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https://www.readbyqxmd.com/read/28104279/effect-of-inhibition-of-fatty-acid-amide-hydrolase-on-mptp-induced-dopaminergic-neuronal-damage
#1
J M Viveros-Paredes, R E Gonzalez-Castañeda, A Escalante-Castañeda, A R Tejeda-Martínez, F Castañeda-Achutiguí, M E Flores-Soto
INTRODUCTION: Parkinson's disease (PD) is a neurodegenerative disorder characterised by balance problems, muscle rigidity, and slow movement due to low dopamine levels and loss of dopaminergic neurons in the substantia nigra pars compacta (SNpc). The endocannabinoid system is known to modulate the nigrostriatal pathway through endogenous ligands such as anandamide (AEA), which is hydrolysed by fatty acid amide hydrolase (FAAH). The purpose of this study was to increase AEA levels using FAAH inhibitor URB597 to evaluate the modulatory effect of AEA on dopaminergic neuronal death induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)...
January 16, 2017: Neurología: Publicación Oficial de la Sociedad Española de Neurología
https://www.readbyqxmd.com/read/28103941/involvement-of-the-endocannabinoid-system-in-the-physiological-response-to-transient-common-carotid-artery-occlusion-and-reperfusion
#2
Marina Quartu, Laura Poddighe, Tiziana Melis, Maria Pina Serra, Marianna Boi, Sara Lisai, Gianfranca Carta, Elisabetta Murru, Laura Muredda, Maria Collu, Sebastiano Banni
BACKGROUND: The transient global cerebral hypoperfusion/reperfusion achieved by induction of Bilateral Common Carotid Artery Occlusion followed by Reperfusion (BCCAO/R) may trigger a physiological response in an attempt to preserve tissue and function integrity. There are several candidate molecules among which the endocannabinoid system (ECS) and/or peroxisome-proliferator activated receptor-alpha (PPAR-alpha) may play a role in modulating oxidative stress and inflammation. The aims of the present study are to evaluate whether the ECS, the enzyme cyclooxygenase-2 (COX-2) and PPAR-alpha are involved during BCCAO/R in rat brain, and to identify possible markers of the ongoing BCCAO/R-induced challenge in plasma...
January 19, 2017: Lipids in Health and Disease
https://www.readbyqxmd.com/read/28092019/urb597-and-the-cannabinoid-win55-212-2-reduce-behavioral-and-neurochemical-deficits-induced-by-mptp-in-mice-possible-role-of-redox-modulation-and-nmda-receptors
#3
Angel Escamilla-Ramírez, Esperanza García, Guadalupe Palencia-Hernández, Ana Laura Colín-González, Sonia Galván-Arzate, Isaac Túnez, Julio Sotelo, Abel Santamaría
Several physiological events in the brain are regulated by the endocannabinoid system (ECS). While synthetic cannabinoid receptor (CBr) agonists such as WIN55,212-2 act directly on CBr, agents like URB597, a fatty acid amide hydrolase (FAAH) inhibitor, induce a more "physiological" activation of CBr by increasing the endogenous levels of the endocannabinoid anandamide (AEA). Herein, we compared the pre- and post-treatment efficacy of URB597 and WIN55,212-2 on different endpoints evaluated in the toxic model produced by the mitochondrial toxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in mice...
January 14, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28079617/manipulation-of-the-endocannabinoid-system-in-colitis-a-comprehensive-review
#4
Kristina L Leinwand, Mark E Gerich, Edward J Hoffenberg, Colm B Collins
BACKGROUND: Inflammatory bowel disease (IBD) is a lifelong disease of the gastrointestinal tract whose annual incidence and prevalence is on the rise. Current immunosuppressive therapies available for treatment of IBD offer limited benefits and lose effectiveness, exposing a significant need for the development of novel therapies. In the clinical setting, cannabis has been shown to provide patients with IBD symptomatic relief, although the underlying mechanisms of their anti-inflammatory effects remain unclear...
February 2017: Inflammatory Bowel Diseases
https://www.readbyqxmd.com/read/28065729/n-acylethanolamine-hydrolyzing-acid-amidase-and-fatty-acid-amide-hydrolase-inhibition-differentially-affect-n-acylethanolamine-levels-and-macrophage-activation
#5
Mireille Alhouayek, Pauline Bottemanne, Alexandros Makriyannis, Giulio G Muccioli
N-acylethanolamines (NAEs) such as N-palmitoylethanolamine and anandamide are endogenous bioactive lipids having numerous functions, including the control of inflammation. Their levels and therefore actions can be controlled by modulating the activity of two hydrolytic enzymes, N-acylethanolamine-hydrolyzing acid amidase (NAAA) and fatty acid amide hydrolase (FAAH). As macrophages are key to inflammatory processes, we used lipopolysaccharide-activated J774 macrophages, as well as primary mouse alveolar macrophages, to study the effect of FAAH and NAAA inhibition, using PF-3845 and AM9053 respectively, on macrophage activation and NAE levels measured by HPLC-MS...
January 5, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28065722/peripheral-endocannabinoid-signaling-controls-hyperphagia-in-western-diet-induced-obesity
#6
Donovan A Argueta, Nicholas V DiPatrizio
The endocannabinoid system in the brain and periphery plays a major role in controlling food intake and energy balance. We reported that tasting dietary fats was met with increased levels of the endocannabinoids, 2-arachidonoyl-sn-glycerol (2-AG) and anandamide, in the rat upper small intestine, and pharmacological inhibition of this local signaling event dose-dependently blocked sham feeding of fats. We now investigated the contribution of peripheral endocannabinoid signaling in hyperphagia associated with chronic consumption of a western-style diet in mice ([WD] i...
January 5, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28046144/endocannabinoids-concentrations-in-plasma-associated-with-feed-efficiency-and-carcass-composition-of-beef-steers
#7
V M Artegoitia, A P Foote, R M Lewis, D A King, S D Shackelford, T L Wheeler, H C Freetly
Endocannabinoids, including anandamide (AEA) and 2-arachidonoylglycerol (2-AG), are a class of endogenous lipid mediators that activate cannabinoids receptors and may be involved in the control of feed intake and energy metabolism. The objective of this study was to quantify AEA and 2-AG in plasma and identify possible associations with production traits and carcass composition in finishing beef steers. Individual DMI and BW gain were measured on 140 Angus-sired steers for 105 d on a finishing ration. Blood samples were collected on d 84 of the experiment, which was 40 d before slaughter...
December 2016: Journal of Animal Science
https://www.readbyqxmd.com/read/28017680/circulating-levels-of-endocannabinoids-respond-acutely-to-voluntary-exercise-are-altered-in-mice-selectively-bred-for-high-voluntary-wheel-running-and-differ-between-the-sexes
#8
Zoe Thompson, Donovan Argueta, Theodore Garland, Nicholas DiPatrizio
The endocannabinoid system serves many physiological roles, including in the regulation of energy balance, food reward, and voluntary locomotion. Signaling at the cannabinoid type 1 receptor has been specifically implicated in motivation for rodent voluntary exercise on wheels. We studied four replicate lines of high runner (HR) mice that have been selectively bred for 81 generations based on average number of wheel revolutions on days five and six of a six-day period of wheel access. Four additional replicate lines are bred without regard to wheel running, and serve as controls (C) for random genetic effects that may cause divergence among lines...
December 22, 2016: Physiology & Behavior
https://www.readbyqxmd.com/read/27999147/quantitative-profiling-of-endocannabinoids-and-related-n-acylethanolamines-in-human-csf-using-nano-lc-ms-ms
#9
Vasudev Kantae, Shinji Ogino, Marek Noga, Amy C Harms, Robin M van Dongen, Gerrit L J Onderwater, Arn M J M van den Maagdenberg, Gisela M Terwindt, Mario van der Stelt, Michel D Ferrari, Thomas Hankemeier
Endocannabinoids, a class of lipid messengers, have emerged as crucial regulators of synaptic communication in the central nervous system (CNS). Dysregulation of these compounds has been implicated in many brain disorders. Although some studies have identified and quantified a limited number of target compounds, a method that provides comprehensive quantitative information on endocannabinoids and related N-acylethanolamines (NAEs) in CSF is currently lacking as measurements are challenging due to low concentrations under normal physiological conditions...
December 20, 2016: Journal of Lipid Research
https://www.readbyqxmd.com/read/27997038/inflammation-of-peripheral-tissues-and-injury-to-peripheral-nerves-induce-diferring-effects-in-the-expression-of-the-calcium-sensitive-anandamide-synthesising-enzyme-and-related-molecules-in-rat-primary-sensory-neurons
#10
João Sousa-Valente, Angelika Varga, Jose Vicente Torres Perez, Agnes Jenes, John Wahba, Ken Mackie, Benjamin Cravatt, Natsuo Ueda, Kazuhito Tsuboi, Peter Santha, Gabor Jancso, Hiren Tailor, António Avelino, Istvan Nagy
Elevation of intracellular Ca(2+) concentration induces the synthesis of N-arachydonoylethanolamine (anandamide) in a sub-population of primary sensory neurons. N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) is the only known enzyme, which synthesises anandamide in a Ca(2+) -dependent manner. NAPE-PLD mRNA, as well as anandamide's main targets, the excitatory transient receptor potential vanilloid type 1 ion channel (TRPV1) and the inhibitory cannabinoid type 1 (CB1) receptor and the main anandamide-hydrolysing enzyme fatty acid amide hydrolase (FAAH) are all expressed by sub-populations of nociceptive primary sensory neurons...
December 20, 2016: Journal of Comparative Neurology
https://www.readbyqxmd.com/read/27989417/1-heteroarylpropan-2-ones-as-inhibitors-of-fatty-acid-amide-hydrolase-studies-on-structure-activity-relationships-and-metabolic-stability
#11
Stefan Zahov, David Garzinsky, Walburga Hanekamp, Matthias Lehr
The serine hydrolase fatty acid amide hydrolase (FAAH) catalyzes the degradation of the endocannabinoid anandamide, which possesses analgesic and anti-inflammatory effects. A new series of 1-heteroarylpropan-2-ones was synthesized and evaluated for FAAH inhibition. Structure-activity relationship studies revealed that 1H-benzotriazol-1-yl, 1H-7-azabenzotriazol-1-yl, 1H-tetrazol-1-yl and 2H-tetrazol-2-yl substituents have the highest impact on inhibitory potency. Furthermore, attempts were made to increase the limited metabolic stability of the ketone functionality of these compounds towards metabolic reduction by introduction of shielding alkyl substituents in proximity of this serine reactive group...
November 15, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27977335/fatty-acid-amide-hydrolase-morphine-interaction-influences-ventilatory-response-to-hypercapnia-and-postoperative-opioid-outcomes-in-children
#12
Vidya Chidambaran, Valentina Pilipenko, Kristie Spruance, Raja Venkatasubramanian, Jing Niu, Tsuyoshi Fukuda, Tomoyuki Mizuno, Kejian Zhang, Kenneth Kaufman, Alexander A Vinks, Lisa J Martin, Senthilkumar Sadhasivam
AIM: Fatty acid amide hydrolase (FAAH) degrades anandamide, an endogenous cannabinoid. We hypothesized that FAAH variants will predict risk of morphine-related adverse outcomes due to opioid-endocannabinoid interactions. PATIENTS & METHODS: In 101 postsurgical adolescents receiving morphine analgesia, we prospectively studied ventilatory response to 5% CO2 (HCVR), respiratory depression (RD) and vomiting. Blood was collected for genotyping and morphine pharmacokinetics...
January 2017: Pharmacogenomics
https://www.readbyqxmd.com/read/27966915/hydrophobic-ligand-entry-and-exit-pathways-of-the-cb1-cannabinoid-receptor
#13
Jakub Jakowiecki, Slawomir Filipek
It has been reported that some hydrophobic ligands of G-protein-coupled receptors access the receptor's binding site from the membrane rather than from bulk water. In order to identify the most probable ligand entrance pathway into the CB1 receptor, we performed several steered molecular dynamics (SMD) simulations of two CB1 agonists, THC and anandamide, pulling them from the receptor's binding site with constant velocity. The four main directions of ligand pulling were probed: between helices TM4 and TM5, between TM5 and TM6, between TM7 and TM1/TM2, and toward the bulk water...
December 27, 2016: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/27938441/a-dual-inhibitor-of-faah-and-trpv1-channels-shows-dose-dependent-effect-on-depression-like-behaviour-in-rats
#14
Christian Kirkedal, Gregers Wegener, Fabricio Moreira, Sâmia Regiane Lourenco Joca, Nico Liebenberg
OBJECTIVE: The cannabinoid receptor 1 (CB1) and transient receptor potential cation channel subfamily V member 1 (TRPV1) are proposed to mediate opposite behavioural responses. Their common denominator is the endocannabinoid ligand anandamide (AEA), which is believed to mediate antidepressant-like effect via CB1-R stimulation and depressive-like effect via TRPV1 activation. This is supposed to explain the bell-shaped dose-response curve for anandamide in preclinical models. METHODS: We investigated this assumption by administering the dual inhibitor of AEA hydrolysis and TRPV1 activation N-arachidonoyl-serotonin (AA-5HT) into the medial prefrontal cortex of rats...
December 12, 2016: Acta Neuropsychiatrica
https://www.readbyqxmd.com/read/27930725/avertin%C3%A2-but-not-volatile-anesthetics-addressing-the-two-pore-domain-k-channel-task-1-slows-down-cilia-driven-particle-transport-in-the-mouse-trachea
#15
Ghulam Murtaza, Petra Mermer, Uwe Pfeil, Wolfgang Kummer
RATIONALE: Volatile anesthetics inhibit mucociliary clearance in the airways. The two-pore domain K+ channel, TASK-1, represents one of their molecular targets in that they increase its open probability. Here, we determine whether particle transport speed (PTS) at the mucosal surface of the mouse trachea, an important factor of the cilia-driven mechanism in mucociliary clearance, is regulated by TASK-1. METHODOLOGY/RESULTS: RT-PCR analysis revealed expression of TASK-1 mRNA in the manually dissected and laser-assisted microdissected tracheal epithelium of the mouse...
2016: PloS One
https://www.readbyqxmd.com/read/27899300/role-of-the-endocannabinoid-system-in-the-control-of-mouse-myometrium-contractility-during-the-menstrual-cycle
#16
Ester Pagano, Pierangelo Orlando, Stefania Finizio, Antonietta Rossi, Lorena Buono, Fabio Arturo Iannotti, Fabiana Piscitelli, Angelo A Izzo, Vincenzo Di Marzo, Francesca Borrelli
Cannabis and cannabinoids are known to affect female reproduction. However, the role of the endocannabinoid system in mouse uterine contractility in the dioestrus and oestrus phases has not been previously investigated. The present study aimed at filling this gap. Endocannabinoid (anandamide and 2-arachidonoylglycerol) levels were measured in mouse uterus at dioestrus and oestrus phases by liquid chromatography-mass spectrometry; quantitative reverse transcription-PCR and western blot were used to measured the expression of cannabinoid receptors and enzymes involved in the metabolism of endocannabinoids...
January 15, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27893106/evidence-for-a-gpr18-role-in-diurnal-regulation-of-intraocular-pressure
#17
Sally Miller, Emma Leishman, Olivia Oehler, Laura Daily, Natalia Murataeva, Jim Wager-Miller, Heather Bradshaw, Alex Straiker
Purpose: The diurnal cycling of intraocular pressure (IOP) was first described in humans more than a century ago. This cycling is preserved in other species. The physiologic underpinning of this diurnal variation in IOP remains a mystery, even though elevated pressure is indicated in most forms of glaucoma, a common cause of blindness. Once identified, the system that underlies diurnal variation would represent a natural target for therapeutic intervention. Methods: Using normotensive mice, we measured the regulation of ocular lipid species by the enzymes fatty acid amide hydrolase (FAAH) and N-arachidonoyl phosphatidylethanolamine phospholipase (NAPE-PLD), mRNA expression of these enzymes, and their functional role in diurnal regulation of IOP...
November 1, 2016: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/27890711/the-endogenous-lipid-n-arachidonoyl-glycine-is-hypotensive-and-nitric-oxide-cgmp-dependent-vasorelaxant
#18
Yousuf M Al Suleimani, Ahmed S Al Mahruqi
N-arachidonoyl glycine (NAGLY), is the endogenous lipid that activates the G protein-couple receptor 18 (GPR18) with vasodilatory activity in resistance arteries. This study investigates its hemodynamic effects and mechanisms of vasorelaxation. Hemodynamic effects of NAGLY in rats were assessed using a Biopac system and its vascular responses were assessed using a wire myograph. NAGLY (1mg/kg) decreased blood pressure by 69.4±5.5% and reduced renal blood flow by 88±12% and the effects were not sensitive to inhibition by O-1918 (3mg/kg)...
January 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27890602/the-endocannabinoid-hydrolysis-inhibitor-sa-57-intrinsic-antinociceptive-effects-augmented-morphine-induced-antinociception-and-attenuated-heroin-seeking-behavior-in-mice
#19
Jenny L Wilkerson, Sudeshna Ghosh, Mohammed Mustafa, Rehab A Abdullah, Micah J Niphakis, Roberto Cabrera, Rafael L Maldonado, Benjamin F Cravatt, Aron H Lichtman
Although opioids are highly efficacious analgesics, their abuse potential and other untoward side effects diminish their therapeutic utility. The addition of non-opioid analgesics offers a promising strategy to reduce required antinociceptive opioid doses that concomitantly reduce opioid-related side effects. Inhibitors of the primary endocannabinoid catabolic enzymes fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) show opioid-sparing effects in preclinical models of pain. As simultaneous inhibition of these enzymes elicits enhanced antinociceptive effects compared with single enzyme inhibition, the present study tested whether the dual FAAH-MAGL inhibitor SA-57 [4-[2-(4-chlorophenyl)ethyl]-1-piperidinecarboxylic acid 2-(methylamino)-2-oxoethyl ester] produces morphine-sparing antinociceptive effects, without major side effects associated with either drug class...
March 1, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/27889577/brain-uptake-and-metabolism-of-the-endocannabinoid-anandamide-labeled-in-either-the-arachidonoyl-or-ethanolamine-moiety
#20
Kun Hu, Shilpa Sonti, Sherrye T Glaser, Richard I Duclos, Samuel J Gatley
INTRODUCTION: Anandamide (N-arachidonoylethanolamine) is a retrograde neuromodulator that activates cannabinoid receptors. The concentration of anandamide in the brain is controlled by fatty acid amide hydrolase (FAAH), which has been the focus of recent drug discovery efforts. Previous studies in C57BL/6 mice using [(3)H-arachidonoyl]anandamide demonstrated deposition of tritium in thalamus and cortical areas that was blocked by treatment with an FAAH inhibitor and that was not seen in FAAH-knockout mice...
February 2017: Nuclear Medicine and Biology
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