olvanil, receptor selectivity, cannabinoid signaling
- MeSH terms
- Animals, Arachidonic Acids, Binding, Competitive, Biological Transport, Calcium, Capsaicin, Cell Line, Dose-Response Relationship, Drug, Humans, Ligands, Receptors, Drug, Tumor Cells, Cultured, Receptors, Cannabinoid, TRPV Cation Channels, Rats, Polyunsaturated Alkamides, Endocannabinoids
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
