Results 21 to 30 of about 247,667 (242)
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
doaj +1 more source
Allosteric modulation of adenosine A1 and cannabinoid 1 receptor signaling by G‐peptides
Pharmacology Research & Perspectives, 2020 While allosteric modulation of GPCR signaling has gained prominence to address the need for receptor specificity, efforts have mainly focused on allosteric sites adjacent to the orthosteric ligand‐binding pocket and lipophilic molecules that target ...
Anja M. Touma +3 more
doaj +1 more source
Biochemical and Biophysical Research Communications - BBRC, 2013 The purpose of the current study was to investigate the ability of the third-generation selective estrogen receptor modulators (SERMs) bazedoxifene and lasofoxifene to bind and act on CB2 cannabinoid receptor. We have identified, for the first time, that
Pritesh Kumar, Z. Song
semanticscholar +1 more source
Allosteric modulators of cannabinoid receptor 1: developing compounds for improved specificity
Drug metabolism reviews (Softcover ed.), 2018 The cannabinoid receptor 1 (CB1) is a G protein-coupled receptor (GPCR) that is located primarily in the central nervous system. CB1 is a therapeutic target which may impact pathways to mediate pain, neurodegenerative disorders, hunger, and drug-seeking ...
Rachel Dopart +3 more
semanticscholar +1 more source
Molecules, 2021 The cannabinoid 1 (CB1) receptor regulates appetite and body weight; however, unwanted central side effects of both agonists (in wasting disorders) or antagonists (in obesity and diabetes) have limited their therapeutic utility.
Saoirse Elizabeth O’Sullivan +2 more
doaj +1 more source
Neuron, 2016 Summary Muscarinic receptors represent a promising therapeutic target for schizophrenia, but the mechanisms underlying the antipsychotic efficacy of muscarinic modulators are not well understood. Here we report that activation of M4 receptors on striatal
Daniel J Foster +13 more
semanticscholar +1 more source
Microglial Cannabinoid CB2 Receptors in Pain Modulation
International 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
Allosteric Modulators of the CB1 Cannabinoid Receptor: A Structural Update Review
Cannabis and Cannabinoid Research, 2016 In 2005, the first evidence of an allosteric binding site at the CB1R was provided by the identification of three indoles of the company Organon that were allosteric enhancers of agonist binding affinity and, functionally, allosteric inhibitors of ...
P. Morales +3 more
semanticscholar +1 more source
Frontiers in Neuroscience, 2016 Endocannabinoids activate two types of specific receptors, namely cannabinoid CB1 and CB2. Contrary to the psychotropic actions of agonists of CB1 receptors, and serious side effects of the selective antagonists of this receptor, drugs acting on CB2 ...
Gema Navarro +5 more
doaj +1 more source
The Endocannabinoid System and Oligodendrocytes in Health and Disease
Frontiers in Neuroscience, 2018 Cannabinoid-based interventions are being explored for central nervous system (CNS) pathologies such as neurodegeneration, demyelination, epilepsy, stroke, and trauma. As these disease states involve dysregulation of myelin integrity and/or remyelination,
Alexander A. Ilyasov +7 more
doaj +1 more source