Fatty acid amide hydrolase (FAAH) regulates hypercapnia/ischemia-induced increases in n-acylethanolamines in mouse brain
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چکیده
منابع مشابه
Ex-vivo imaging of fatty acid amide hydrolase (FAAH) activity and its inhibition in the mouse brain
There is recent behavioral evidence that FAAH inhibitors produce a sub-set of cannabinoid receptor agonist effects, suggesting both anandamide-specific behavioral functions, and possible regional differences in FAAH inhibitory effects. Here we introduce a novel imaging method to quantify regional differences in brain FAAH activity. Upon intravenous [H]anandamide administration, brain FAAH activ...
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Fatty acid amide hydrolase (FAAH) is a promising target for the development of drugs to treat neurological diseases. In search of new FAAH inhibitors, we identified 2-(4-cyclohexylphenoxy)-N-(3-(oxazolo[4,5-b]pyridin-2-yl)phenyl)acetamide, 4g, with an IC50 of 2.6 µM as a chemical starting point for the development of potent FAAH inhibitors. Preliminary hit-to-lead optimisation resulted in 2-(4-...
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The pentane extract of the Peruvian plant Lepidium meyenii (Maca) has been shown to possess neuroprotective activity in vitro and in vivo. The involvement of the endocannabinoid system has been shown to be a possible mechanism of action. Some of the lipophilic constituents of Maca such as the macamides have been reported to possess significant pharmacological properties as shown in cell culture...
متن کاملEndocannabinoid metabolism in the absence of fatty acid amide hydrolase (FAAH): discovery of phosphorylcholine derivatives of N-acyl ethanolamines.
Lipid transmitters are tightly regulated by a balance of biosynthetic and degradative enzymes. Termination of the activity of the N-acyl ethanolamine (NAE) class of lipid-signaling molecules, including the endocannabinoid anandamide (AEA), is principally mediated by the integral membrane enzyme fatty acid amide hydrolase (FAAH) in vivo. FAAH(-/-) mice are highly sensitized to the pharmacologica...
متن کاملThe Molecular Basis for Dual Fatty Acid Amide Hydrolase (FAAH)/Cyclooxygenase (COX) Inhibition
The design of multitarget-directed ligands is a promising strategy for discovering innovative drugs. Here, we report a mechanistic study that clarifies key aspects of the dual inhibition of the fatty acid amide hydrolase (FAAH) and the cyclooxygenase (COX) enzymes by a new multitarget-directed ligand named ARN2508 (2-[3-fluoro-4-[3-(hexylcarbamoyloxy)phenyl]phenyl]propanoic acid). This potent d...
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ژورنال
عنوان ژورنال: Journal of Neurochemistry
سال: 2017
ISSN: 0022-3042
DOI: 10.1111/jnc.14067