ω-Heteroarylalkylcarbamates as inhibitors of fatty acid amide hydrolase (FAAH)

MedChemComm ◽  
2014 ◽  
Vol 5 (7) ◽  
pp. 932-936 ◽  
Author(s):  
Tobias Terwege ◽  
Helmut Dahlhaus ◽  
Walburga Hanekamp ◽  
Matthias Lehr
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Inhibitory Potency ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

A series of heteroaryl-substituted alkylcarbamates have been synthesized and evaluated for their inhibitory potency against fatty acid amide hydrolase (FAAH).

scholarly journals (Indolylalkyl)piperidine carbamates as inhibitors of fatty acid amide hydrolase (FAAH)

MedChemComm ◽  
2017 ◽  
Vol 8 (3) ◽  
pp. 616-620 ◽  
Author(s):  
Helmut Dahlhaus ◽  
Walburga Hanekamp ◽  
Matthias Lehr
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Metabolic Stability ◽  
Inhibitory Potency ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

Studies on FAAH inhibitory potency and metabolic stability of indolyl-substituted alkyl- and alkylpiperidine carbamates are described.

Fatty acid amide hydrolase inhibitors display broad selectivity and inhibit multiple carboxylesterases as off-targets

2007 ◽  
Vol 52 (4) ◽  
pp. 1095-1105 ◽  
Author(s):  
Di Zhang ◽  
Anita Saraf ◽  
Teodozyi Kolasa ◽  
Pramila Bhatia ◽  
Guo Zhu Zheng ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

Exacerbation of Background Nuclear Cataracts in Sprague-Dawley Rats in Embryo-Fetal Development Studies With JNJ-42165279, a Fatty Acid Amide Hydrolase Inhibitor

2021 ◽  
pp. 019262332110104
Author(s):  
Marjolein van Heerden ◽  
Wendy Roosen ◽  
Sophie Lachau-Durand ◽  
Graham Bailey ◽  
Anthony Ndifor
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
In Utero ◽  
Histological Evaluation ◽  
High Dose ◽  
Lens Fiber ◽  
Sprague Dawley ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

Fetal examinations in embryo-fetal developmental (EFD) studies are based on macroscopic and dissecting microscopic evaluations, and histopathology is rarely performed other than to confirm macroscopic findings. Fetal lens examination is therefore generally limited to the presence, size, shape, and color of any abnormality. In a Sprague-Dawley rat EFD study with the fatty acid amide hydrolase (FAAH) inhibitor JNJ-42165279, an unusually high incidence of macroscopic granular foci was noted within the lens of gestation day 21 fetuses across all groups including controls, with higher incidence in the high-dose group. On histological evaluation of the lenses from fetuses with/without gross findings, primary lens fiber hypertrophy (swelling) and degeneration were observed across vehicle- and JNJ-42165279-exposed fetuses. In a follow-up study to investigate the progression or resolution of the fetal lens changes, animals exposed to suprapharmacological doses of JNJ-42165279 in utero had higher incidence of nuclear cataracts as detected via slit-lamp ophthalmic examinations on postnatal days 18 to 21 and 35 to 41. No histologic correlates for these cataracts were identified. We conclude that fetal primary lens fiber hypertrophy and nuclear cataracts at ophthalmology, are common background changes in this rat strain that are exacerbated by in utero exposure to the FAAH inhibitor JNJ-42165279.

S203. Fatty Acid Amide Hydrolase Polymorphism C385A Associated With Dopamine D2/3 Receptor Levels: A PET Study With [11C]-(+)-PHNO

2019 ◽  
Vol 85 (10) ◽  
pp. S376
Author(s):  
Esmaeil Mansouri ◽  
Rachel F. Tyndale ◽  
Christian S. Hendershot ◽  
Laura M. Best ◽  
Patricia Di Ciano ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Dopamine D2 ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

scholarly journals Fatty Acid Amide Hydrolase Deficiency Enhances Intraplaque Neutrophil Recruitment in Atherosclerotic Mice

2013 ◽  
Vol 33 (2) ◽  
pp. 215-223 ◽  
Author(s):  
Sébastien Lenglet ◽  
Aurélien Thomas ◽  
Oliver Soehnlein ◽  
Fabrizio Montecucco ◽  
Fabienne Burger ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Neutrophil Recruitment ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

scholarly journals Elevated Brain Fatty Acid Amide Hydrolase Induces Depressive-Like Phenotypes in Rodent Models: A Review

2021 ◽  
Vol 22 (3) ◽  
pp. 1047
Author(s):  
Dorsa Rafiei ◽  
Nathan J. Kolla
Keyword(s):  
Depressive Symptoms ◽  
Fatty Acid ◽  
Animal Models ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Endocannabinoid System ◽  
Animal Models Of Depression ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

Altered activity of fatty acid amide hydrolase (FAAH), an enzyme of the endocannabinoid system, has been implicated in several neuropsychiatric disorders, including major depressive disorder (MDD). It is speculated that increased brain FAAH expression is correlated with increased depressive symptoms. The aim of this scoping review was to establish the role of FAAH expression in animal models of depression to determine the translational potential of targeting FAAH in clinical studies. A literature search employing multiple databases was performed; all original articles that assessed FAAH expression in animal models of depression were considered. Of the 216 articles that were screened for eligibility, 24 articles met inclusion criteria and were included in this review. Three key findings emerged: (1) FAAH expression is significantly increased in depressive-like phenotypes; (2) genetic knockout or pharmacological inhibition of FAAH effectively reduces depressive-like behavior, with a dose-dependent effect; and (3) differences in FAAH expression in depressive-like phenotypes were largely localized to animal prefrontal cortex, hippocampus and striatum. We conclude, based on the animal literature, that a positive relationship can be established between brain FAAH level and expression of depressive symptoms. In summary, we suggest that FAAH is a tractable target for developing novel pharmacotherapies for MDD.

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