Results 31 to 40 of about 1,309,192 (242)

Differential β-arrestin2 requirements for constitutive and agonist-induced internalization of the CB1 cannabinoid receptor [PDF]

, 2013
CB1 cannabinoid receptor (CB1R) undergoes both constitutive and agonist-induced internalization, but the underlying mechanisms of these processes and the role of beta-arrestins in the regulation of CB1R function are not completely understood.
Boros, Eszter, Hunyady, L., Gyombolai, Pál, Boros, E., Turu, G., Turu, Gábor, Gyombolai, P., Hunyady, László   +7 more
core   +1 more source

Pharmacological Evaluation of Cannabinoid Receptor Modulators Using GRAB_eCB2.0 Sensor. [PDF]

Int 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.
Shivshankar S, Nimely J, Puhl H, Iyer MR.   +3 more
europepmc   +2 more sources

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, Rabia U. Malik, Tejas Gupte, Sivaraj Sivaramakrishnan   +3 more
doaj   +1 more source

The cannabinoid 1 receptor (CNR1) 1359 G/A polymorphism modulates susceptibility to ulcerative colitis and the phenotype in Crohn's disease. [PDF]

, 2010
Recent evidence suggests a crucial role of the endocannabinoid system, including the cannabinoid 1 receptor (CNR1), in intestinal inflammation. We therefore investigated the influence of the CNR1 1359 G/A (p.Thr453Thr; rs1049353) single nucleotide ...
Brand, Stephan, Burkhard Göke, Göke, Burkhard, Storr, Martin, Göke Burkhard, Ochsenkühn, Thomas, Stephan Brand, Brand Stephan, Thomas Ochsenkühn, Storr Martin, Pfennig, Simone, Dominik Emmerdinger, Peter Lohse, Martin Storr, Emmerdinger Dominik, Diegelmann, Julia, Lohse, Peter, Simone Pfennig, Diegelmann Julia, Emmerdinger, Dominik, Julia Diegelmann, Ochsenkühn Thomas, Lohse Peter, Pfennig Simone   +23 more
core   +1 more source

The Peripheral Cannabinoid Receptor Type 1 (CB₁) as a Molecular Target for Modulating Body Weight in Man

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, Andrew S. Yates, Richard K. Porter   +2 more
doaj   +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, Yifei Wu, Zhuangzhuang Tian, Yuanfan Xu, Chaoran Wu, Zilong Wang   +5 more
openaire   +2 more sources

Targeting cannabinoid CB2 receptors in the Central Nervous System. Medicinal chemistry approaches with focus on neurodegenerative disorders

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, Paula Morales, Carmen Rodríguez-Cueto, Javier Fernández-Ruiz, Nadine Jagerovic, Rafael Franco   +5 more
doaj   +1 more source

Ethnomedicine-based discovery and characterization of plant-derived GABAΑ receptor modulators with new scaffolds [PDF]

, 2014
Inhibitory neurotransmission in the central nervous system (CNS) largely relies on the actions of gamma aminobutyric acid (GABA) on GABAA receptors, heteropentameric ligand-gated chloride channels assembled from 19 possible subunits (α1-6, β1-3, γ1-3, δ,
Rueda, Diana Carolina
core   +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, Alexander A. Ilyasov, Carolanne E. Milligan, Carolanne E. Milligan, Emily P. Pharr, Emily P. Pharr, Allyn C. Howlett, Allyn C. Howlett   +7 more
doaj   +1 more source

R-flurbiprofen reduces neuropathic pain in rodents by restoring endogenous cannabinoids [PDF]

, 2010
Background: R-flurbiprofen, one of the enantiomers of flurbiprofen racemate, is inactive with respect to cyclooxygenase inhibition, but shows analgesic properties without relevant toxicity. Its mode of action is still unclear.
Geisslinger, Gerd, Gerd Geisslinger, Ziebell Simone, Julia Metzner, Ziebell, Simone, Koch, Marco, Myrczek, Thekla, Marian, Claudiu, Dehghani, Faramarz, Rohini Kuner, Schmidt Helmut, Bechmann Ingo, Marian Claudiu, Nina Wijnvoord, Dehghani Faramarz, Philipp Bishay, Bishay, Philipp, Kuner, Rohini, Helmut Schmidt, Faramarz Dehghani, Koch Marco, Bechmann, Ingo, Metzner, Julia, Geisslinger Gerd, Irmgard Tegeder, Tegeder Irmgard, Simone Ziebell, Wijnvoord, Nina, Tegeder, Irmgard, Claudiu Marian, Kuner Rohini, Costigan, Michael, Wijnvoord Nina, Annett Häussler, Ingo Bechmann, Michael Costigan, Schmidt, Helmut, Häussler, Annett, Bechmann, Ingo Jürgen, Myrczek Thekla, Bishay Philipp, Häussler Annett, Marco Koch, Costigan Michael, Thekla Myrczek, Metzner Julia   +45 more
core   +1 more source