Pharmacological Evaluation of Cannabinoid Receptor Modulators Using GRABeCB2.0 Sensor. [PDF]
Int J Mol SciCannabinoid receptors CB1R and CB2R are G-protein coupled receptors acted upon by endocannabinoids (eCBs), namely 2-arachidonoylglycerol (2-AG) and N-arachidonoyl ethanolamine (AEA), with unique pharmacology and modulate disparate physiological processes.
Shivshankar S +3 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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Life, 2022 The cannabinoid receptors CB1R and CB2R are members of the G protein-coupled receptor (GPCR) family. These receptors have recently come to light as possible therapeutic targets for conditions affecting the central nervous system. However, because CB1R is
Anjela Manandhar +3 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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Allosteric Modulators Targeting Cannabinoid cb1 and cb2 Receptors: Implications for Drug Discovery [PDF]
Future Medicinal Chemistry, 2019 Allosteric modulators of cannabinoid receptors hold great therapeutic potential, as they do not possess intrinsic efficacy, but instead enhance or diminish the receptor's response of orthosteric ligands allowing for the tempering of cannabinoid receptor ...
Francesca Gado +2 more
exaly +2 more sources
Cannabinoid receptor type-1: breaking the dogmas [version 1; referees: 3 approved]
F1000Research, 2016 The endocannabinoid system (ECS) is abundantly expressed in the brain. This system regulates a plethora of physiological functions and is composed of cannabinoid receptors, their endogenous ligands (endocannabinoids), and the enzymes involved in the ...
Arnau Busquets Garcia +3 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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British Journal of Pharmacology, 2013 BACKGROUND AND PURPOSE: The cannabinoid receptor type 1 (CB1 ) has an allosteric binding site. The drugs ORG27569 {5-chloro-3-ethyl-N-[2-[4-(1-piperidinyl)phenyl]ethyl]-1H-indole-2-carboxamide} and PSNCBAM-1 {1-(4-chlorophenyl)-3-[3-(6-pyrrolidin-1 ...
William John Redmond +2 more
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The development and therapeutic potential of classical and next-generation cannabinoid ligands
Pharmacological ResearchThe endogenous cannabinoid system (ECS) is a complex network that plays a crucial role in various physiological processes, and its modulation through cannabinoid ligands has garnered significant interest in pharmacological research. Cannabinoid receptors,
Verónica Muñoz-Canales +4 more
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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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