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An Analysis of the Putative CBD Binding Site in the Ionotropic Cannabinoid Receptors

Chanté Muller, Patricia H. Reggio

2020Frontiers in Cellular Neuroscience27 citationsDOIOpen Access PDF

Abstract

Cannabinoids have been long studied for their therapeutic properties, particularly for their use in the treatment of pain. As new therapies are sought after to treat conditions of chronic pain, so is a better understanding of the ligands and their target receptors or channels. A recently published cryo-EM structure showed the putative binding location of a well-known cannabinoid ligand, cannabidiol (CBD), in TRPV2, a channel that has been implicated in inflammation and chronic pain. TRPV2, along with TRPV1, TRPV3, TRPV4, TRPA1, and TRPM8 all have the capability to be modulated by cannabinoid ligands and are located in the peripheral nervous system. Here, we analyze the putative CBD binding site in each of these channels and compare structural and sequential information with experimental data.

Topics & Concepts

CannabidiolIonotropic effectCannabinoid receptorTRPV1Chronic painCannabinoidNeurosciencePharmacologyTransient receptor potential channelNeuropathic painBinding siteChemistryReceptorMedicineBiologyBiochemistryCannabisGlutamate receptorAntagonistPsychiatryIon Channels and ReceptorsCannabis and Cannabinoid ResearchBiochemical Analysis and Sensing Techniques
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