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Cholesterol as a modulator of cannabinoid receptor CB2 signaling [PDF]

open access: yesScientific 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
doaj   +3 more sources

Pharmacological Evaluation of Cannabinoid Receptor Modulators Using GRABeCB2.0 Sensor. [PDF]

open access: yesInt J Mol Sci
Cannabinoid 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. A genetically encoded GPCR activation-based sensor that was developed recently—GRABeCB2.0—has been
Shivshankar S   +3 more
europepmc   +3 more sources

Endocannabinoid Modulation in Headache: Mechanisms, Models, and Translational Therapies [PDF]

open access: yesCells
Headache 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
doaj   +2 more sources

Phytocannabinoids as Novel SGLT2 Modulators for Renal Glucose Reabsorption in Type 2 Diabetes Management [PDF]

open access: yesPharmaceuticals
Background: Sodium–glucose cotransporter 2 (SGLT2) inhibitors have transformed type 2 diabetes mellitus (T2DM) management by promoting glucosuria, lowering glycated hemoglobin (HbA1c), blood pressure, and weight; however, their use is limited by ...
Raymond Rubianto Tjandrawinata   +4 more
doaj   +2 more sources

The Vertical and Horizontal Pathways in the Monkey Retina Are Modulated by Typical and Atypical Cannabinoid Receptors

open access: yesCells, 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
doaj   +1 more source

Microglial Cannabinoid CB2 Receptors in Pain Modulation

open access: yesInternational Journal of Molecular Sciences, 2023
Pain, especially chronic pain, can strongly affect patients’ quality of life. Cannabinoids ponhave been reported to produce potent analgesic effects in different preclinical pain models, where they primarily function as agonists of Gi/o protein-coupled cannabinoid CB1 and CB2 receptors.
Kangtai Xu   +5 more
openaire   +2 more sources

CB1 Cannabinoid Receptor Signaling and Biased Signaling

open access: yesMolecules, 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
doaj   +1 more source

Understanding the Dynamics of the Structural States of Cannabinoid Receptors and the Role of Different Modulators

open access: yesLife, 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
doaj   +1 more source

In Silico Prediction and Validation of CB2 Allosteric Binding Sites to Aid the Design of Allosteric Modulators

open access: yesMolecules, 2022
Although the 3D structures of active and inactive cannabinoid receptors type 2 (CB2) are available, neither the X-ray crystal nor the cryo-EM structure of CB2-orthosteric ligand-modulator has been resolved, prohibiting the drug discovery and development ...
Jiayi Yuan   +7 more
doaj   +1 more source

Endogenous Cannabinoid Receptors Modulate Plasticity at Immature Synapses

open access: yesJournal of Integrative Neuroscience, 2022
Background: To explore the mechanism of endocannabinoid cannabinoid receptor 1 (CB1) receptor pathway that regulates synaptic plasticity in the dorsal horn of the spinal cord of rats with neuropathic pain at different ages. Methods: Neonatal, juvenile, and adult male sprague dawley (SD) rats were divided into the spinal nerve preservation injury (SNI),
Jie Cheng   +6 more
openaire   +3 more sources

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