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https://www.readbyqxmd.com/read/29787777/examination-of-the-effects-of-cannabinoid-ligands-on-decision-making-in-a-rat-gambling-task
#1
Jacqueline-Marie N Ferland, Madison Carr, Angela M Lee, Myrthe E Hoogeland, Catharine A Winstanley, Tommy Pattij
Although exposure to delta-9-tetrahydrocannabinol (THC) is perceived to be relatively harmless, mounting evidence has begun to show that it is associated with a variety of cognitive deficits, including poor decision making. THC-induced impairments in decision making are thought to be the result of cannabinoid CB1 receptor activation, and although clinical literature suggests that chronic activation via THC contributes to perturbations in decision making, acute CB1 receptor modulation has yielded mixed results...
May 19, 2018: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29621749/the-endocannabinoid-system-affects-myocardial-glucose-metabolism-in-the-doca-salt-model-of-hypertension
#2
Agnieszka Polak, Ewa Harasim-Symbor, Barbara Malinowska, Irena Kasacka, Alicja Lewandowska, Adrian Chabowski
BACKGROUND/AIMS: Recent interest in the use of cannabinoids as therapeutic agents has revealed the involvement of the endogenous cannabinoid system (ECS) in the regulation of the cardiovascular system in hypertension. Abnormalities in glucose metabolism and insulin action are commonly detected in hypertensive animals. Thus, potential antihypertensive drugs should be investigated with respect to modulation of glucose homeostasis. Therefore, the aim of the present study was to evaluate the effects of the ECS activation after chronic fatty acid amide hydrolase inhibitor (URB597) administration on plasma glucose and insulin concentrations as well as parameters of myocardial glucose metabolism in the deoxycorticosterone acetate (DOCA)-salt hypertensive rats, an animal model of secondary hypertension...
2018: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29562280/the-use-of-cannabinoids-in-colitis-a-systematic-review-and-meta-analysis
#3
Daniel G Couch, Henry Maudslay, Brett Doleman, Jonathan N Lund, Saoirse E O'Sullivan
Background: Clinical trials investigating the use of cannabinoid drugs for the treatment of intestinal inflammation are anticipated secondary to preclinical literature demonstrating efficacy in reducing inflammation. Methods: We systematically reviewed publications on the benefit of drugs targeting the endo-cannabinoid system in intestinal inflammation. We collated studies examining outcomes for meta-analysis from EMBASE, MEDLINE and Pubmed until March 2017. Quality was assessed according to mSTAIR and SRYCLE score...
March 19, 2018: Inflammatory Bowel Diseases
https://www.readbyqxmd.com/read/29531281/author-correction-the-faah-inhibitor-urb597-suppresses-hippocampal-maximal-dentate-afterdischarges-and-restores-seizure-induced-impairment-of-short-and-long-term-synaptic-plasticity
#4
Roberto Colangeli, Massimo Pierucci, Arcangelo Benigno, Giuseppe Campiani, Stefania Butini, Giuseppe Di Giovanni
A correction to this article has been published and is linked from the HTML and PDF versions of this paper. The error has been fixed in the paper.
March 12, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29519609/chronic-treatment-with-urb597-ameliorates-post-stress-symptoms-in-a-rat-model-of-ptsd
#5
Sharon Fidelman, Tomer Mizrachi Zer-Aviv, Rachel Lange, Cecilia J Hillard, Irit Akirav
Activating the endocannabinoid system has become a major focus in the search for novel therapeutics for anxiety and deficits in fear extinction, two defining features of PTSD. We examined whether chronic treatment with the fatty acid amide hydrolase (FAAH) inhibitor URB597 (0.2, 0.3, 0.4 mg/kg, i.p.) or the CB1/2 receptor agonist WIN55,212-2 (0.25, 0.5 mg/kg, i.p.) injected for 3 weeks to rats exposed to the shock and reminders model of PTSD would attenuate post-stress symptoms and affect basolateral amygdala (BLA) and CA1 CB1 receptors...
May 2018: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29504066/anticonvulsive-effects-of-endocannabinoids-an-investigation-to-determine-the-role-of-regulatory-components-of-endocannabinoid-metabolism-in-the-pentylenetetrazol-induced-tonic-clonic-seizures
#6
Parisa Zareie, Mehdi Sadegh, Mohammad Reza Palizvan, Homeira Moradi-Chameh
2-Arachidonoylglycerol (2-AG) and anandamide are two major endocannabinoids produced, released and eliminated by metabolic pathways. Anticonvulsive effect of 2-AG and CB1 receptor is well-established. Herein, we designed to investigate the anticonvulsive influence of key components of the 2-AG and anandamide metabolism. Tonic-clonic seizures were induced by an injection of Pentylenetetrazol (80 mg/kg, i.p.) in adult male Wistar rats. Delay and duration for the seizure stages were considered for analysis. Monoacylglycerol lipase blocker (JJKK048; 1 mg/kg) or alpha/beta hydroxylase domain 6 blocker (WWL70; 5 mg/kg) were administrated alone or with 2-AG to evaluate the anticonvulsive potential of these enzymes...
June 2018: Metabolic Brain Disease
https://www.readbyqxmd.com/read/29458190/cannabinoids-prevent-depressive-like-symptoms-and-alterations-in-bdnf-expression-in-a-rat-model-of-ptsd
#7
Or Burstein, Noa Shoshan, Ravid Doron, Irit Akirav
Posttraumatic stress disorder (PTSD) is a debilitating condition highly comorbid with depression. The endocannabinoid (eCB) system and brain-derived neurotrophic factor (BDNF) are suggestively involved in both disorders. We examined whether cannabinoids can prevent the long-term depressive-like symptoms induced by exposure to the shock and situational reminders (SRs) model of PTSD. The CB1/2 receptor agonist WIN55,212-2 (0.5 mg/kg; i.p.), the fatty acid hydrolase (FAAH) inhibitor URB597 (0.3 mg/kg, i.p...
June 8, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29408178/characterization-of-fatty-acid-amide-hydrolase-activity-by-a-fluorescence-based-assay
#8
Florian M Dato, Andreas Maaßen, Bernd Goldfuß, Markus Pietsch
Fatty acid amide hydrolase (FAAH) is involved in many human diseases, particularly cancer, pain and inflammation as well as neurological, metabolic and cardiovascular disorders. Therefore, FAAH is an attractive target for the development of low-molecular-weight inhibitors as therapeutics, which requires robust assays that can be used for high-throughput screening (HTS) of compound libraries. Here, we report the development of a fluorometric assay based on FAAH's ability to effectively hydrolyze medium-chain fatty acid amides, introducing N-decanoyl-substituted 5-amino-2-methoxypyridine (D-MAP) as new amide substrate...
April 1, 2018: Analytical Biochemistry
https://www.readbyqxmd.com/read/29364174/molecular-understanding-of-the-activation-of-cb1-and-blockade-of-trpv1-receptors-implications-for-novel-treatment-strategies-in-osteoarthritis
#9
Jakub Mlost, Magdalena Kostrzewa, Natalia Malek, Katarzyna Starowicz
Osteoarthritis (OA) is a joint disease in which cartilage degenerates as a result of mechanical and biochemical changes. The main OA symptom is chronic pain involving both peripheral and central mechanisms of nociceptive processing. Our previous studies have implicated the benefits of dual- over single-acting compounds interacting with the endocannabinoid system (ECS) in OA treatment. In the present study, we focused on the specific molecular alterations associated with pharmacological treatment. OA was induced in Wistar rats by intra-articular injection of 3 mg of monoiodoacetate (MIA)...
January 24, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29329382/adolescent-synthetic-cannabinoid-exposure-produces-enduring-changes-in-dopamine-neuron-activity-in-a-rodent-model-of-schizophrenia-susceptibility
#10
David D Aguilar, Andrea Giuffrida, Daniel J Lodge
Background: Epidemiological studies recognize cannabis intake as a risk factor for schizophrenia, yet the majority of adolescents who use marijuana do not develop psychosis. Similarly, the abuse of synthetic cannabinoids poses a risk for psychosis. For these reasons, it is imperative to understand the effects of adolescent cannabinoid exposure in susceptible individuals. Methods: We recently developed a novel rodent model of schizophrenia susceptibility, the F2 methylazoxymethanol acetate rat, where only a proportion (~40%) of rats display a schizophrenia-like phenotype...
April 1, 2018: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29285108/elevation-of-arachidonoylethanolamide-levels-by-activation-of-the-endocannabinoid-system-protects-against-colitis-and-ameliorates-remote-organ-lesions-in-mice
#11
Xiaolin Zhao, Peng Liang, Jin Liu, Haixia Jiang, Xiaoshuai Fan, Guo Chen, Cheng Zhou
The endocannabinoid system (ECS) is a potential pharmaceutical target for the treatment of inflammatory bowel diseases (IBDs). The aim of this study was to explore the effects of activation of the ECS on IBD and the associated neural inflammation-induced disruption of the blood-brain barrier (BBB). In a mouse model of trinitrobenzene sulfonic acid-induced colitis, the inhibition of fatty acid amide hydrolase with URB597 elevated the arachidonoylethanolamide concentration of the colon. Macroscopic alterations of the colons were evaluated, and the 7-day survival rate of mice was analyzed...
December 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29197803/redox-system-and-phospholipid-metabolism-in-the-kidney-of-hypertensive-rats-after-faah-inhibitor-urb597-administration
#12
Michał Biernacki, Ewa Ambrożewicz, Agnieszka Gęgotek, Marek Toczek, Katarzyna Bielawska, Elżbieta Skrzydlewska
Primary and secondary hypertension is associated with kidney redox imbalance resulting in enhanced reactive oxygen species (ROS) and enzymes dependent phospholipid metabolism. The fatty acid amide hydrolase inhibitor, URB597, modulates the levels of endocannabinoids, particularly of anandamide, which is responsible for controlling blood pressure and regulating redox balance. Therefore, this study aimed to compare the effects of chronic URB597 administration to spontaneously hypertensive rats (SHR) and rats with secondary hypertension (DOCA-salt rats) on the kidney metabolism associated with the redox and endocannabinoid systems...
May 2018: Redox Biology
https://www.readbyqxmd.com/read/29186065/binge-alcohol-exposure-transiently-changes-the-endocannabinoid-system-a-potential-target-to-prevent-alcohol-induced-neurodegeneration
#13
Daniel J Liput, James R Pauly, Audra L Stinchcomb, Kimberly Nixon
Excessive alcohol consumption leads to neurodegeneration, which contributes to cognitive decline that is associated with alcohol use disorders (AUDs). The endocannabinoid system has been implicated in the development of AUDs, but little is known about how the neurotoxic effects of alcohol impact the endocannabinoid system. Therefore, the current study investigated the effects of neurotoxic, binge-like alcohol exposure on components of the endocannabinoid system and related N-acylethanolamines (NAEs), and then evaluated the efficacy of fatty acid amide hydrolase (FAAH) inhibition on attenuating alcohol-induced neurodegeneration...
November 29, 2017: Brain Sciences
https://www.readbyqxmd.com/read/29169961/the-cannabinoid-transporter-inhibitor-omdm-2-reduces-social-interaction-further-evidence-for-transporter-mediated-endocannabinoid-release
#14
Alexandre Seillier, Andrea Giuffrida
Experimental evidence suggests that the transport of endocannabinoids might work bi-directionally. Accordingly, it is possible that pharmacological blockade of the latter affects not only the re-uptake, but also the release of endocannabinoids, thus preventing them from stimulating CB1 receptors. We used biochemical, pharmacological, and behavioral approaches to investigate the effects of the transporter inhibitor OMDM-2 on social interaction, a behavioral assay that requires activation of CB1 receptors. The underlying mechanisms of OMDM-2 were compared with those of the Fatty Acid Amide Hydrolase (FAAH) inhibitor URB597...
March 1, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29156899/modulating-the-endocannabinoid-pathway-as-treatment-for-peripheral-neuropathic-pain-a-selected-review-of-preclinical-studies
#15
Shannon O'Hearn, Patrick Diaz, Bo Angela Wan, Carlo DeAngelis, Nicholas Lao, Leila Malek, Edward Chow, Alexia Blake
Chemotherapy-induced neuropathic pain is a distressing and commonly occurring side effect of many commonly used chemotherapeutic agents, which in some cases may prevent cancer patients from being able to complete their treatment. Cannabinoid based therapies have the potential to manage or even prevent pain associated with this syndrome. Pre-clinical animal studies that investigate the modulation of the endocannabinoid system (endogenous cannabinoid pathway) are being conducted to better understand the mechanisms behind this phenomenon...
December 2017: Annals of Palliative Medicine
https://www.readbyqxmd.com/read/29071769/inhibition-of-fatty-acid-amide-hydrolase-in-the-central-amygdala-alleviates-co-morbid-expression-of-innate-anxiety-and-excessive-alcohol-intake
#16
Serena Stopponi, Yannick Fotio, Ana Domi, Anna Maria Borruto, Luis Natividad, Marisa Roberto, Roberto Ciccocioppo, Nazzareno Cannella
Fatty acid amide hydrolase (FAAH) is an enzyme that prominently degrades the major endocannabinoid N-arachidonoylethanolamine (anandamide). Inhibition of this enzyme leads to increased anandamide levels in brain regions that modulate stress and anxiety. Recently, we found that genetically selected Marchigian Sardinian alcohol-preferring (msP) rats display hyperactive FAAH in amygdalar regions that was associated with increased stress sensitivity and a hyper-anxious phenotype. Our previous work has also demonstrated that msPs display an innate preference for and excessive consumption of alcohol, potentially reflecting a form of self-medication to gain relief from hyper-anxious states...
October 26, 2017: Addiction Biology
https://www.readbyqxmd.com/read/29038048/the-influence-of-doca-salt-hypertension-and-chronic-administration-of-the-faah-inhibitor-urb597-on-k-ca-2-3-k-ca-3-1-edh-type-relaxation-in-rat-small-mesenteric-arteries
#17
Monika Kloza, Marta Baranowska-Kuczko, Barbara Malinowska, Olga Karpińska, Ewa Harasim-Symbor, Irena Kasacka, Hanna Kozłowska
The aim of this study was to examine the influence of deoxycorticosterone acetate-salt (DOCA-salt) hypertension and chronic treatment with the fatty acid amide hydrolase inhibitor, URB597, on small and intermediate conductance calcium-activated potassium channels and endothelium-dependent hyperpolarization (KCa 2.3/KCa 3.1-EDH) in rat small mesenteric arteries (sMAs). The EDH-type response was investigated, in endothelium-intact sMAs using a wire myograph, by examining acetylcholine-evoked vasorelaxation in the presence of Nω -nitro-L-arginine methyl ester and indomethacin (inhibitors of nitric oxide synthase and cyclooxygenase, respectively)...
December 2017: Vascular Pharmacology
https://www.readbyqxmd.com/read/28976704/human-serum-albumin-a-modulator-of-cannabinoid-drugs
#18
Loris Leboffe, Alessandra di Masi, Viviana Trezza, Fabio Polticelli, Paolo Ascenzi
The endocannabinoid system is a unique neuromodulatory system that affects a wide range of biological processes and maintains the homeostasis in all mammal body systems. In recent years, several pharmacological tools to target endocannabinoid neurotransmission have been developed, including direct and indirect cannabinoid agonists and cannabinoid antagonists. Due to their hydrophobic nature, cannabinoid agonists and antagonists need to bind specific transporters to allow their distribution in body fluids. Human serum albumin (HSA), the most abundant plasma protein, is a key determinant of drug pharmacokinetics...
November 2017: IUBMB Life
https://www.readbyqxmd.com/read/28963903/fatty-acid-amide-hydrolase-inhibitor-urb597-may-protect-against-kainic-acid-induced-damage-to-hippocampal-neurons-dependence-on-the-degree-of-injury
#19
Irina B Mikheeva, Liubov Shubina, Nataliya Matveeva, Luybov L Pavlik, Valentina F Kitchigina
OBJECTIVE: Status epilepticus (SE) provokes changes, which lead to neuronal alterations. Endocannabinoids (eCBs) can affect the neuronal survival during excitotoxicity and brain damage. Using a kainic acid (KA)-induced experimental SE model, we investigated whether cellular changes entail damage to endoplasmic reticulum (ER), mitochondria, and nuclei in hippocampal cells (CA1 field), and whether these alterations can be diminished by treatment with URB597, an inhibitor of eCB enzymatic degradation...
September 22, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/28947487/cannabinoid-cb-1-discrimination-effects-of-endocannabinoids-and-catabolic-enzyme-inhibitors
#20
COMPARATIVE STUDY
Michael Z Leonard, Shakiru O Alapafuja, Lipin Ji, Vidyanand G Shukla, Yingpeng Liu, Spyros P Nikas, Alexandros Makriyannis, Jack Bergman, Brian D Kangas
An improved understanding of the endocannabinoid system has provided new avenues of drug discovery and development toward the management of pain and other behavioral maladies. Exogenous cannabinoid type 1 (CB1 ) receptor agonists such as Δ9 -tetrahydrocannabinol are increasingly used for their medicinal actions; however, their utility is constrained by concern regarding abuse-related subjective effects. This has led to growing interest in the clinical benefit of indirectly enhancing the activity of the highly labile endocannabinoids N -arachidonoylethanolamine [AEA (or anandamide)] and/or 2-arachidonoylglycerol (2-AG) via catabolic enzyme inhibition...
December 2017: Journal of Pharmacology and Experimental Therapeutics
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