Endocannabinoids at physiological concentrations are crossing cellular membranes by facilitated diffusion, a process that can be studied by measuring transport kinetics. Here, we describe a radiosubstrate-based assay using arachidonoyl[1-(3)H]ethanolamine or arachidonoyl[1,2,3-(3)H]glycerol to measure the cellular endocannabinoid uptake in a three-phase assay with human U937 cells.
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http://dx.doi.org/10.1007/978-1-4939-3539-0_20 | DOI Listing |
Eur J Med Chem
January 2025
Department of Radiology and Imaging Sciences, Emory University, 1364 Clifton Road, Atlanta, GA, 30322, United States. Electronic address:
Monoacylglycerol lipase (MAGL) is a 33 kDa cytosolic serine hydrolase that is widely distributed in the central nervous system and peripheral tissues. MAGL hydrolyzes monoacylglycerols into fatty acids and glycerol, playing a crucial role in endocannabinoid degradation. Inhibition of MAGL in the brain elevates levels of 2-arachidonoylglycerol and leads to decreased pro-inflammatory prostaglandin and thromboxane production.
View Article and Find Full Text PDFCurr Top Behav Neurosci
January 2025
Pharma Research and Early Development (pRED), Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd, Basel, Switzerland.
Cannabis sativa has been used therapeutically since early civilizations, with key cannabinoids Δ-tetrahydrocannabinol (THC) 3.1 and cannabidiol characterized in the 1960s, leading to the discovery of cannabinoid receptors type 1 (CBR) and type 2 (CBR) and the endocannabinoid system (ECS) in the 1990s. The ECS, involving endogenous ligands like 2-arachidonoylglycerol (2-AG) 1.
View Article and Find Full Text PDFRev Cardiovasc Med
December 2024
Liver Unit, University of Calgary Cumming School of Medicine, Calgary, AB T2N 4N1, Canada.
Sci Rep
December 2024
Department of Veterinary Clinical Sciences, College of Veterinary Medicine, Purdue University, West Lafayette, IN, 47907, USA.
Unregulated, systemic inflammation negatively impacts health and production in dairy cows. Soluble mediators and platelets have been studied for their expansive role in mediating inflammation. Our objectives were to compare the plasma oxylipin and endocannabinoid profiles, and the platelet and plasma proteomic profiles of healthy cows to cows experiencing elevated systemic inflammation as indicated by plasma haptoglobin (Hp) concentrations.
View Article and Find Full Text PDFEur J Nucl Med Mol Imaging
December 2024
Center for Radiopharmaceutical Sciences, Institute of Pharmaceutical Sciences, Department of Chemistry and Applied Biosciences, ETH Zurich, Zurich, CH-8093, Switzerland.
Purpose: The monoacylglycerol lipase (MAGL) plays a pivotal role in modulating the endocannabinoid system and is considered an attractive therapeutic target for diseases in both the central nervous system and periphery. The current study aimed to develop and evaluate a suitable carbon-11 labeled tracer for imaging MAGL in preclinical studies.
Methods: (R)-YH168 was synthesized via a multi-step pathway and its half-maximal inhibitory concentration (IC) values were measured using an enzymatic assay.
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