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Unraveling GPCRs Allosteric Modulation. Cannabinoid 1 Receptor as a Case Study.
Proteins
November 2024
Department of Chemistry, University of Southern California, Los Angeles, California, USA.
G-protein-coupled receptors (GPCRs) constitute one of the most prominent families of integral membrane receptor proteins that mediate most transmembrane signaling processes. Malfunction of these signal transduction processes is one of the underlying causes of many human pathologies (Parkinson's, Huntington's, heart diseases, etc), provoking that GPCRs are the largest family of druggable proteins. However, these receptors have been targeted traditionally by orthosteric ligands, which usually causes side effects due to the simultaneous targeting of homologous receptor subtypes.
View Article and Find Full Text PDFA Review of Cardiovascular Effects of Marijuana Use.
J Cardiopulm Rehabil Prev
November 2024
Author Affiliations: Marshfield Clinic Research Institute, Marshfield, Wisconsin (Dr Rezkalla); Cardiovascular Research Institute, Huntington Medical Research Institutes, Pasadena, California (Dr Kloner); and Cardiovascular Division, Dept. of Medicine, Keck School of Medicine of University of Southern California, Los Angeles, California (Dr Kloner).
Objective: Cannabinoids exert their effects on body tissues via cannabinoid 1 (CB1) and cannabinoid 2 (CB2) receptors. Receptors are present in brain, myocardium, vascular endothelium, platelets, and adipose tissues. Under normal physiologic conditions, endocannabinoid effects are minimal.
View Article and Find Full Text PDFA combination of peripherally restricted CB and CB cannabinoid receptor agonists reduces bladder afferent sensitisation in cystitis.
Eur J Pharmacol
December 2024
Discipline of Human Physiology, Flinders Health & Medical Research Institute, College of Medicine and Public Health, Flinders University, South Australia, Australia. Electronic address:
Cannabinoid agonists can potentially ameliorate lower urinary tract symptoms (LUTS), including pain associated with interstitial cystitis/bladder pain syndrome (IC/BPS). This study aims to determine the contributions of the cannabinoid 1 receptors (CBRs) and CBRs in regulating the activity of different functional classes of afferents, comparing normal healthy bladder with bladders from guinea pigs with protamine/zymosan-induced cystitis. The mechanosensitivity of different functional afferent classes was determined by ex vivo single-unit extracellular recordings.
View Article and Find Full Text PDFVisual exposure to green light therapy reduces knee joint pain and alters the lipidome in osteoarthritic rats.
Pain
October 2024
Departments of Pharmacology and Anaesthesia, Pain Management & Perioperative Medicine, Dalhousie University, Halifax, NS, Canada.
Visual exposure to dim, green, light has been found to reduce pain levels in patients living with migraine, low back pain, and fibromyalgia. Preclinical studies discovered that the analgesic effect of green light was due to the central release of endogenous opioids and a reduction in inflammatory cytokines in the cerebrospinal fluid. The present study assessed the effect of green light therapy (GLT) on joint pain in a rat model of osteoarthritis (OA) and investigated the role of endolipids.
View Article and Find Full Text PDFProteomic Profile of Circulating Extracellular Vesicles in the Brain after Δ9-Tetrahydrocannabinol Inhalation.
Biomolecules
September 2024
Department of Neurobiology and Behavior, University of California Irvine, Irvine, CA 92697, USA.
Article Synopsis
- The study investigates how the main active component of cannabis, THC, affects the signaling of extracellular vesicles (EVs) in the brain, which play a role in intercellular communication.
- THC was found to activate certain cells in the brain, leading to increased expression of cannabinoid receptors and the release of EVs containing RNA.
- Additionally, the research showed that both acute and chronic THC exposure had different effects on EV proteins, with variations based on sex, enhancing our understanding of cannabis's impact on brain signaling.
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