Cholesterol as a modulator of cannabinoid receptor CB2 signaling [PDF]
Scientific Reports, 2021 Signaling through integral membrane G protein-coupled receptors (GPCRs) is influenced by lipid composition of cell membranes. By using novel high affinity ligands of human cannabinoid receptor CB2, we demonstrate that cholesterol increases basal ...
Alexei Yeliseev +7 more
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The Role of Cannabinoid Receptors in the Descending Modulation of Pain
Pharmaceuticals, 2010 The endogenous antinociceptive descending pathway represents a circuitry of the supraspinal central nervous system whose task is to counteract pain. It includes the periaqueductal grey (PAG)-rostral ventromedial medulla (RVM)-dorsal horn (DH) axis, which
Francesco Rossi +4 more
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Multiple binding modes underlie Cannabis sativa cannabinoids recognition by peroxisome proliferator-activated receptor gamma [PDF]
Frontiers in BioinformaticsIntroductionPeroxisome proliferator-activated receptor gamma (PPARγ) is a ligand-activated nuclear receptor with broad therapeutic relevance across various pathologies, including type 2 diabetes, obesity, cancer, and inflammatory disorders.
N. R. Carina Alves +4 more
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Frontiers in Pharmacology, 2022 Positive allosteric modulation of the type 1 cannabinoid receptor (CB1R) has substantial potential to treat both neurological and immune disorders.
Asher L. Brandt +10 more
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Direct modulation of human GABA-A α1β2γ2 receptors by the endocannabinoid 2-arachidonoylglycerol: implications for cannabinoid-related ligands and limitations for anxiolytic drug development [PDF]
Frontiers in NeuroscienceAnxiety disorders are associated with impaired inhibitory neurotransmission mediated by γ-aminobutyric acid type A (GABA-A) receptors. Although benzodiazepines remain effective anxiolytics, their clinical utility is limited by sedation, cognitive ...
Edgar Mixcoha +6 more
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Structural basis for positive allosteric regulation of CB2 receptor [PDF]
Nature CommunicationsThe synthetic positive allosteric modulator (PAM) of cannabinoid receptor CB2, Ec21a, exhibits better subtype selectivity and receptor specificity over orthosteric ligands, which holds promise for treating neuropathic pain and seizure without causing ...
Xuehui Wang +7 more
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Endocannabinoid Modulation in Headache: Mechanisms, Models, and Translational Therapies [PDF]
CellsHeadache disorders, including migraine, tension-type headache, trigeminal autonomic cephalalgias, post-traumatic headache and medication overuse headache, represent a major global health burden and remain difficult to treat despite therapeutic advances ...
Jie Wen, Yumin Zhang
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Cannabinoid CB1 receptors drive oligodendrocyte maturation during myelin regeneration [PDF]
Cell Communication and SignalingOligodendrocytes, the myelin-producing cells in the central nervous system, derive from oligodendrocyte progenitor cells during both development and remyelination.
Sara Ezquerro-Herce +6 more
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Cells, 2021 The endocannabinoid (eCB) system has been found in all visual parts of the central ner-vous system and plays a role in the processing of visual information in many species, including monkeys and humans. Using anatomical methods, cannabinoid receptors are
Joseph Bouskila +4 more
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CB1 Cannabinoid Receptor Signaling and Biased Signaling
Molecules, 2021 The CB1 cannabinoid receptor is a G-protein coupled receptor highly expressed throughout the central nervous system that is a promising target for the treatment of various disorders, including anxiety, pain, and neurodegeneration.
Luciana M. Leo, Mary E. Abood
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