keyword
MENU ▼
Read by QxMD icon Read
search

URB597

keyword
https://www.readbyqxmd.com/read/27889577/brain-uptake-and-metabolism-of-the-endocannabinoid-anandamide-labeled-in-either-the-arachidonoyl-or-ethanolamine-moiety
#1
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...
November 9, 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/27771531/involvement-of-cb1-and-trpv1-receptors-located-in-the-ventral-medial-prefrontal-cortex-in-the-modulation-of-stress-coping-behavior
#2
A G Sartim, F A Moreira, S R L Joca
Cannabinoid type-1 (CB1) and transient receptor potential vanilloid type-1 (TRPV1) receptors may have opposite roles in modulating neural activity and, consequently, in regulating the stress response. These receptors are widely expressed in several brain structures, including the ventral medial prefrontal cortex (vmPFC). The functional consequences of the interaction between CB1 and TRPV1, however, have scarcely been explored. Therefore, we investigated if CB1 and TRPV1 receptors located in the vmPFC would be involved in the behavioral changes induced by the stress of the forced swim test (FST)...
October 19, 2016: Neuroscience
https://www.readbyqxmd.com/read/27746343/revealing-the-role-of-the-endocannabinoid-system-modulators-sr141716a-urb597-and-vdm-11-in-sleep-homeostasis
#3
Eric Murillo-Rodríguez, Sergio Machado, Nuno Barbosa Rocha, Henning Budde, Ti-Fei Yuan, Oscar Arias-Carrión
The endocannabinoid system comprises receptors (CB1 and CB2 cannabinoid receptors), enzymes (Fatty Acid Amide Hydrolase [FAAH], which synthesizes the endocannabinoid anandamide), as well as the anandamide membrane transporter (AMT). Importantly, previous experiments have demonstrated that the endocannabinoid system modulates multiple neurobiological functions, including sleep. For instance, SR141716A (the CB1 cannabinoid receptor antagonist) as well as URB597 (the FAAH inhibitor) increase waking in rats whereas VDM-11 (the blocker of the AMT) enhances sleep in rodents...
December 17, 2016: Neuroscience
https://www.readbyqxmd.com/read/27737792/effects-of-alprazolam-and-cannabinoid-related-compounds-in-an-animal-model-of-panic-attack
#4
Luara A Batista, Andrea S Haibara, Luiz C Schenberg, Fabricio A Moreira
Selective stimulation of carotid chemoreceptors by intravenous infusion of low doses of potassium cyanide (KCN) produces short-lasting escape responses that have been proposed as a model of panic attack. In turn, preclinical studies suggest that facilitation of the endocannabinoid system attenuate panic-like responses. Here, we compared the effects of cannabinoid-related compounds to those of alprazolam, a clinically effective panicolytic, on the duration of the escape reaction induced by intravenous infusion of KCN (80μg) in rats...
October 11, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27737789/chronic-stress-leads-to-epigenetic-dysregulation-in-the-neuropeptide-y-and-cannabinoid-cb1-receptor-genes-in-the-mouse-cingulate-cortex
#5
Ermelinda Lomazzo, Florian König, Leila Abassi, Ruth Jelinek, Beat Lutz
Persistent stress triggers a variety of mechanisms, which may ultimately lead to the occurrence of anxiety- and depression-related disorders. Epigenetic modifications represent a mechanism by which chronic stress mediates long-term effects. Here, we analyzed brain tissue from mice exposed to chronic unpredictable stress (CUS), which induced impaired emotional and nociceptive behaviors. As endocannabinoid (eCB) and neuropeptide-Y (Npy) systems modulate emotional processes, we hypothesized that CUS may affect these systems through epigenetic mechanisms...
October 11, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27737788/chronic-faah-inhibition-during-nicotine-abstinence-alters-habenular-cb1-receptor-activity-and-precipitates-depressive-like-behaviors
#6
A Simonnet, E Zamberletti, M Cador, T Rubino, S Caillé
The role of the endocannabinoid system in nicotine addiction is being increasingly acknowledged. Acute inhibition of anandamide (AEA) degradation efficiently reduces nicotine withdrawal-induced affective symptoms in rats and fatty acid amide hydrolase (FAAH), the degradation enzyme of AEA, has been proposed as a possible treatment against nicotine addiction. However, it is unclear whether chronic inhibition of AEA during nicotine abstinence will have beneficial or deleterious affective side-effects. Using a rat model of nicotine addiction, we found that, during abstinence, rats injected daily with a FAAH inhibitor (URB597) developed a depressive-like phenotype...
October 11, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27659731/parabens-inhibit-fatty-acid-amide-hydrolase-a-potential-role-in-paraben-enhanced-3t3-l1-adipocyte-differentiation
#7
Sean D Kodani, Haley B Overby, Christophe Morisseau, Jiangang Chen, Ling Zhao, Bruce D Hammock
Parabens are a class of small molecules that are regularly used as preservatives in a variety of personal care products. Several parabens, including butylparaben and benzylparaben, have been found to interfere with endocrine signaling and to stimulate adipocyte differentiation. We hypothesized these biological effects could be due to interference with the endocannabinoid system and identified fatty acid amide hydrolase (FAAH) as the direct molecular target of parabens. FAAH inhibition by parabens yields mixed-type and time-independent kinetics...
November 16, 2016: Toxicology Letters
https://www.readbyqxmd.com/read/27567396/endocannabinoids-inhibit-neurogenic-inflammation-in-murine-joints-by-a-non-canonical-cannabinoid-receptor-mechanism
#8
Eugene Krustev, Milind M Muley, Jason J McDougall
Neurogenic inflammation is a local inflammatory response that is driven by the peripheral release of neuropeptides from small diameter afferents which occurs in many organs including joints. The knee joint has a rich endocannabinoid system which has been shown to decrease acute synovitis. The aim of this study was to investigate the influence of joint afferents on leukocyte-endothelial interactions within the synovial microcirculation of mice and determine the role of endocannabinoids on this inflammatory response...
August 22, 2016: Neuropeptides
https://www.readbyqxmd.com/read/27553121/emotional-arousal-state-influences-the-ability-of-amygdalar-endocannabinoid-signaling-to-modulate-anxiety
#9
Maria Morena, Kira D Leitl, Haley A Vecchiarelli, J Megan Gray, Patrizia Campolongo, Matthew N Hill
Systemic activation of cannabinoid receptors often induces biphasic effects on emotional memory and anxiety depending on the levels of emotional arousal associated to the experimental context. The basolateral nucleus of the amygdala (BLA) represents a crucial structure for the ability of endocannabinoid (eCB) signaling to modulate emotional behaviour, and receives dense projections from brainstem arousal system nuclei. We examined whether changes in emotional arousal state would influence the ability of acute eCB manipulations within the BLA to modulate anxiety...
December 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27441413/involvement-of-endocannabinoid-neurotransmission-in-the-bed-nucleus-of-stria-terminalis-in-cardiovascular-responses-to-acute-restraint-stress-in-rats
#10
Lucas Gomes-de-Souza, Leandro A Oliveira, Ricardo Benini, Patrícia Rodella, Willian Costa-Ferreira, Carlos C Crestani
BACKGROUND AND PURPOSE: Endocannabinoid signalling has been reported as an important neurochemical mechanism involved in responses to stress. Previous studies provided evidence of endocannabinoid release in the bed nucleus of the stria terminalis (BNST) during aversive stimuli. Nevertheless, a possible involvement of this neurochemical mechanism in stress responses has never been evaluated. Therefore, in the present study we investigated the involvement of BNST endocannabinoid neurotransmission, acting via local CB1 receptors, in the cardiovascular responses to acute restraint stress in rats...
October 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27424778/cannabinoid-receptor-agonist-win55-212-2-and-fatty-acid-amide-hydrolase-inhibitor-urb597-may-protect-against-cognitive-impairment-in-rats-of-chronic-cerebral-hypoperfusion-via-pi3k-akt-signaling
#11
Shao-Hua Su, Yue-Qing Wang, Yi-Fang Wu, Da-Peng Wang, Qi Lin, Jian Hai
The present study further investigated the protective effects of cannabinoid receptor agonist WIN55,212-2 (WIN) and fatty acid amide hydrolase (FAAH) inhibitor URB597 (URB) on chronic cerebral hypoperfusion (CCH)-induced cognitive impairment in rats. Spatial learning and memory were assessed with the Morris water maze and by measuring Long-term potentiation. The expression of microtubule-associated protein-2 (MAP)-2, growth-associated protein-43 (GAP)-43, synaptophysin, cannabinoid receptor 1 (CB1), brain-derived neurotrophic factor (BDNF), FAAH, N-acylphosphatidylethanolamine phospholipase D(NAPE-PLD) and monoacyl glycerol lipase (MGL) as well as phosphoinositide 3-kinase (PI3K)/AKT signaling pathway molecules and downstream targets including AKT, phosphorylated (p-)AKT, cyclic AMP response element- binding protein (CREB), p-CREB, Bcl-2-associated death protein (BAD), p-BAD, glycogen synthase kinase (GSK)-3β, p-GSK-3β, forkhead box protein (FOXO) 3A and p-FOXO3A was determined by western blotting...
October 15, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27404450/quantitative-proteomics-analysis-of-zebrafish-exposed-to-sub-lethal-dosages-of-%C3%AE-methyl-amino-l-alanine-bmaa
#12
Ann Kristin Frøyset, Essa Ahsan Khan, Kari Espolin Fladmark
The non-protein amino acid β-methylamino-L-alanine (BMAA) is a neurotoxin present in microalgae and shown to accumulate in the food web. BMAA has been linked to the complex neurodegenerative disorder of Guam and to increased incidents sporadic ALS. Two main neurotoxic routes are suggested; an excitotoxic by acting as an agonist towards glutamate receptors and a metabolic by misincorporating into cellular proteins. We have used zebrafish, an increasingly used model for neurodegenerative diseases, to further identify signaling components involved in BMAA-induced toxicity...
2016: Scientific Reports
https://www.readbyqxmd.com/read/27318096/fatty-acid-amide-hydrolase-inhibition-for-the-symptomatic-relief-of-parkinson-s-disease
#13
Marta Celorrio, Diana Fernández-Suárez, Estefanía Rojo-Bustamante, Víctor Echeverry-Alzate, María J Ramírez, Cecilia J Hillard, José A López-Moreno, Rafael Maldonado, Julen Oyarzábal, Rafael Franco, María S Aymerich
Elements of the endocannabinoid system are strongly expressed in the basal ganglia where they suffer profound rearrangements after dopamine depletion. Modulation of the levels of the endocannabinoid 2-arachidonoyl-glycerol by inhibiting monoacylglycerol lipase alters glial phenotypes and provides neuroprotection in a mouse model of Parkinson's disease. In this study, we assessed whether inhibiting fatty acid amide hydrolase could also provide beneficial effects on the time course of this disease. The fatty acid amide hydrolase inhibitor, URB597, was administered chronically to mice treated with 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine and probenecid (MPTPp) over 5weeks...
October 2016: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/27307500/discriminative-stimulus-properties-of-the-endocannabinoid-catabolic-enzyme-inhibitor-sa-57-in-mice
#14
Robert A Owens, Bogna Ignatowska-Jankowska, Mohammed Mustafa, Patrick M Beardsley, Jenny L Wiley, Abdulmajeed Jali, Dana E Selley, Micah J Niphakis, Benjamin F Cravatt, Aron H Lichtman
Whereas the inhibition of fatty acid amide hydrolase (FAAH) or monoacylglycerol lipase (MAGL), the respective major hydrolytic enzymes of N-arachidonoyl ethanolamine (AEA) and 2-arachidonoylglycerol (2-AG), elicits no or partial substitution for Δ(9)-tetrahydrocannabinol (THC) in drug-discrimination procedures, combined inhibition of both enzymes fully substitutes for THC, as well as produces a constellation of cannabimimetic effects. The present study tested whether C57BL/6J mice would learn to discriminate the dual FAAH-MAGL inhibitor SA-57 (4-[2-(4-chlorophenyl)ethyl]-1-piperidinecarboxylic acid 2-(methylamino)-2-oxoethyl ester) from vehicle in the drug-discrimination paradigm...
August 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27154553/dissociating-the-role-of-endocannabinoids-in-the-pleasurable-and-motivational-properties-of-social-play-behaviour-in-rats
#15
E J Marijke Achterberg, Maaike M H van Swieten, Nina V Driel, Viviana Trezza, Louk J M J Vanderschuren
Social play behaviour is a vigorous form of social interaction, abundant during the juvenile and adolescent phases of life in many mammalian species, including humans. Social play is highly rewarding and it is important for social and cognitive development. Being a rewarding activity, social play can be dissociated in its pleasurable and motivational components. We have previously shown that endocannabinoids modulate the expression of social play behaviour in rats. In the present study, we investigated whether endocannabinoids modulate the motivational and pleasurable properties of social play behaviour, using operant and place conditioning paradigms, respectively...
August 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27150075/urb597-inhibits-oxidative-stress-induced-by-alcohol-binging-in-the-prefrontal-cortex-of-adolescent-rats
#16
Renan Pelição, Matheus C Santos, Leandro C Freitas-Lima, Silvana S Meyrelles, Elisardo C Vasquez, Ester M Nakamura-Palacios, Lívia C M Rodrigues
Heavy episodic drinking (binging), which is highly prevalent among teenagers, results in oxidative damage. Because the prefrontal cortex (PFC) is not completely mature in adolescents, this brain region may be more vulnerable to the effects of alcohol during adolescence. As endocannabinoids may protect the immature PFC from the harmful effects of high doses of alcohol, this study investigated the effect of the fatty acid amide hydrolase (FAAH) inhibitor URB597 on oxidative stress induced by acute or chronic binge alcohol intake in adolescent rats...
June 15, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27117424/design-synthesis-and-biological-evaluation-of-potent-faah-inhibitors
#17
Wei Tuo, Natascha Leleu-Chavain, Amélie Barczyk, Nicolas Renault, Lucas Lemaire, Philippe Chavatte, Régis Millet
A new series of 3-carboxamido-5-aryl-isoxazoles was designed, synthesized and evaluated for their biological activity. Different pharmacomodulations have been explored and the lipophilicity of these compounds was assessed. Investigation of the in vitro biological activity led to the identification of 5 compounds as potent FAAH inhibitors, their good FAAH inhibition capacity is probably correlated with their suitable lipophilicity. Specifically, compound 25 showed similar inhibition potency against FAAH in comparison with URB597, one of the most potent FAAH inhibitor known to date...
June 1, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27091613/distinct-neuronal-activation-patterns-are-associated-with-pcp-induced-social-withdrawal-and-its-reversal-by-the-endocannabinoid-enhancing-drug-urb597
#18
Julien Matricon, Alexandre Seillier, Andrea Giuffrida
The fatty acid amide hydrolase inhibitor, URB597, an endocannabinoid enhancing drug, reverses social withdrawal in the sub-chronic PCP rat model of schizophrenia, but reduces social interaction (SI) in controls. To identify the anatomical substrates associated with PCP-induced social withdrawal and the contrasting effects of URB597 on SI in PCP- versus saline-treated rats, we analyzed SI-induced c-Fos expression in 28 brain areas relevant to schizophrenia and/or social behavior following vehicle or URB597 administration...
September 2016: Neuroscience Research
https://www.readbyqxmd.com/read/27086176/crosstalk-between-liver-antioxidant-and-the-endocannabinoid-systems-after-chronic-administration-of-the-faah-inhibitor-urb597-to-hypertensive-rats
#19
Michał Biernacki, Wojciech Łuczaj, Agnieszka Gęgotek, Marek Toczek, Katarzyna Bielawska, Elżbieta Skrzydlewska
Hypertension is accompanied by perturbations to the endocannabinoid and antioxidant systems. Thus, potential pharmacological treatments for hypertension should be examined as modulators of these two metabolic systems. The aim of this study was to evaluate the effects of chronic administration of the fatty acid amide hydrolase (FAAH) inhibitor [3-(3-carbamoylphenyl)phenyl]N-cyclohexylcarbamate (URB597) on the endocannabinoid system and on the redox balance in the livers of DOCA-salt hypertensive rats. Hypertension caused an increase in the levels of endocannabinoids [anandamide (AEA), 2-arachidonoyl-glycerol (2-AG) and N-arachidonoyl-dopamine (NADA)] and CB1 receptor and the activities of FAAH and monoacylglycerol lipase (MAGL)...
June 15, 2016: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/26969765/protective-role-of-cannabinoid-cb1-receptors-and-vascular-effects-of-chronic-administration-of-faah-inhibitor-urb597-in-doca-salt-hypertensive-rats
#20
Marta Baranowska-Kuczko, Hanna Kozłowska, Monika Kloza, Olga Karpińska, Marek Toczek, Ewa Harasim, Irena Kasacka, Barbara Malinowska
AIMS: This study examined whether the fall in blood pressure (BP) induced by the chronic inhibition of fatty acid amide hydrolase (FAAH) by URB597 in deoxycorticosterone acetate (DOCA-salt) hypertensive rats correlates with endocannabinoid-mediated vascular changes. MAIN METHODS: Functional studies were performed in isolated endothelium-intact aortas and small mesenteric arteries (sMAs) using organ bath technique and wire myography, respectively. KEY FINDINGS: In the DOCA-salt rats, methanandamide-stimulated relaxation was enhanced in sMAs or diminished in aortas...
April 15, 2016: Life Sciences
keyword
keyword
63335
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"