Results 171 to 180 of about 22,623 (220)

Plant fatty acid (ethanol) amide hydrolases

Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids, 2006
Fatty acid amide hydrolase (FAAH) plays a central role in modulating endogenous N-acylethanolamine (NAE) levels in vertebrates, and, in part, constitutes an "endocannabinoid" signaling pathway that regulates diverse physiological and behavioral processes in animals.
Rhidaya, Shrestha, Sang-chul, Kim, John M, Dyer, Richard A, Dixon, Kent D, Chapman   +4 more
openaire   +2 more sources

Novel inhibitors of fatty acid amide hydrolase

Bioorganic & Medicinal Chemistry Letters, 2007
A class of bisarylimidazole derivatives are identified as potent inhibitors of the enzyme fatty acid amide hydrolase (FAAH). Compound 17 (IC(50)=2 nM) dose-dependently (0.1-10mg/kg, iv) potentiates the effects of exogenous anandamide (1 mg/kg, iv) in a rat thermal escape test (Hargreaves test), and shows robust antinociceptive activity in animal models
S Y, Sit, Charlie, Conway, Robert, Bertekap, Kai, Xie, Clotilde, Bourin, Kevin, Burris, Hongfeng, Deng   +6 more
openaire   +2 more sources

Fatty Acid Amide Hydrolase: From Characterization to Therapeutics

Chemistry & Biodiversity, 2007
AbstractFatty acid amide hydrolase (FAAH) is an integral membrane enzyme within the amidase‐signature family that terminates the action of several endogenous lipid messengers, including oleamide and the endocannabinoid anandamide. The hydrolysis of such messengers leads to molecules devoid of biological activity, and, therefore, modulates a number of ...
Labar, Geoffray, Michaux, Catherine
openaire   +3 more sources

Fatty Acid Amide Hydrolase Inhibitors – Progress and Potential

CNS & Neurological Disorders - Drug Targets, 2011
Fatty acid amide hydrolase (FAAH) is responsible for hydrolysis of endocannabinoid, anandamide (AEA), and N-acyl ethanolamines such as palmitoylethanolamine (PEA) and N-oleoylethanolamide (OEA). Genetic deletion or pharmacological inactivation of FAAH shows site-specific elevation of AEA that plays a role in the modulation of pain and other ...
Khanna, Ish K., Alexander, Christopher W.   +1 more
openaire   +3 more sources

STRUCTURE AND FUNCTION OF FATTY ACID AMIDE HYDROLASE

Annual Review of Biochemistry, 2005
▪ Abstract  Fatty acid amide hydrolase (FAAH) is a mammalian integral membrane enzyme that degrades the fatty acid amide family of endogenous signaling lipids, which includes the endogenous cannabinoid anandamide and the sleep-inducing substance oleamide.
Michele K, McKinney, Benjamin F, Cravatt
openaire   +2 more sources

Novel propanamides as fatty acid amide hydrolase inhibitors

European Journal of Medicinal Chemistry, 2017
Fatty acid amide hydrolase (FAAH) has a key role in the control of the cannabinoid signaling, through the hydrolysis of the endocannabinoids anandamide and in some tissues 2-arachidonoylglycerol. FAAH inhibition represents a promising strategy to activate the cannabinoid system, since it does not result in the psychotropic and peripheral side effects ...
Alessandro Deplano, Carmine Marco Morgillo, Monica Demurtas, Emmelie Björklund, Mariateresa Cipriano, Mona Svensson, Sanaz Hashemian, Giovanni Smaldone, Emilia Pedone, F. Javier Luque, Maria G. Cabiddu, Ettore Novellino, Christopher J. Fowler, Bruno Catalanotti, Valentina Onnis   +14 more
openaire   +5 more sources

Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase

Bioorganic & Medicinal Chemistry Letters, 2008
A series of thiadiazolopiperazinyl aryl urea fatty acid amide hydrolase (FAAH) inhibitors is described. The molecules were found to inhibit the enzyme by acting as mechanism-based substrates, forming a covalent bond with Ser241. SAR and PK properties are presented.
John M, Keith, Richard, Apodaca, Wei, Xiao, Mark, Seierstad, Kanaka, Pattabiraman, Jiejun, Wu, Michael, Webb, Mark J, Karbarz, Sean, Brown, Sandy, Wilson, Brian, Scott, Chui-Se, Tham, Lin, Luo, James, Palmer, Michelle, Wennerholm, Sandra, Chaplan, J Guy, Breitenbucher   +16 more
openaire   +2 more sources

Fatty acid amide hydrolase, anandamide, and neurological diseases

2023
The endocannabinoid anandamide (N-arachidonoylethanolamine, AEA) is a bioactive lipid that has been shown to regulate a number of important pathophysiological conditions in humans, including several neurological disorders. AEA acts on cannabinoid receptors, and many studies reported that it may also interact with other targets, such as vanilloid and ...
F. Fezza, E. Criscuolo, M. L. De Sciscio, M. Maccarrone   +3 more
openaire   +1 more source

Fatty Acid Amide Hydrolase Inhibition by Neurotoxic Organophosphorus Pesticides

Toxicology and Applied Pharmacology, 2001
Organophosphorus (OP) compound-induced inhibition of acetylcholinesterase (AChE) and neuropathy target esterase explains the rapid onset and delayed neurotoxic effects, respectively, for OP insecticides and related compounds but apparently not a third or intermediate syndrome with delayed onset and reduced limb mobility.
G B, Quistad, S E, Sparks, J E, Casida
openaire   +2 more sources

Inhibitor of Fatty Acid Amide Hydrolase — Learning from Tragic Failures

New England Journal of Medicine, 2017
A large number of drugs can induce prolongation of cardiac repolarization and life-threatening cardiac arrhythmias. The prediction of this side effect is however challenging as it usually develops in some genetically predisposed individuals with normal cardiac repolarization at baseline. Here, we describe a platform based on a genetically diverse panel
Michael, Schapira, Bénédicte, De Vroey, Jean-Michel, Ghilain   +2 more
openaire   +7 more sources