Fatty acid amide hydrolase (FAAH) inhibition enhances memory acquisition through activation of PPAR- nuclear receptors
نویسندگان
چکیده
منابع مشابه
The 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...
متن کاملDiscovery and molecular basis of potent noncovalent inhibitors of fatty acid amide hydrolase (FAAH).
Fatty acid amide hydrolase (FAAH), an amidase-signature family member, is an integral membrane enzyme that degrades lipid amides including the endogenous cannabinoid anandamide and the sleep-inducing molecule oleamide. Both genetic knock out and pharmacological administration of FAAH inhibitors in rodent models result in analgesic, anxiolytic, and antiinflammatory phenotypes. Targeting FAAH act...
متن کاملN-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors.
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-...
متن کاملEx-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...
متن کاملFatty Acid Amide Hydrolase (FAAH) Inhibitors: Discovery in Lepidium meyenii (Maca) Extracts
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...
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ژورنال
عنوان ژورنال: Learning & Memory
سال: 2009
ISSN: 1072-0502
DOI: 10.1101/lm.1145209