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https://www.readbyqxmd.com/read/28633967/the-effects-of-chronic-faah-inhibition-on-myocardial-lipid-metabolism-in-normotensive-and-doca-salt-hypertensive-rats
#1
Agnieszka Polak, Ewa Harasim-Symbor, Barbara Malinowska, Irena Kasacka, Anna Pędzińska-Betiuk, Jolanta Weresa, Adrian Chabowski
AIMS: There is significant evidence that the endocannabinoid system (ECS) takes part in the regulation of the cardiovascular system in hypertension. It is quite well established that hypertension causes several changes in the heart metabolism, but it is still unknown whether the ECS affects this process. Therefore, we investigated the influence of prolonged ECS activation on myocardial lipid metabolism in deoxycorticosterone acetate (DOCA)-salt hypertensive rats by chronic fatty acid amide hydrolase (FAAH) inhibition...
June 17, 2017: Life Sciences
https://www.readbyqxmd.com/read/28611585/role-of-n-arachidonoyl-serotonin-aa-5-ht-in-sleep-wake-cycle-architecture-sleep-homeostasis-and-neurotransmitters-regulation
#2
Eric Murillo-Rodríguez, Vincenzo Di Marzo, Sergio Machado, Nuno B Rocha, André B Veras, Geraldo A M Neto, Henning Budde, Oscar Arias-Carrión, Gloria Arankowsky-Sandoval
The endocannabinoid system comprises several molecular entities such as endogenous ligands [anandamide (AEA) and 2-arachidonoylglycerol (2-AG)], receptors (CB1 and CB2), enzymes such as [fatty acid amide hydrolase (FAHH) and monoacylglycerol lipase (MAGL)], as well as the anandamide membrane transporter. Although the role of this complex neurobiological system in the sleep-wake cycle modulation has been studied, the contribution of the blocker of FAAH/transient receptor potential cation channel subfamily V member 1 (TRPV1), N-arachidonoyl-serotonin (AA-5-HT) in sleep has not been investigated...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28596366/activity-based-protein-profiling-reveals-off-target-proteins-of-the-faah-inhibitor-bia-10-2474
#3
Annelot C M van Esbroeck, Antonius P A Janssen, Armand B Cognetta, Daisuke Ogasawara, Guy Shpak, Mark van der Kroeg, Vasudev Kantae, Marc P Baggelaar, Femke M S de Vrij, Hui Deng, Marco Allarà, Filomena Fezza, Zhanmin Lin, Tom van der Wel, Marjolein Soethoudt, Elliot D Mock, Hans den Dulk, Ilse L Baak, Bogdan I Florea, Giel Hendriks, Luciano De Petrocellis, Herman S Overkleeft, Thomas Hankemeier, Chris I De Zeeuw, Vincenzo Di Marzo, Mauro Maccarrone, Benjamin F Cravatt, Steven A Kushner, Mario van der Stelt
A recent phase 1 trial of the fatty acid amide hydrolase (FAAH) inhibitor BIA 10-2474 led to the death of one volunteer and produced mild-to-severe neurological symptoms in four others. Although the cause of the clinical neurotoxicity is unknown, it has been postulated, given the clinical safety profile of other tested FAAH inhibitors, that off-target activities of BIA 10-2474 may have played a role. Here we use activity-based proteomic methods to determine the protein interaction landscape of BIA 10-2474 in human cells and tissues...
June 9, 2017: Science
https://www.readbyqxmd.com/read/28583049/n-arachidonoyl-serotonin-a-dual-faah-and-trpv1-blocker-inhibits-the-retrieval-of-contextual-fear-memory-role-of-the-cannabinoid-cb1-receptor-in-the-dorsal-hippocampus
#4
Pedro H Gobira, Isabel V Lima, Luara A Batista, Antônio C de Oliveira, Leonardo B Resstel, Carsten T Wotjak, Daniele C Aguiar, Fabricio A Moreira
Anandamide, an endocannabinoid, inhibits aversive responses by activating the CB1 cannabinoid receptor. At high concentrations, however, anandamide may exert pro-aversive activities mediated by the transient receptor potential vanilloid type-1 channel (TRPV1). Accordingly, N-arachidonoyl-serotonin (AA-5-HT), a dual blocker of the anandamide-hydrolysing enzyme fatty acid amide hydrolase (FAAH) and the TRPV1 channel, induces anxiolytic-like effects. Here we tested the hypothesis that AA-5-HT inhibits the expression of contextual fear conditioning by facilitating CB1 receptor signalling in the dorsal hippocampus of mice...
June 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28579484/acylethanolamides-and-endocannabinoid-signaling-system-in-dorsal-striatum-of-rats-exposed-to-perinatal-asphyxia
#5
Mariana I Holubiec, Juan I Romero, Eduardo Blanco, Tamara Logica Tornatore, Juan Suarez, Fernando Rodríguez de Fonseca, Pablo Galeano, Francisco Capani
Endocannabinoids (eCBs) and acylethanolamides (AEs) have lately received more attention due to their neuroprotective functions in neurological disorders. Here we analyze the alterations induced by perinatal asphyxia (PA) in the main metabolic enzymes and receptors of the eCBs/AEs in the dorsal striatum of rats. To induce PA, we used a model developed by Bjelke et al. (1991). Immunohistochemical techniques were carried out to determine the expression of neuronal and glial markers (NeuN and GFAP), eCBs/AEs synthesis and degradation enzymes (DAGLα, NAPE-PLD and FAAH) and their receptors (CB1 and PPARα)...
June 1, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28577869/polyunsaturated-fatty-acids-differentially-modulate-cell-proliferation-and-endocannabinoid-system-in-two-human-cancer-lines
#6
Repossi Gastón, Pasqualini María Eugenia, Undurti N Das, Aldo R Eynard
BACKGROUND AND AIMS: Evidence suggests that quantity and quality of dietary polyunsaturated fatty acids (PUFAs) play a role in the development of cancer. However, the mechanisms involved in this interaction(s) are not clear. Endocannabinoids are lipid metabolites known to have growth modulatory actions. We studied the effect of supplementation with PUFAs ω-6 and ω-3 (essential fatty acids, EFAs), saturated and monounsaturated fatty acids (non-EFAs) on the growth of tumor cells and modifications in their endocannabinoid content...
January 2017: Archives of Medical Research
https://www.readbyqxmd.com/read/28570479/sensitization-of-c-fiber-nociceptors-in-mice-with-sickle-cell-disease-is-decreased-by-local-inhibition-of-anandamide-hydrolysis
#7
Megan L Uhelski, Kalpna Gupta, Donald A Simone
Chronic pain and hyperalgesia, as well as pain resulting from episodes of vasoocclusion, are characteristic features of sickle cell disease (SCD) and are difficult to treat. Since there is growing evidence that increasing local levels of endocannabinoids can decrease hyperalgesia, we examined the effects of URB597, a fatty acid amide hydrolase (FAAH) inhibitor which blocks the hydrolysis of the endogenous cannabinoid anandamide (AEA), on hyperalgesia and sensitization of cutaneous nociceptors in a humanized mouse model of SCD...
May 31, 2017: Pain
https://www.readbyqxmd.com/read/28549792/endocannabinoids-modulate-apoptosis-in-endometriosis-and-adenomyosis
#8
Elif Bilgic, Elif Guzel Meydanli, Sevil Kose, Makbule Cisel Aydin, Eda Karaismailoglu, Irem Akar, Alp Usubutun, Petek Korkusuz
Adenomyosis that is a form of endometriosis is the growth of ectopic endometrial tissue within the muscular wall of the uterus (myometrium), which may cause dysmenorrhea and infertility. Endocannabinoid mediated apoptotic mechanisms of endometriosis and adenomyosis are not known. We hypothesized that the down regulation of endocannabinoid receptors and/or alteration in their regulatory enzymes may have a direct role in the pathogenesis of endometriosis and adenomyosis through apoptosis. Endocannabinoid receptors CB1 and CB2, their synthesizing and catabolizing enzymes (FAAH, NAPE-PLD, DAGL, MAGL) and the apoptotic indexes were immunohistochemically assessed in endometriotic and adenomyotic tissues...
May 23, 2017: Acta Histochemica
https://www.readbyqxmd.com/read/28545594/early-blockade-of-joint-inflammation-with-a-fatty-acid-amide-hydrolase-inhibitor-decreases-end-stage-osteoarthritis-pain-and-peripheral-neuropathy-in-mice
#9
Jason J McDougall, Milind M Muley, Holly T Philpott, Allison Reid, Eugene Krustev
BACKGROUND: The endocannabinoid system has been shown to reduce inflammatory flares and pain in rodent models of arthritis. A limitation of endocannabinoids is that they are rapidly denatured by hydrolysing enzymes such as fatty acid amide hydrolase (FAAH) which renders them physiologically inert. Osteoarthritis (OA) is primarily a degenerative joint disease; however, it can incorporate mild inflammation and peripheral neuropathy. The aim of this study was to determine whether early blockade of FAAH bioactivity could reduce OA-associated inflammation and joint neuropathy...
May 25, 2017: Arthritis Research & Therapy
https://www.readbyqxmd.com/read/28535469/novel-propanamides-as-fatty-acid-amide-hydrolase-inhibitors
#10
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
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 characterizing the agonists of the cannabinoid receptors. Here we present the discovery of a novel class of profen derivatives, the N-(heteroaryl)-2-(4-((2-(trifluoromethyl)pyridin-4-yl)amino)phenyl)propanamides, as FAAH inhibitors...
May 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28534260/pharmacogenetics-of-cannabinoids
#11
Szymon Hryhorowicz, Michal Walczak, Oliwia Zakerska-Banaszak, Ryszard Słomski, Marzena Skrzypczak-Zielińska
Although the application of medical marijuana and cannabinoid drugs is controversial, it is a part of modern-day medicine. The list of diseases in which cannabinoids are promoted as a treatment is constantly expanding. Cases of significant improvement in patients with a very poor prognosis of glioma or epilepsy have already been described. However, the occurrence of side effects is still difficult to estimate, and the current knowledge of the therapeutic effects of cannabinoids is still insufficient. In our opinion, the answers to many questions and concerns regarding the medical use of cannabis can be provided by pharmacogenetics...
May 22, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28501776/inhibition-of-senp3-by-urb597-ameliorates-neurovascular-unit-dysfunction-in-rats-with-chronic-cerebral-hypoperfusion
#12
Da-Peng Wang, Ke-Jia Liu, Graham Kasper, Qi Lin, Jian Hai
Disruption of the neurovascular unit (NVU), induced by chronic cerebral hypoperfusion (CCH), has been broadly found in various neurological disorders. SUMO-specific protease 3 (SENP3) is expressed in neurons, astrocytes, and microglia, and regulates a variety of cell events. However, whether SENP3 is involved in neurovascular injury under the condition of CCH is still elusive. To address this issue, we investigated the effect of the fatty acid amide hydrolase (FAAH) inhibitor URB597 on NVU and the role of SENP3 in this process, as well as the underling mechanisms...
July 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28499834/n-stearoyltyrosine-protects-primary-cortical-neurons-against-oxygen-glucose-deprivation-induced-apoptosis-through-inhibiting-anandamide-inactivation-system
#13
Heng-Jing Cui, Sha Liu, Rui Yang, Guo-Hui Fu, Yang Lu
N-stearoylthrosine (NST), a synthesized anandamide (AEA) analogue, plays a neuroprotective role in neurodegenerative diseases and cerebrovascular diseases. Several studies have demonstrated that the endocannabinoids systems (ECS) are involved in the neuroprotective effects against cerebral ischemic injury. Oxygen-glucose deprivation (OGD)-induced neuronal injury elevated the levels of endocannabinoids and activated ECS. This research was conducted to investigate the neuroprotective effect of NST against OGD-induced neuronal injury in cultured primary cortical neurons and the potential mechanism involved...
May 9, 2017: Neuroscience Research
https://www.readbyqxmd.com/read/28488728/fatty-acid-amide-hydrolase-faah-regulates-hypercapnia-ischemia-induced-increases-in-n-acylethanolamines-in-mouse-brain
#14
Lin Lin, Adam H Metherel, Peter J Jones, Richard P Bazinet
N-acylethanolamines (NAEs) are endogenous lipid ligands for several receptors including cannabinoid receptors and peroxisome proliferator-activated receptor-alpha (PPAR-α), which regulate numerous physiological functions. Fatty acid amide hydrolase (FAAH) is, largely, responsible for the degradation of NAEs. However, at high concentrations of ethanolamines and unesterified fatty acids, FAAH can also catalyze the reverse reaction, producing NAEs. Several brain insults such as ischemia and hypoxia increase brain unesterified fatty acids...
May 10, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28481838/contribution-of-endocannabinoid-gene-expression-and-genotype-on-low-back-pain-susceptibility-and-chronicity
#15
Divya Ramesh, Amy D'Agata, Angela Starkweather, Erin Young
A major research emphasis has been focused on defining the molecular changes that occur from acute to chronic pain in order to identify potential therapeutic targets for chronic pain. As the endocannabinoid system is dynamically involved in pain signaling, a plausible mechanism that may contribute to chronic pain vulnerability involves alterations in the amount of circulating endocannabinoids. Therefore, this study sought to examine cannabinoid type-1 (CNR1), type-2 (CNR2) receptors, fatty acid amide hydrolase (FAAH) and the vanilloid receptor (TRPV1) gene expression profiles among individuals with acute and chronic LBP at their baseline visit...
May 5, 2017: Clinical Journal of Pain
https://www.readbyqxmd.com/read/28479394/ampk-contributes-to-aerobic-exercise-induced-antinociception-downstream-of-endocannabinoids
#16
Tanya S King-Himmelreich, Christine V Möser, Miriam C Wolters, Julia Schmetzer, Yannik Schreiber, Nerea Ferreirós, Otto Q Russe, Gerd Geisslinger, Ellen Niederberger
Physical exercise has been repeatedly associated with decreased nociceptive responses but the underlying mechanisms have still not been fully clarified. In this study, we investigated exercise-induced effects after a single bout of treadmill running on the mouse model of formalin-induced inflammatory nociception. As potential molecular mediators, we focused on endogenous endocannabinoids as well as AMP-activated protein kinase (AMPK). Our results showed that wild type mice display a reduced nociceptive response in the formalin test after treadmill running, while exercise had no effect on inflammatory nociception in AMPKα2 knockout mice...
May 4, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28478955/spatial-distribution-of-cannabinoid-receptor-1-and-fatty-acid-amide-hydrolase-in-the-cat-ovary-and-oviduct
#17
Andrea Pirone, Carla Lenzi, Angela Briganti, Francesco Abbate, Maria Levanti, Francesca Abramo, Vincenzo Miragliotta
Involvement of the endocannabinoid system in female reproduction has been extensively described in humans with the cognate receptors and ligands being found in the ovaries and genital tract. In human, an imbalance of the endocannabinoid system is linked with both ectopic pregnancy and infertility. In bovine species anandamide levels regulate aspects of sperm-oviduct interaction. Here we report the immunohistochemical distribution of cannabinoid receptor 1 (CB1R) and fatty acid amide hydrolase (FAAH) in cat ovary and oviduct, using paraffin-embedded tissue samples and commercially available antibodies...
May 4, 2017: Acta Histochemica
https://www.readbyqxmd.com/read/28448548/altered-striatal-endocannabinoid-signaling-in-a-transgenic-mouse-model-of-spinocerebellar-ataxia-type-3
#18
Carmen Rodríguez-Cueto, Mariluz Hernández-Gálvez, Cecilia J Hillard, Patricia Maciel, Sara Valdeolivas, José A Ramos, María Gómez-Ruiz, Javier Fernández-Ruiz
Spinocerebellar ataxia type-3 (SCA-3) is the most prevalent autosomal dominant inherited ataxia. We recently found that the endocannabinoid system is altered in the post-mortem cerebellum of SCA-3 patients, and similar results were also found in the cerebellar and brainstem nuclei of a SCA-3 transgenic mouse model. Given that the neuropathology of SCA-3 is not restricted to these two brain regions but rather, it is also evident in other structures (e.g., the basal ganglia), we studied the possible changes to endocannabinoid signaling in the striatum of these transgenic mice...
2017: PloS One
https://www.readbyqxmd.com/read/28446875/cannabinoid-modulation-of-memory-consolidation-in-rats-beyond-the-role-of-cannabinoid-receptor-subtype-1
#19
Patrizia Ratano, Maura Palmery, Viviana Trezza, Patrizia Campolongo
The effects induced by exogenous manipulation of endocannabinoid neurotransmission on emotion and memory are often contradictory. Among the different factors involved, of particular interest is the binding affinity of endocannabinoids, and their analogs, for other receptor families beyond cannabinoid receptors, such as the peroxisome proliferator-activated receptors (PPARs), and the transient receptor potential cation channel subfamily V member 1 (TRPV1). The aim of this study was to investigate which receptor subtype mediates cannabinoid effects on memory consolidation for emotionally arousing experiences...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28437860/chronic-inhibition-of-fatty-acid-amide-hydrolase-by-urb597-produces-differential-effects-on-cardiac-performance-in-normotensive-and-hypertensive-rats
#20
Anna Pędzińska-Betiuk, Jolanta Weresa, Marek Toczek, Marta Baranowska-Kuczko, Irena Kasacka, Ewa Harasim-Symbor, Barbara Malinowska
BACKGROUND AND PURPOSE: Fatty acid amide hydrolase (FAAH) inhibitors are postulated to possess anti-hypertensive potential, because their acute injection decreases BP in spontaneously hypertensive rats (SHR), partly through normalization of cardiac contractile function. Here, we examined whether the potential hypotensive effect of chronic FAAH inhibition by URB597 in hypertensive rats correlated with changes in cardiac performance. EXPERIMENTAL APPROACH: Experiments were performed using perfused hearts and left atria isolated from 8- to 10-week-old SHR, age-matched deoxycorticosterone acetate (DOCA)-salt rats and normotensive controls chronically treated with URB597 (1 mg·kg(-1) ) or vehicle...
July 2017: British Journal of Pharmacology
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