Development of Potent Inhibitors of Fatty Acid Amide Hydrolase Useful for the Treatment of Neuropathic Pain
نویسندگان
چکیده
منابع مشابه
Inhibition of fatty acid amide hydrolase: a potential treatment for neuropathic pain.
(CAA)-affected vessel in the Tg2576 mouse model of amyloid deposition. Representative example of CAA in a vessel segment of a living Tg2576 mouse imaged with multiphoton microscopy. Vascular and parenchymal A deposits are identified by fluorescence from systemically administered methoxy-XO4 (red pseudocolor). Fluorescent angiograms with Texas Red dextran were performed to identify fiduciary mar...
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The level of the endocannabinoid anandamide is controlled by fatty acid amide hydrolase (FAAH). In 2011, PF-04457845, an irreversible inhibitor of FAAH, was progressed to phase II clinical trials for osteoarthritic pain. This article discusses a prospective, integrated systems pharmacology model evaluation of FAAH as a target for pain in humans, using physiologically based pharmacokinetic and s...
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Cannabinoid-based medicines have therapeutic potential for the treatment of pain. Augmentation of levels of endocannabinoids with inhibitors of fatty acid amide hydrolase (FAAH) is analgesic in models of acute and inflammatory pain states. The aim of this study was to determine whether local inhibition of FAAH alters nociceptive responses of spinal neurons in the spinal nerve ligation model of ...
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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...
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Fatty Acid Amide Hydrolase (FAAH) is an intracellular serine enzyme involved in the biological degradation of the fatty acid ethanolamide family of signaling lipids, which exerts neuroprotective, anti-inflammatory, and analgesic properties. In the present study, a conjugated 2,4-dioxo-pyrimidine-1-carboxamide scaffold was confirmed as a novel template for FAAH inhibitors, based on which, a seri...
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ژورنال
عنوان ژورنال: ChemMedChem
سال: 2018
ISSN: 1860-7179
DOI: 10.1002/cmdc.201800397