scholarly journals N-Cyclohexanecarbonylpentadecylamine: a selective inhibitor of the acid amidase hydrolysing N-acylethanolamines, as a tool to distinguish acid amidase from fatty acid amide hydrolase

2004 ◽  
Vol 379 (1) ◽  
pp. 99-106 ◽  
Author(s):  
Kazuhito TSUBOI ◽  
Christine HILLIGSMANN ◽  
Séverine VANDEVOORDE ◽  
Didier M. LAMBERT ◽  
Natsuo UEDA
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Physiological Role ◽  
Ph Optimum ◽  
Ph Values ◽  
Amide Hydrolase ◽  
Derivatives Of ◽  
Fatty Acid Amide

Anandamide (N-arachidonoylethanolamine) and other bioactive N-acylethanolamines are degraded to their corresponding fatty acids and ethanolamine. This hydrolysis is mostly attributed to catalysis by FAAH (fatty acid amide hydrolase), which exhibits an alkaline pH optimum. In addition, we have identified another amidase which catalyses the same reaction exclusively at acidic pH values [Ueda, Yamanaka and Yamamoto (2001) J. Biol. Chem. 276, 35552–35557]. In attempts to find selective inhibitors of this acid amidase, we screened various derivatives of palmitic acid, 1-hexadecanol, and 1-pentadecylamine with N-palmitoylethanolamine as substrate. Here we show that N-cyclohexanecarbonylpentadecylamine inhibits the acid amidase from rat lung with an IC50 of 4.5 µM, without inhibiting FAAH at concentrations up to 100 µM. The inhibition was reversible and non-competitive. This compound also inhibited the acid amidase in intact alveolar macrophages. With the aid of this inhibitor, it was revealed that rat basophilic leukaemia cells possess the acid amidase as well as FAAH. Thus the inhibitor may be a useful tool to distinguish the acid amidase from FAAH in various tissues and cells and to elucidate the physiological role of the enzyme.

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.

scholarly journals Suppression of acute and anticipatory nausea by peripherally restricted fatty acid amide hydrolase inhibitor in animal models: role of PPARα and CB1 receptors

2017 ◽  
Vol 174 (21) ◽  
pp. 3837-3847 ◽  
Author(s):  
Erin M Rock ◽  
Guillermo Moreno-Sanz ◽  
Cheryl L Limebeer ◽  
Gavin N Petrie ◽  
Roberto Angelini ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Animal Models ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Cb1 Receptors ◽  
Anticipatory Nausea ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

Role of the basolateral amygdala in mediating the effects of the fatty acid amide hydrolase inhibitor URB597 on HPA axis response to stress

2014 ◽  
Vol 24 (9) ◽  
pp. 1511-1523 ◽  
Author(s):  
Gaurav Bedse ◽  
Roberto Colangeli ◽  
Angelo M. Lavecchia ◽  
Adele Romano ◽  
Fabio Altieri ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Hpa Axis ◽  
Basolateral Amygdala ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Response To Stress ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

scholarly journals Role of Steroids on the Membrane Binding Ability of Fatty Acid Amide Hydrolase

2019 ◽  
Vol 4 (1) ◽  
pp. 42-50 ◽  
Author(s):  
Annalaura Sabatucci ◽  
Monica Simonetti ◽  
Daniel Tortolani ◽  
Clotilde B. Angelucci ◽  
Enrico Dainese ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Membrane Binding ◽  
Acid Amide ◽  
Binding Ability ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

Role of Fatty Acid Amide Hydrolase in the Transport of the Endogenous Cannabinoid Anandamide

2001 ◽  
Vol 59 (6) ◽  
pp. 1369-1375 ◽  
Author(s):  
Theresa A. Day ◽  
Fariborz Rakhshan ◽  
Dale G. Deutsch ◽  
Eric L. Barker
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Amide Hydrolase ◽  
Endogenous Cannabinoid ◽  
Fatty Acid Amide

scholarly journals Design, Synthesis, and In Vitro Evaluation of Carbamate Derivatives of 2-Benzoxazolyl- and 2-Benzothiazolyl-(3-hydroxyphenyl)-methanones as Novel Fatty Acid Amide Hydrolase Inhibitors

2007 ◽  
Vol 50 (17) ◽  
pp. 4236-4242 ◽  
Author(s):  
Mikko J. Myllymäki ◽  
Susanna M. Saario ◽  
Antti O. Kataja ◽  
Joel A. Castillo-Melendez ◽  
Tapio Nevalainen ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Design Synthesis ◽  
In Vitro Evaluation ◽  
Amide Hydrolase ◽  
Derivatives Of ◽  
Fatty Acid Amide

Inhibition of fatty acid amide hydrolase and cyclooxygenase by the N-(3-methylpyridin-2-yl)amide derivatives of flurbiprofen and naproxen

2013 ◽  
Vol 720 (1-3) ◽  
pp. 383-390 ◽  
Author(s):  
Mariateresa Cipriano ◽  
Emmelie Björklund ◽  
Alan A. Wilson ◽  
Cenzo Congiu ◽  
Valentina Onnis ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Amide Derivatives ◽  
Amide Hydrolase ◽  
Derivatives Of ◽  
Fatty Acid Amide

scholarly journals The role of fatty acid amide hydrolase inhibition in nicotine reward and dependence

Life Sciences ◽  
2013 ◽  
Vol 92 (8-9) ◽  
pp. 458-462 ◽  
Author(s):  
Pretal P. Muldoon ◽  
Aron H. Lichtman ◽  
Loren H. Parsons ◽  
M. Imad Damaj
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

The role of fatty acid amide hydrolase enzyme inhibitors in Alzheimer's disease

2021 ◽  
Author(s):  
Smita Jain ◽  
Akansha Bisht ◽  
Kanika Verma ◽  
Swarnima Negi ◽  
Sarvesh Paliwal ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Fatty Acid ◽  
Enzyme Inhibitors ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

scholarly journals Exploring the fatty acid amide hydrolase and cyclooxygenase inhibitory properties of novel amide derivatives of ibuprofen

2020 ◽  
Vol 35 (1) ◽  
pp. 815-823 ◽  
Author(s):  
Alessandro Deplano ◽  
Jessica Karlsson ◽  
Mona Svensson ◽  
Federica Moraca ◽  
Bruno Catalanotti ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Amide Derivatives ◽  
Amide Hydrolase ◽  
Derivatives Of ◽  
Fatty Acid Amide
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