Article
Biochemistry & Molecular Biology
Chaoling Chen, Weili Wang, Justin L. Poklis, Aron H. Lichtman, Joseph K. Ritter, Gaizun Hu, Dengpiao Xie, Ningjun Li
Summary: The study suggests that FAAH activation and the consequent reduction of AEA contribute to renal fibrogenesis, while FAAH inhibition protects against fibrogenesis in renal cells independently of CB receptors via the AEA-COX-2 pathway.
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE
(2022)
Article
Chemistry, Medicinal
Tugce Gur Maz, Sumeyye Turanli, H. Burak Caliskan, Burcu Caliskan, Erden Banoglu
Summary: A series of novel piperazine urea derivatives with thiadiazole moieties were designed, synthesized, and investigated for their inhibition potential against human fatty acid amide hydrolase (hFAAH). The urea derivatives possessing p-chlorophenylthiadiazole and benzylpiperazine fragments were identified as effective inhibitors of hFAAH, with compounds containing 4-chlorobenzyl and 4-fluorobenzyl tails showing the highest activity.
ARCHIV DER PHARMAZIE
(2022)
Article
Biochemistry & Molecular Biology
Alessandro Deplano, Jessica Karlsson, Federica Moraca, Mona Svensson, Claudia Cristiano, Carmine Marco Morgillo, Christopher J. Fowler, Roberto Russo, Bruno Catalanotti, Valentina Onnis
Summary: The study identifies Flu-AM4 as a dual-action FAAH/substrate-selective COX inhibitor with anti-inflammatory and analgesic activity in animal pain models.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Anugrah D. Santoso, Dirk De Ridder
Summary: Modulation of FAAH has immense potential as a new therapeutic candidate for several disorders, but further exploration is still needed to determine the best treatment strategy.
CANNABIS AND CANNABINOID RESEARCH
(2023)
Article
Genetics & Heredity
Lisa Bornscheuer, Andreas Lundin, Yvonne Forsell, Catharina Lavebratt, Philippe A. Melas
Summary: This study explores the relationship between fatty acid amide hydrolase (FAAH) and subjective well-being, and found a functional polymorphism in the FAAH gene to be associated with decreased well-being and increased alcohol dependence. The findings suggest that chronically elevated levels of anandamide may disrupt the well-being system, leading to increased alcohol intake.
Article
Neurosciences
Karla Chavira-Ramos, Mario Orozco-Morales, Cimen Karasu, Alexey A. Tinkov, Michael Aschner, Abel Santamaria, Ana Laura Colin-Gonzalez
Summary: Endocannabinoid-based therapies show potential as a tool for treating neurodegenerative disorders, with experimental studies demonstrating the neuroprotective properties of the FAAH inhibitor URB597 in preventing early toxic effects induced by QUIN in rat cortical tissue. The protective effects of URB597 were found to be mediated by the activation of CB1 receptors and were similar to those observed with AEA, suggesting a potential link between FAAH inhibition and the protective effects of endocannabinoids.
NEUROTOXICITY RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Sanela Rajlic, Luise Surmann, Pia Zimmermann, Christina Katharina Weisheit, Laura Bindila, Hendrik Treede, Markus Velten, Andreas Daiber, Georg Daniel Duerr
Summary: Ischemic cardiomyopathy leads to inflammation and left ventricular dysfunction. Animal studies suggest that the endocannabinoid system may have cardioprotective effects, including cardiomyocyte adaptation, inflammation, and remodeling. This study investigates the potential cardioprotective effect of the endocannabinoid anandamide (AEA) after ischemia and reperfusion using FAAH (-/-) mice and suggests that increased endocannabinoids may have detrimental effects on cardiomyocyte survival due to PPAR-alpha activation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Veterinary Sciences
Vikram Thakur, Mohammad Bashashati, Josue Enriquez, Munmun Chattopadhyay
Summary: This study assessed specific gastrointestinal symptoms in Type 1 diabetic mice and evaluated treatment options for this condition. The results showed that inhibiting endocannabinoid degradation may have a therapeutic effect on gastrointestinal dysmotility.
VETERINARY SCIENCES
(2022)
Article
Neuroimaging
Kevin M. Crombie, Anthony A. Privratsky, Chloe M. Schomaker, Mickela Heilicher, Marisa C. Ross, Anneliis Sartin-Tarm, Kyrie Sellnow, Elisabeth B. Binder, G. Andrew James, Josh M. Cisler
Summary: This study found that genetic variation in the FAAH gene influences the physiological, cognitive, and neural fear learning characteristics in women with PTSD. Different genotypes showed divergent physiological and neural responses, suggesting that targeting FAAH may be a promising therapeutic approach for PTSD.
NEUROIMAGE-CLINICAL
(2022)
Review
Neurosciences
Shivanshu Bajaj, Shreshta Jain, Preeti Vyas, Sandhya Bawa, Divya Vohora
Summary: Alzheimer's disease is a neurodegenerative disease with potential therapeutic targets in the endocannabinoid system. Inhibitors of monoacylglycerol (MAGL) and fatty acid amide hydrolase (FAAH) possess multi-faceted properties for the treatment of Alzheimer's disease.
BRAIN RESEARCH BULLETIN
(2021)
Review
Psychiatry
S. Alisha Epps
Summary: Depression and epilepsy show bidirectional comorbidity, and exploring the endocannabinoid system may lead to more effective treatments for both conditions.
FRONTIERS IN PSYCHIATRY
(2022)
Article
Cell Biology
Jie Wen, Scott Sackett, Mikiei Tanaka, Yumin Zhang
Summary: Chronic neuropathic pain resulting from peripheral nerve damage is a significant clinical problem. Inhibition of endocannabinoid hydrolysis and oxygenation simultaneously may be a suitable strategy for the treatment of inflammatory and neuropathic pain. This study demonstrates that the combination of a fatty acid amide hydrolase (FAAH) inhibitor and a substrate-selective COX-2 inhibitor reduces pain behaviors and inflammatory response in a chronic constriction injury (CCI) mouse model.
Article
Neurosciences
Yannick Fotio, Alex Mabou Tagne, Kwang-Mook Jung, Daniele Piomelli
Summary: In this study, the effects of two novel brain-permeable FAAH inhibitors, ARN14633 and ARN14280, were investigated in a rat model of predator stress-induced long-term anxiety. The results showed that these inhibitors effectively reduced anxiety-like behaviors and were correlated with the inhibition of FAAH activity and increase in FAAH substrate levels. This study supports the potential clinical application of FAAH inhibitors in the management of PTSD.
PSYCHOPHARMACOLOGY
(2023)
Review
Pharmacology & Pharmacy
Greta Niemela, Garth E. Terry
Summary: Recent research suggests that chronic alcohol exposure induces changes in the endocannabinoid system, making it a potential target for understanding and treating AUD. Studies focused on the role of FAAH, an enzyme that degrades anandamide, in the biology of AUD and found that FAAH modulation may impact alcohol consumption and withdrawal symptoms. Inhibition of FAAH shows promise for reducing withdrawal symptoms but may also lead to increased alcohol preference and intake, indicating the need for further research.
CANNABIS AND CANNABINOID RESEARCH
(2021)
Review
Cell Biology
Alessandro Papa, Silvia Pasquini, Chiara Contri, Sandra Gemma, Giuseppe Campiani, Stefania Butini, Katia Varani, Fabrizio Vincenzi
Summary: Polypharmacology challenges the traditional paradigm of one-drug, one target, one disease by using multitarget compounds for the treatment of complex diseases. The endocannabinoid system is an attractive therapeutic target in central nervous system disorders and neurodegenerative diseases.