Results 71 to 80 of about 43,721 (231)

Neuronal and ion channel mechanisms of noxious heat sensing in mammals: A puzzle of sensory physiology and pharmacology

British Journal of Pharmacology, EarlyView.
Transient receptor potential vanilloid 1 (TRPV1) was the first noxious heat‐sensitive channel discovered. In rodents, its role is robust in the heat response of the cell body of polymodal nociceptors, but surprisingly small in that of the peripheral terminals in the skin.
Gábor Pethő, Peter W. Reeh
wiley   +1 more source

The F238L Point Mutation in the Cannabinoid Type 1 Receptor Enhances Basal Endocytosis via Lipid Rafts

Frontiers in Molecular Neuroscience, 2018
Defining functional domains and amino acid residues in G protein coupled receptors (GPCRs) represent an important way to improve rational drug design for this major class of drug targets.
Melanie Wickert, Keri L. Hildick, Gemma L. Baillie, Ruth Jelinek, Alejandro Aparisi Rey, Krisztina Monory, Miriam Schneider, Miriam Schneider, Ruth A. Ross, Jeremy M. Henley, Beat Lutz, Beat Lutz   +11 more
doaj   +1 more source

Distinct Roles of β-Arrestin 1 and β-Arrestin 2 in ORG27569-induced Biased Signaling and Internalization of the Cannabinoid Receptor 1 (CB1)*

Journal of Biological Chemistry, 2013
Background: CB1 is activated by agonist CP55940 in a G protein-dependent manner. Results: β-Arrestin 2 plays a role in CB1 internalization, whereas β-arrestin 1 is critical for ORG27569-induced ERK1/2, MEK1/2, and c-Src phosphorylation.
K. Ahn, M. Mahmoud, J. Shim, D. Kendall
semanticscholar   +1 more source

Peripheral targets for neuropathic pain

British Journal of Pharmacology, EarlyView.
Neuropathic pain represents a significant clinical challenge, with still limited pharmacological approaches to symptomatic relief. This review focuses on molecular targets implicated in neuropathic pain, particularly those involved in peripheral mechanisms. Using the IUPHAR/BPS database of biological targets, their occurrence together with ‘neuropathic
Amirhossein Afsharipour, Cosmin I. Ciotu, Felix J. Resch, Michael J. M. Fischer   +3 more
wiley   +1 more source

Structure of a Signaling Cannabinoid Receptor 1-G Protein Complex

Cell, 2019
Summary Cannabis elicits its mood-enhancing and analgesic effects through the cannabinoid receptor 1 (CB1), a G protein coupled receptor (GPCR) that signals primarily through the adenylyl cyclase-inhibiting heterotrimeric G protein Gi.
K. K. Kumar, M. Shalev-Benami, M. Robertson, Hongli Hu, S. Banister, S. Hollingsworth, Naomi R. Latorraca, Hideaki E. Kato, D. Hilger, S. Maeda, W. Weis, D. Farrens, R. Dror, S. Malhotra, B. Kobilka, G. Skiniotis   +15 more
semanticscholar   +1 more source

Cannabinoid CB1 allosteric ligands suppress inflammatory pain in male mice without tolerance, motor impairment, memory deficits or respiratory depression

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Positive allosteric modulators (PAMs) engage sites distinct from the orthosteric CB1 cannabinoid receptor binding site. GAT211, a racemic ligand, contains GAT228 (R) and GAT229 (S) enantiomers. Whether enantiomer‐mediated differences in allosteric activation or positive allosteric modulation translate into differences in
Ifeoluwa D. Solomon, Sumanta Garai, Ganesh A. Thakur, Andrea G. Hohmann   +3 more
wiley   +1 more source

Cannabinoids: A New Group of Agonists of PPARs

PPAR Research, 2007
Cannabinoids have been used medicinally and recreationally for thousands of years and their effects were proposed to occur mainly via activation of the G-protein-coupled receptor CB1/CB2 (cannabinoid receptor 1/2).
Yan Sun, Andy Bennett
doaj   +1 more source

Transmembrane Helical Domain of the Cannabinoid CB1 Receptor [PDF]

Biophysical Journal, 2009
Brain cannabinoid (CB(1)) receptors are G-protein coupled receptors and belong to the rhodopsin-like subfamily. A homology model of the inactive state of the CB(1) receptor was constructed using the x-ray structure of beta(2)-adrenergic receptor (beta(2)AR) as the template.
openaire   +2 more sources

Circadian disruption elicits sex‐specific gut microbiota, endocannabinoidome, and lipid mediator responses

The FEBS Journal, EarlyView.
Circadian disruption via constant light induces sex‐specific remodeling of the microbiome, lipid mediators, and immune responses. Females exhibit broader gut microbiota alterations, reduced jejunal oxylipins, increased hypothalamic N‐acylethanolamines, and a more inflammatory cytokine profile. Muscle responses are sex‐ and fiber type‐dependent: females
Pejman A. Pashaki, Timothy D. Niepokny, Tina Khalilzadehsabet, Elizabeth Dumais, Nicolas Flamand, Vincenzo Di Marzo, Eric M. Mintz, Cristoforo Silvestri   +7 more
wiley   +1 more source

Muscarinic cannabinoid suppression of excitation, a novel form of coincidence detection

Pharmacological Research
Δ9-tetrahydrocannabinol (THC), the chief psychoactive ingredient of cannabis, acts in the brain primarily via cannabinoid CB1 receptors. These receptors are implicated in several forms of synaptic plasticity – depolarization-induced suppression of ...
Michaela Dvorakova, Ken Mackie, Alex Straiker   +2 more
doaj   +1 more source