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URB597

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https://www.readbyqxmd.com/read/28526975/lipid-nanoparticles-for-administration-of-poorly-water-soluble-neuroactive-drugs
#1
Elisabetta Esposito, Markus Drechsler, Paolo Mariani, Federica Carducci, Michela Servadio, Francesca Melancia, Patrizia Ratano, Patrizia Campolongo, Viviana Trezza, Rita Cortesi, Claudio Nastruzzi
This study describes the potential of solid lipid nanoparticles and nanostructured lipid carriers as nano-formulations to administer to the central nervous system poorly water soluble drugs. Different neuroactive drugs, i.e. dimethylfumarate, retinyl palmitate, progesterone and the endocannabinoid hydrolysis inhibitor URB597 have been studied. Lipid nanoparticles constituted of tristearin or tristearin in association with gliceryl monoolein were produced. The nanoencapsulation strategy allowed to obtain biocompatible and non-toxic vehicles, able to increase the solubility of the considered neuroactive drugs...
September 2017: Biomedical Microdevices
https://www.readbyqxmd.com/read/28501776/inhibition-of-senp3-by-urb597-ameliorates-neurovascular-unit-dysfunction-in-rats-with-chronic-cerebral-hypoperfusion
#2
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...
May 11, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28446875/cannabinoid-modulation-of-memory-consolidation-in-rats-beyond-the-role-of-cannabinoid-receptor-subtype-1
#3
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
#4
Anna Pedzinska-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 blood pressure (BP) in spontaneously hypertensive rats (SHR) partially through normalization of cardiac contractile function. Here, we examined whether the potential hypotensive effect of chronic FAAH inhibition by URB597 in hypertensive rats correlates with changes in cardiac performance. EXPERIMENTAL APPROACH: Experiments were performed using perfused hearts and left atria isolated from 8-10 week old SHR, age-matched deoxycorticosterone acetate (DOCA-salt) rats and normotensive controls chronically treated with URB597 (1 mg kg(-1) ) or vehicle...
April 24, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28404744/the-role-of-cb1-in-intestinal-permeability-and-inflammation
#5
Mustafa A Karwad, Daniel G Couch, Elena Theophilidou, Sarir Sarmad, David A Barrett, Michael Larvin, Karen L Wright, Jonathan N Lund, Saoirse E O'Sullivan
The endocannabinoid system has previously been shown to play a role in the permeability and inflammatory response of the human gut. The goal of our study was to determine the effects of endogenous anandamide (AEA) and 2-arachidonoyl glycerol (2-AG) on the permeability and inflammatory response of intestinal epithelium under normal, inflammatory, and hypoxic conditions. Human intestinal mucosa was modeled using Caco-2 cells. Human tissue was collected from planned colorectal resections. Accumulation of AEA and 2-AG was achieved by inhibiting their metabolizing enzymes URB597 (a fatty acid amide hydrolase inhibitor) and JZL184 (a monoacylglycerol lipase inhibitor)...
April 12, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28356298/activation-of-cb1-receptors-by-2-arachidonoylglycerol-attenuates-vasoconstriction-induced-by-u46619-and-angiotensin-ii-in-human-and-rat-pulmonary-arteries
#6
Olga Karpińska, Marta Baranowska-Kuczko, Monika Kloza, Ewa Ambrożewicz, Tomasz Kozłowski, Irena Kasacka, Barbara Malinowska, Hanna Kozłowska
Recent evidence suggests that endocannabinoids acting via cannabinoid CB1 receptors may modulate vascular responses of various vasoconstrictors in the rodent systemic vasculature. The aim of the study was to investigate whether endocannabinoids modulate the contractile responses evoked by a thromboxane A2 analog (U46619), angiotensin II (Ang II), serotonin (5-HT) and phenylephrine which stimulate distinct Gq/11-protein coupled receptors (TP, AT1, 5-HT2 and α1-adrenergic) in isolated endothelium-intact human (hPAs) and rat pulmonary arteries (rPAs)...
March 29, 2017: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/28192082/endocannabinoid-dependent-protection-against-kainic-acid-induced-long-term-alteration-of-brain-oscillations-in-guinea-pigs
#7
Liubov Shubina, Rubin Aliev, Valentina Kitchigina
Changes in rhythmic activity can serve as early biomarkers of pathological alterations, but it remains unclear how different types of rhythmic activity are altered during neurodegenerative processes. Glutamatergic neurotoxicity, evoked by kainic acid (KA), causes hyperexcitation and acute seizures that result in delayed brain damage. We employed wide frequency range (0.1-300Hz) local field potential recordings in guinea pigs to study the oscillatory activity of the hippocampus, entorhinal cortex, medial septum, and amygdala in healthy animals for three months after KA introduction...
April 15, 2017: Brain Research
https://www.readbyqxmd.com/read/28157650/urb597-reduces-biochemical-behavioral-and-morphological-alterations-in-two-neurotoxic-models-in-rats
#8
Marisol Maya-López, Hipolito A Ruiz-Contreras, María de Jesús Negrete-Ruíz, Julián Elías Martínez-Sánchez, Juan Benítez-Valenzuela, Ana Laura Colín-González, Juana Villeda-Hernández, Laura Sánchez-Chapul, Carmen Parra-Cid, Edgar Rangel-López, Abel Santamaría
BACKGROUND: URB597 is a compound largely linked to the inhibition of fatty acid amide hydrolase (FAAH), an enzyme responsible for the metabolic degradation of the endocannabinoid anandamide (AEA). Despite this pharmacological property accounts for its modulatory profile demonstrated in some neurotoxic paradigms, the possible protective properties of this agent have been poorly investigated, and deserve exploration in different neurotoxic models. In this study, we explored the effects of URB597 on oxidative damage to lipids and other major endpoints of toxicity in two neurotoxic models in vivo in rats (the first one produced by the mitochondrial neurotoxin 3-nitropropionic acid [3-NP], and the other generated by the striatal injection of the pro-oxidant toxin 6-hydroxidopamine [6-OHDA]) in order to provide further supporting evidence of its modulatory profile...
April 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28104279/effect-of-inhibition-of-fatty-acid-amide-hydrolase-on-mptp-induced-dopaminergic-neuronal-damage
#9
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/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
#10
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...
May 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28042028/urb597-improves-cognitive-impairment-induced-by-chronic-cerebral-hypoperfusion-by-inhibiting-mtor-dependent-autophagy
#11
Dapeng Wang, Qi Lin, Shaohua Su, Kejia Liu, Yifang Wu, Jian Hai
Chronic cerebral hypoperfusion (CCH) is associated with various ischemic cerebrovascular diseases that are characterized by cognitive impairment. The role of autophagy in cognitive dysfunction under conditions of CCH is poorly understood. To address this issue, the present study investigated the effect of the fatty acid amide hydrolase (FAAH) inhibitor URB597 on autophagy and cognition in a CCH model as well as the underlying mechanisms. Cognitive function was evaluated with the Morris water maze and by assessing long-term potentiation (LTP)...
March 6, 2017: Neuroscience
https://www.readbyqxmd.com/read/27889577/brain-uptake-and-metabolism-of-the-endocannabinoid-anandamide-labeled-in-either-the-arachidonoyl-or-ethanolamine-moiety
#12
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
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
#13
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)...
January 6, 2017: Neuroscience
https://www.readbyqxmd.com/read/27746343/revealing-the-role-of-the-endocannabinoid-system-modulators-sr141716a-urb597-and-vdm-11-in-sleep-homeostasis
#14
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
#15
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
#16
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...
February 2017: Neuropharmacology
https://www.readbyqxmd.com/read/27737788/chronic-faah-inhibition-during-nicotine-abstinence-alters-habenular-cb1-receptor-activity-and-precipitates-depressive-like-behaviors
#17
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...
February 2017: Neuropharmacology
https://www.readbyqxmd.com/read/27659731/parabens-inhibit-fatty-acid-amide-hydrolase-a-potential-role-in-paraben-enhanced-3t3-l1-adipocyte-differentiation
#18
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
#19
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
#20
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
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