Results 171 to 180 of about 8,951 (213)

Targeting Endocannabinoid Signaling: FAAH and MAG Lipase Inhibitors

Annual Review of Pharmacology and Toxicology, 2021
Inspired by the medicinal properties of the plant Cannabis sativa and its principal component (−)- trans-Δ9-tetrahydrocannabinol (THC), researchers have developed a variety of compounds to modulate the endocannabinoid system in the human brain. Inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL), which are the enzymes ...
Mario Van Der Stelt
exaly   +5 more sources

Chiral 3-(4,5-dihydrooxazol-2-yl)phenyl alkylcarbamates as novel FAAH inhibitors: Insight into FAAH enantioselectivity by molecular docking and interaction fields

European Journal of Medicinal Chemistry, 2009
Fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) are the main enzymes responsible for the hydrolysis of endogenous cannabinoids N-arachidonoylethanolamide (AEA) and 2-arachidonoylglycerol (2-AG), respectively.
Susanna M Saario, Antti Poso, Ari M P Koskinen   +2 more
exaly   +2 more sources

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Assay of FAAH Activity

2016
Fatty acid amide hydrolase (FAAH) is an intracellular enzyme responsible for the hydrolysis of endogenous anandamide (AEA), a reaction that terminates the biological effects of this lipid mediator. The final products of this reaction are arachidonic acid and ethanolamine.
Bari M, Feole M, Maccarrone M
openaire   +3 more sources

Enhanced microglial activity in FAAH−/− animals

Life Sciences, 2015
Several lines of evidence suggest that the endocannabinoid system is involved in the regulation of glial activity. Enhanced levels of the endocannabinoid N-arachidonoyl ethanolamine (AEA, also referred to as anandamide) as well as non-cannabinoid lipids like palmitoylethanolamine (PEA) due to genetic deletion or pharmacologic blockade of its degrading ...
F, Ativie, O, Albayram, K, Bach, B, Pradier, A, Zimmer, A, Bilkei-Gorzo   +5 more
openaire   +2 more sources

The fatty acid amide hydrolase (FAAH)

Chemistry and Physics of Lipids, 2000
The topic of this review is fatty acid amide hydrolase (FAAH), one of the best-characterized enzymes involved in the hydrolysis of bioactive lipids such as anandamide, 2-arachidonoylglycerol (2-AG), and oleamide. Herein, we discuss the nomenclature, the various assays that have been developed, the relative activity of the various substrates and the ...
N, Ueda, R A, Puffenbarger, S, Yamamoto, D G, Deutsch   +3 more
openaire   +2 more sources

The fatty acid amide hydrolase (FAAH)

Prostaglandins, Leukotrienes and Essential Fatty Acids (PLEFA), 2002
The fatty acid amide hydrolase (FAAH), is the enzyme responsible for the hydrolysis of anandamide, an endocannabinoid. The FAAH knockout, the assays for FAAH, the activity of its substrates, its reversibility and its cloning from rat, mouse, human, and pig are covered in this review.
D G, Deutsch, N, Ueda, S, Yamamoto
openaire   +2 more sources

Systemic and spinal administration of FAAH, MAGL inhibitors and dual FAAH/MAGL inhibitors produce antipruritic effect in mice

Archives of Dermatological Research, 2016
The increase of endocannabinoid tonus by inhibiting fatty acid amide hydrolase (FAAH) or monoacylglycerol lipase (MAGL) represents a promising therapeutic approach in a variety of disease to overcome serious central side effects of exocannabinoids. Recent studies reported that systemic administration of FAAH and MAGL inhibitors produce antipruritic ...
Ozgur, Yesilyurt, Mutlu, Cayirli, Yusuf Serdar, Sakin, Melik, Seyrek, Ahmet, Akar, Ahmet, Dogrul   +5 more
openaire   +2 more sources

Supra-spinal FAAH is required for the analgesic action of paracetamol in an inflammatory context

Neuropharmacology, 2015
International audienceParacetamol (acetaminophen) is the most commonly used analgesic in the world. Recently, a new view of its action has emerged: that paracetamol would be a pro-drug that should be metabolized by the FAAH enzyme into AM404, its active ...
Laurence Daulhac, Myriam Antri, Alain Eschalier   +2 more
exaly   +2 more sources

Molecular Dynamics Analysis of FAAH Complexed with Anandamide

2015
Fatty Acid Amide Hydrolase (FAAH) is a very interesting serine hydrolase that promotes the hydrolysis of both amides and esters, such as the endogenous cannabinoid anandamide or N-arachidonoyl ethanolamine (AEA), and the sleep-inducing lipid oleamide.
Sérgio F. Sousa, João T. S. Coimbra, MARINO, Tiziana, Pedro A. Fernandes, Maria J. Ramos, RUSSO, Nino   +5 more
openaire   +2 more sources

Macamides and their synthetic analogs: Evaluation of in vitro FAAH inhibition

Bioorganic and Medicinal Chemistry, 2013
Maca (Lepidium meyenii), a traditional food crop of the Peruvian Andes is now widely touted as a dietary supplement. Among the various chemical constituents isolated from the plant are a unique series of non-polar, long-chain fatty acid N-benzylamides known as macamides.
Alejandro Pino-Figueroa, Timothy J Maher   +1 more
exaly   +3 more sources