Results 171 to 180 of about 13,969 (210)

Radiometric Assay of FAAH Activity

2022
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 AEA cleavage are arachidonic acid and ethanolamine.
Bari, Monica, Feole, Monica, Fava, Marina, Maccarrone, Mauro   +3 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

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)

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

Preclinical Characterization of the FAAH Inhibitor JNJ-42165279 [PDF]

ACS Medicinal Chemistry Letters, 2015
The pre-clinical characterization of the aryl piperazinyl urea inhibitor of fatty acid amide hydrolase (FAAH) JNJ-42165279 is described. JNJ-42165279 covalently inactivates the FAAH enzyme, but is highly selective with regard to other enzymes, ion channels, transporters, and receptors.
Mark S Tichenor, Lin Luo
exaly   +3 more sources

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

Finding fault with Bial's fatal FAAH inhibitor [PDF]

Nature Reviews Drug Discovery, 2017
exaly   +2 more sources

Structure based design of novel irreversible FAAH inhibitors

Bioorganic & Medicinal Chemistry Letters, 2009
Fatty acid amide hydrolase (FAAH) has attracted significant attention due to its promise as an analgesic target. This has resulted in the discovery of numerous chemical classes as inhibitors of this potential therapeutic target. In this paper we disclose a new series of novel FAAH irreversible azetidine urea inhibitors.
Jane L, Wang, Scott J, Bowen, Barbara A, Schweitzer, Heather M, Madsen, Joseph, McDonald, Matthew J, Pelc, Ruth E, Tenbrink, David, Beidler, Atli, Thorarensen   +8 more
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

Arylboronic acids as dual-action FAAH and TRPV1 ligands

Bioorganic & Medicinal Chemistry Letters, 2016
A series of 31 arylboronic acids designed on the basis of the pharmacophore model for a variety of TRPV1 antagonists was prepared and tested on FAAH and TRPV1 channel. Four of them, that is, compounds 3c, 4a, 5a,b acted as dual FAAH/TRPV1 blockers with IC50 values between 0.56 and 8.11μM whereas ten others (compounds 1c,f-i, 2c-f, 4b) inhibited FAAH ...
MORERA, ENRICO, Di Marzo, Vincenzo, MONTI, LUDOVICA, Allarà, Marco, Schiano Moriello, Aniello, NALLI, Marianna, ORTAR, Giorgio, De Petrocellis, Luciano   +7 more
openaire   +2 more sources