The in vivo administration of ethinylestradiol to female rats causes dose-dependent decreases in tri-, di- and monoacylglycerol lipase activities in post-heparin heart effluents; monoacylglycerol lipase is less sensitive to estrogen than the other two.
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Highly Specific Miniaturized Fluorescent Monoacylglycerol Lipase Probes Enable Translational Research.
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Leibniz Forschungsinstitut für Molekulare Pharmakologie, Campus Berlin-Buch, 13125 Berlin, Germany.
Monoacylglycerol lipase (MAGL) is the pivotal catabolic enzyme responsible for signal termination in the endocannabinoid system. Inhibition of MAGL offers unique advantages over the direct activation of cannabinoid receptors in treating cancer, metabolic disorders, and inflammatory diseases. Although specific fluorescent molecular imaging probes are commonly used for the real-time analysis of the localization and distribution of drug targets in cells, they are almost invariably composed of a linker connecting the pharmacophore with a large fluorophore.
View Article and Find Full Text PDFRole of endocannabinoid neurotransmission in the insular cortex on cardiovascular, autonomic and behavioral responses evoked by acute restraint stress in rats.
Neuropharmacology
March 2025
Institute of Science, Technology and Innovation- Federal University of Lavras, Antônio Carlos Pinheiro de Alcântara, 855 - Jardim Califórnia Garden, São Sebastião Do Paraíso, Minas Gerais, Brazil. Electronic address:
This study aimed to investigate the role of endocannabinoid mechanisms present within the insular cortex (IC) on cardiovascular, autonomic and anxiogenic-like responses evoked by an acute session of restraint in rats. For this, bilateral guide cannulas directed to the IC were implanted in male Wistar rats for intrabrain microinjection of the selective CB receptor antagonist AM251, the selective TRPV1 receptor antagonist capsazepine, the fatty acid amide hydrolase (FAAH) inhibitor URB597 or the monoacylglycerol lipase (MAGL) inhibitor JZL184. The effects of pharmacological treatments were evaluated on restraint-evoked increases in blood pressure and heart rate, sympathetically-mediated cutaneous vasoconstriction and in delayed anxiogenic-like effect assessed 24h after stress exposure in the elevated plus maze (EPM) and open field (OF).
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Department of Pharmacology and Pharmacodynamics, Medical University of Lublin, 4a Chodzki Str., 20-093 Lublin, Poland.
Background: The endocannabinoid system (ECS) is one of the most important systems modulating functions in the body. The ECS, via cannabinoid (CB: CB1 and CB2) receptors, endocannabinoids occurring in the brain (e.g.
View Article and Find Full Text PDFGenome-wide analysis reveals the evolutionary history of TAG intracellular lipases and their roles in different molting stages of Decapods.
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Centre for Research on Environmental Ecology and Fish Nutrition of the Ministry of Agriculture and Rural Affairs, Shanghai Ocean University, Shanghai 201306, China; Key Laboratory of Freshwater Aquatic Genetic Resources Certified by the Ministry of Agriculture and Rural Affairs of China, Shanghai Ocean University, Shanghai 201306, China; Shanghai Collaborative Innovation Center for Cultivating Elite Breeds and Green-culture of Aquaculture animals, Shanghai 201306, China. Electronic address:
Intracellular lipases can be broadly divided into two categories: neutral lipases and acid lipases. Adipose triglyceride lipase (ATGL), hormone-sensitive lipase (HSL), and monoacylglycerol lipase (MAGL) are three key neutral lipases responsible for the hydrolysis of triacylglycerol (TAG) in lipid droplets (LDs). Although these three TAG intracellular lipase genes have been identified and characterized in multiple model species, their evolutionary history remains largely unknown.
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bioRxiv
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School of Neuroscience, Virginia Polytechnic and State University, 970 Washington Street SW, Blacksburg, VA 24061.
Alcohol use disorder (AUD) affects millions of people and represents a significant health and economic burden. Pain represents a frequently under-treated aspect of hyperkatifeia during alcohol withdrawal, yet to date no drugs have received FDA approval for the treatment of this indication in AUD patients. This study aims to evaluate the potential of targeting bioactive lipid signaling pathways as a therapeutic approach for treating alcohol withdrawal-related pain.
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