ArticleFrontiers in molecular biosciences2020
A Closer Look at Anandamide Interaction With TRPV1.
Article in Frontiers in molecular biosciences, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 48 citations in OpenAlex.
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- Expression, Distribution and Function of the Transient Receptor Potential Vanilloid Type 1 (TRPV1) in Endometrial Cancer.International journal of molecular sciences · 2025Article
- Anandamide Modulates Thermal Avoidance in Caenorhabditis elegans Through Vanilloid and Cannabinoid Receptor Interplay.Neurochemical research · 2024Article
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- Anandamide modulation of monocyte-derived Langerhans cells: implications for immune homeostasis and skin inflammation.Frontiers in immunology · 2024Article
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- Potent dual MAGL/FAAH inhibitor AKU-005 engages endocannabinoids to diminish meningeal nociception implicated in migraine pain.The journal of headache and pain · 2023Article
- Natural Active Ingredients and TRPV1 Modulation: Focus on Key Chemical Moieties Involved in Ligand-Target Interaction.Plants (Basel, Switzerland) · 2023Review
- Endocannabinoids produced in photoreceptor cells in response to light activateScience signaling · 2022Article
- Cannabidiol (CBD) as a novel treatment in the early phases of psychosis.Psychopharmacology · 2022Review
- The Endocannabinoid System and Physical Activity-A Robust Duo in the Novel Therapeutic Approach against Metabolic Disorders.International journal of molecular sciences · 2022Review
- Anti-Microbial Activity of Phytocannabinoids and Endocannabinoids in the Light of Their Physiological and Pathophysiological Roles.Biomedicines · 2022Review
- Targeting CB2 and TRPV1: Computational Approaches for the Identification of Dual Modulators.Frontiers in molecular biosciences · 2022Article
- Chronic Pain and the Endocannabinoid System: Smart Lipids - A Novel Therapeutic Option?Medical cannabis and cannabinoids · 2022Review
- The interaction of TRPV1 and lipids: Insights into lipid metabolism.Frontiers in physiology · 2022Review
- Potassium channels as molecular targets of endocannabinoids.Channels (Austin, Tex.) · 2021Review
- TRPV1 channels as a newly identified target for vitamin D.Channels (Austin, Tex.) · 2021Review
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The transient receptor potential subfamily vanilloid type 1 ion channel (TRPV1), located in the peripheral nervous system has been implicated in the perception of pain and possesses the ability to be modulated by various cannabinoid ligands. Because of its location, TRPV1 is an ideal target for the development of novel pain therapeutics. Literature precedent suggests a wide range of cannabinoid ligands can activate TRPV1, but the location and mode of entry is not well understood. Understanding the modes in which cannabinoids can enter and bind to TRPV1 can aid in rational drug design. The first endogenous ligand identified for TRPV1 was the endocannabinoid, anandamide (AEA). The Molecular Dynamics (MD) studies discussed here investigate the entry mode of AEA into TRPV1. During the course of the 10+ microsecond MD simulations, two distinct binding modes were observed: AEA binding in the tunnel formed by the S1-S4 region, and AEA binding in the vanilloid binding pocket, with preference for the former. Unbiased MD simulations have revealed multiple spontaneous binding events into the S1-S4 region, with only one event of AEA binding the vanilloid binding pocket. These results suggest that AEA enters TRPV1 via a novel location between helices S1-S4 via the lipid bilayer.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.