Cited by 356Cannabis and Cannabinoid ResearchIon Channels and ReceptorsPain Mechanisms and Treatments

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Overlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake with negligible capsaicin‐like activity

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De Petrocellis, Luciano, Bisogno, Tiziana, Davis, John B, Pertwee, Roger G, Di Marzo, Vincenzo·2000·FEBS Letters

DOI 10.1016/s0014-5793(00)02082-2

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Abstract

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.

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Authors: De Petrocellis, L., Bisogno, T., Davis, J. B., Pertwee, R. G., & Di Marzo, V.
Affiliations: National Research Council (IT)
University of Aberdeen (GB)
ORCID: Bisogno, Tiziana
Pertwee, Roger G
Venue: FEBS Letters
Publisher: Wiley
Published: 2000-10-09
Volume: 483
Issue: 1
Pages: 52-56
ISSN: 0014-5793 (ISSN-L)
1873-3468
DOI: 10.1016/s0014-5793(00)02082-2
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
Licence: onlinelibrary.wiley.com/termsAndConditions#vor (vor)
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

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Overlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake with negligible capsaicin‐like activity

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