Results 31 to 40 of about 10,682 (172)
Differentiation of CB1 cannabinoid agonists in rats
The FASEB Journal, 2009 Results from GTPγS binding and other in vitro assays suggest that cannabinoid (CB) receptor agonists range in efficacy from partial to full agonists. The present studies compared the in vivo effects of
Carol Anne Paronis +7 more
openaire +1 more source
Allosteric modulators restore orthosteric agonist binding to mutated CB1 receptors
Journal of Pharmacy and Pharmacology, 2020 Abstract Objectives To determine if diminished orthosteric agonist binding due to mutations in extracellular loops 1 or 2 of the cannabinoid receptor 1 (CB1) can be overcome by an allosteric modulator and restore agonist binding. Methods
Rachel Dopart, Debra A Kendall
openaire +3 more sources
Two Janus Cannabinoids That Are Both CB2 Agonists and CB1 Antagonists [PDF]
The Journal of Pharmacology and Experimental Therapeutics, 2017 The cannabinoid signaling system includes two G protein-coupled receptors, CB1 and CB2 These receptors are widely distributed throughout the body and have each been implicated in many physiologically important processes. Although the cannabinoid signaling system has therapeutic potential, the development of receptor-selective ligands remains a ...
Amey, Dhopeshwarkar +4 more
openaire +2 more sources
Frontiers in Behavioral Neuroscience, 2020 Cannabinoid (CB) receptor agonists are of growing interest as targets for anti-seizure therapies. Here we examined the effect of systemic administration of the CB receptor agonist WIN 55,212-2 (WIN) against audiogenic seizures (AGSs) in the Genetically ...
Victor R. Santos +10 more
doaj +1 more source
Pharmacology Research & Perspectives, 2022 Neutral antagonists of GPCRs remain relatively rare—indeed, a large majority of GPCR antagonists are actually inverse agonists. The synthetic cannabinoid receptor agonist (SCRA) EG‐018 was recently reported as a low efficacy cannabinoid receptor agonist.
David B. Finlay +9 more
doaj +1 more source
The Cannabinoid Receptor CB1 Interacts with the WAVE1 Complex and Plays a Role in Actin Dynamics and Structural Plasticity in Neurons. [PDF]
PLoS Biology, 2015 The molecular composition of the cannabinoid type 1 (CB1) receptor complex beyond the classical G-protein signaling components is not known. Using proteomics on mouse cortex in vivo, we pulled down proteins interacting with CB1 in neurons and show that ...
Christian Njoo +3 more
doaj +1 more source
Voltage dependence of the cannabinoid CB1 receptor
Frontiers in Pharmacology, 2022 Cannabinoids produce their characteristic effects mainly by binding to two types of G-protein coupled receptors (GPCRs), the CB1 and CB2 cannabinoid receptors.
Esty Goldberger +2 more
doaj +1 more source
Cell Death and Disease, 2023 Statins are the most prescribed lipid-lowering agents worldwide. Their use is generally safe, although muscular toxicity occurs in about 1 in 10.000 patients.
Hilal Kalkan +9 more
doaj +1 more source
Behavioral effects of the novel potent cannabinoid CB1 agonist AM 4054 [PDF]
Pharmacology Biochemistry and Behavior, 2013 Due to the ubiquity of the CB1 cannabinoid receptor throughout the nervous system, as well as the many potential therapeutic uses of CB1 agonist-based interventions, it is desirable to synthesize novel probes of the CB1 receptor. Here, the acute behavioral effects of systemic (i.p.) administration of the putative novel CB1 full agonist AM 4054 were ...
Peter J, McLaughlin +8 more
openaire +2 more sources
Exploring the Ligand Efficacy of Cannabinoid Receptor 1 (CB1) using Molecular Dynamics Simulations
Scientific Reports, 2018 Cannabinoid receptor 1 (CB1) is a promising therapeutic target for a variety of disorders. Distinct efficacy profiles showed different therapeutic effects on CB1 dependent on three classes of ligands: agonists, antagonists, and inverse agonists.
Sang Won Jung, Art E. Cho, Wookyung Yu
doaj +1 more source