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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
#1
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/28433484/corrigendum-to-biological-characterization-of-pm226-a-chromenoisoxazole-as-a-selective-cb2-receptor-agonist-with-neuroprotective-profile-pharmacol-res-110-august-2016-2016-205-215
#2
M Gómez-Cañas, P Morales, L García-Toscano, C Navarrete, E Muñoz, N Jagerovic, J Fernández-Ruiz, M García-Arencibia, M R Pazos
No abstract text is available yet for this article.
April 19, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28431968/cannabinoid-cb1-and-cb2-receptors-differentially-modulate-l-and-t-type-ca-2-channels-in-rat-retinal-ganglion-cells
#3
Wen-Jing Qian, Ning Yin, Feng Gao, Yanying Miao, Qian Li, Fang Li, Xing-Huai Sun, Xiong-Li Yang, Zhongfeng Wang
Endocannabinoid signaling system is involved in regulating multiple neuronal functions in the central nervous system by activating G-protein coupled cannabinoid CB1 and CB2 receptors (CB1Rs and CB2Rs). Growing evidence has shown that CB1Rs and CB2Rs are extensively expressed in retinal ganglion cells (RGCs). Here, modulation of L- and T-types Ca(2+) channels by activating CB1Rs and CB2Rs in RGCs was investigated. Triple immunofluorescent staining showed that L-type subunit CaV1.2 was co-localized with T-type subunits (CaV3...
April 18, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28428264/cb1-cannabinoid-receptor-drives-oocyte-maturation-and-embryo-development-via-pi3k-akt-and-mapk-pathways
#4
Angela Patricia López-Cardona, Serafín Pérez-Cerezales, Raúl Fernández-González, Ricardo Laguna-Barraza, Eva Pericuesta, Naiara Agirregoitia, Alfonso Gutiérrez-Adán, Ekaitz Agirregoitia
Endocannabinoids have been recognized as mediators of practically all reproductive events in mammals. However, little is known about the role of this system in oocyte maturation. In a mouse model, we observed that activation of the cannabinoid receptor (CB)1 during in vitro oocyte maturation modulated the phosphorylation status of Akt and ERK1/2 and enhanced the subsequent embryo production. In the absence of the CB1 receptor, in vivo oocyte maturation was impaired and embryo development delayed. The CB2 receptor was unable to rescue these effects...
April 20, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28425013/cannabinoids-as-modulators-of-cell-death-clinical-applications-and-future-directions
#5
B M Fonseca, N A Teixeira, G Correia-da-Silva
Endocannabinoids are bioactive lipids that modulate various physiological processes through G-protein-coupled receptors (CB1 and CB2) and other putative targets. By sharing the activation of the same receptors, some phytocannabinoids and a multitude of synthetic cannabinoids mimic the effects of endocannabinoids. In recent years, a growing interest has been dedicated to the study of cannabinoids properties for their analgesic, antioxidant, anti-inflammatory and neuroprotective effects. In addition to these well-recognized effects, various studies suggest that cannabinoids may affect cell survival, cell proliferation or cell death...
April 20, 2017: Reviews of Physiology, Biochemistry and Pharmacology
https://www.readbyqxmd.com/read/28412921/synthetic-cannabinoids-psychopharmacology-clinical-aspects-and-psy-chotic-onset
#6
Giovanni Martinotti, Rita Santacroce, Duccio Papanti, Yasmine Elgharably, Mariya Prilutskaya, Ornella Corazza
Synthetic Cannabinoids (SC) are the widest and most diffused class of Novel Psychoactive Substances. SC are chemically heterogeneous and structurally dissimilar from delta-9-tetrahydrocannabinol, being full agonists of the endocannabinoid system receptors CB1 and CB2. Desired effects include euphoria, talkativeness, feelings of joy and laughter, relaxation. With respect to cannabis, SC intake may also be associated with quicker arise of the effects, shorter duration of action, and larger levels of hangover...
April 13, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28392296/anxious-behavior-induces-elevated-hippocampal-cb2-receptor-gene-expression
#7
James M Robertson, Justin K Achua, Justin P Smith, Melissa A Prince, Clarissa D Staton, Patrick J Ronan, Tangi R Summers, Cliff H Summers
Anxiety is differentially expressed across a continuum of stressful/fearful intensity, influenced endocannabinoid systems and receptors. The hippocampus plays important roles in the regulation of affective behavior, emotion, and anxiety, as well as memory. Location of Cb1/Cb2 receptor action could be important in determining emotional valence, because while the dorsal hippocampus is involved in spatial memory and cognition, the ventral hippocampus has projections to the PFC, BNST, amygdala, and HPA axis, and is important for emotional responses to stress...
April 7, 2017: Neuroscience
https://www.readbyqxmd.com/read/28386998/metabolic-syndrome-induced-bladder-cannabinoid-receptor-changes-in-the-fructose-fed-rats
#8
I-Hung Chen, Juei-Tang Cheng, Yat-Ching Tong
OBJECTIVES: To investigate the effect of metabolic syndrome on the bladder cannabinoid receptors 1 and 2 (CB1/CB2) expression and function in the fructose-fed rats (FR). METHODS: Adult male Sprague-Dawley rats were divided into two groups: (i) Control rats fed with normal chow; and (ii) Rats fed with high-fructose diet (FR) for 9 weeks. The body weight, blood pressure, plasma sugar, insulin, triglyceride and cholesterol were measured. Bladder muscle strips were prepared in organ bath and pre-contracted with 1 µM/L acetylcholine (ACh) or 50 mM/L KCl...
April 6, 2017: Lower Urinary Tract Symptoms
https://www.readbyqxmd.com/read/28374590/binding-site-characterization-of-am1336-a-novel-covalent-inverse-agonist-at-human-cannabinoid-2-receptor-using-mass-spectrometric-analysis
#9
Srikrishnan Mallipeddi, Simion Kreimer, Nikolai Zvonok, V Kiran Vemuri, Barry L Karger, Alexander R Ivanov, Alexandros Makriyannis
Cannabinoid 2 receptor (CB2R), a Class A G-protein coupled receptor (GPCR), is a promising drug target in a wide array of pathological conditions. Rational drug design has been hindered due to our poor understanding of the structural features involved in ligand binding. Binding of a high-affinity biarylpyrazole inverse agonist AM1336 to a library of the human CB2 receptor (hCB2R) cysteine-substituted mutants provided indirect evidence that two cysteines in transmembrane helix-7 (H7) were critical for the covalent attachment...
April 4, 2017: Journal of Proteome Research
https://www.readbyqxmd.com/read/28373843/antihyperalgesic-activities-of-endocannabinoids-in-a-mouse-model-of-antiretroviral-induced-neuropathic-pain
#10
Neha Munawar, Mabayoje A Oriowo, Willias Masocha
Background: Nucleoside reverse transcriptase inhibitors (NRTIs) are the cornerstone of the antiretroviral therapy for human immunodeficiency virus/acquired immune deficiency syndrome (HIV/AIDS). However, their use is sometimes limited by the development of a painful sensory neuropathy, which does not respond well to drugs. Smoked cannabis has been reported in clinical trials to have efficacy in relieving painful HIV-associated sensory neuropathy. Objectives: The aim of this study was to evaluate whether the expression of endocannabinoid system molecules is altered during NRTI-induced painful neuropathy, and also whether endocannabinoids can attenuate NRTI-induced painful neuropathy...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28368293/-%C3%AE-caryophyllene-a-cb2-receptor-selective-phytocannabinoid-suppresses-motor-paralysis-and-neuroinflammation-in-a-murine-model-of-multiple-sclerosis
#11
Thaís Barbosa Alberti, Wagner Luiz Ramos Barbosa, José Luiz Fernandes Vieira, Nádia Rezende Barbosa Raposo, Rafael Cypriano Dutra
(-)-β-caryophyllene (BCP), a cannabinoid receptor type 2 (CB2)-selective phytocannabinoid, has already been shown in precedent literature to exhibit both anti-inflammatory and analgesic effects in mouse models of inflammatory and neuropathic pain. Herein, we endeavored to investigate the therapeutic potential of BCP on experimental autoimmune encephalomyelitis (EAE), a murine model of multiple sclerosis (MS). Furthermore, we sought to demonstrate some of the mechanisms that underlie the modulation BCP exerts on autoimmune activated T cells, the pro-inflammatory scenery of the central nervous system (CNS), and demyelination...
April 1, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28364261/regulation-of-cell-surface-cb2-receptor-during-human-b-cell-activation-and-differentiation
#12
Julie T Castaneda, Airi Harui, Michael D Roth
Cannabinoid receptor type 2 (CB2) is the primary receptor pathway mediating the immunologic consequences of cannabinoids. We recently reported that human peripheral blood B cells express CB2 on both the extracellular membrane and at intracellular sites, where-as monocytes and T cells only express intracellular CB2. To better understand the pattern of CB2 expression by human B cells, we examined CD20(+) B cells from three tissue sources. Both surface and intracellular expression were present and uniform in cord blood B cells, where all cells exhibited a naïve mature phenotype (IgD(+)/CD38(Dim))...
March 31, 2017: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/28356120/in-vivo-tspo-and-cannabinoid-receptor-type-2-availability-early-in-post-stroke-neuroinflammation-in-rats-a-positron-emission-tomography-study
#13
Teruyo Hosoya, Dai Fukumoto, Takeharu Kakiuchi, Shingo Nishiyama, Shigeyuki Yamamoto, Hiroyuki Ohba, Hideo Tsukada, Takatoshi Ueki, Kohji Sato, Yasuomi Ouchi
BACKGROUND: Upregulated levels of 18-kDa translocator proteins (TSPO) and type 2 endocannabinoid receptors (CB2) are considered to reflect different aspects of microglia-related neuroinflammatory responses in the brain. Relative to the increase in the TSPO expression that occurs slightly later during neuroinflammation in a proinflammatory fashion, CB2 activation is considered to relate to the neuroprotective responses that occurs predominantly at an early stage of brain disorders. These findings, however, were deduced from studies with different animal samples under different experimental settings...
March 29, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28348424/immunohistochemistry-detected-and-localized-cannabinoid-receptor-type-2-in-bovine-fetal-pancreas-at-late-gestation
#14
Cecilia Dall'Aglio, Angela Polisca, Maria Grazia Cappai, Francesca Mercati, Alessandro Troisi, Carolina Pirino, Paola Scocco, Margherita Maranesi
At present, data on the endocannabinoid system expression and distribution in the pancreatic gland appear scarce and controversial as descriptions are limited to humans and laboratory animals. Since the bovine pancreas is very similar to the human in endocrine portion development and control, studies on the fetal gland could prove to be very interesting, as an abnormal maternal condition during late pregnancy may be a predisposing trigger for adult metabolic disorders. The present investigation studied cannabinoid receptor type 2 presence and distribution in the bovine fetal pancreas towards the end of gestation...
March 7, 2017: European Journal of Histochemistry: EJH
https://www.readbyqxmd.com/read/28348416/cannabinoid-cb2-receptors-are-involved-in-the-protection-of-raw264-7-macrophages-against-the-oxidative-stress-an-in-vitro-study
#15
Sabrina Giacoppo, Agnese Gugliandolo, Oriana Trubiani, Federica Pollastro, Gianpaolo Grassi, Placido Bramanti, Emanuela Mazzon
Research in the last decades has widely investigated the anti-oxidant properties of natural products as a therapeutic approach for the prevention and the treatment of oxidative-stress related disorders. In this context, several studies were aimed to evaluate the therapeutic potential of phytocannabinoids, the bioactive compounds of Cannabis sativa. Here, we examined the anti-oxidant ability of Cannabigerol (CBG), a non-psychotropic cannabinoid, still little known, into counteracting the hydrogen peroxide (H2O2)-induced oxidative stress in murine RAW264...
January 23, 2017: European Journal of Histochemistry: EJH
https://www.readbyqxmd.com/read/28336953/palmitoylethanolamide-induces-microglia-changes-associated-with-increased-migration-and-phagocytic-activity-involvement-of-the-cb2-receptor
#16
F Guida, L Luongo, S Boccella, M E Giordano, R Romano, G Bellini, I Manzo, A Furiano, A Rizzo, R Imperatore, F A Iannotti, E D'Aniello, F Piscitelli, F Sca Rossi, L Cristino, V Di Marzo, V de Novellis, S Maione
The endogenous fatty acid amide palmitoylethanolamide (PEA) has been shown to exert anti-inflammatory actions mainly through inhibition of the release of pro-inflammatory molecules from mast cells, monocytes and macrophages. Indirect activation of the endocannabinoid (eCB) system is among the several mechanisms of action that have been proposed to underlie the different effects of PEA in vivo. In this study, we used cultured rat microglia and human macrophages to evaluate whether PEA affects eCB signaling. PEA was found to increase CB2 mRNA and protein expression through peroxisome proliferator-activated receptor-α (PPAR-α) activation...
March 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28326930/effects-of-jwh015-in-cytokine-secretion-in-primary-human-keratinocytes-and-fibroblasts-and-its-suitability-for-topical-transdermal-delivery
#17
Alicia Bort, Perla A Alvarado-Vazquez, Carolina Moracho-Vilrriales, Kristopher G Virga, Giuseppe Gumina, Alfonso Romero-Sandoval, Scott Asbill
Background JWH015 is a cannabinoid (CB) receptor type 2 agonist that produces immunomodulatory effects. Since skin cells play a key role in inflammatory conditions and tissue repair, we investigated the ability of JWH015 to promote an anti-inflammatory and pro-wound healing phenotype in human primary skin cells. Methods Human primary keratinocytes and fibroblasts were stimulated with lipopolysaccharide. The mRNA expression of cannabinoid receptors was determined using RT-PCR. The effects of JWH015 (0.05, 0...
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28320859/2-arachidonoylglycerol-ameliorates-inflammatory-stress-induced-insulin-resistance-in-cardiomyocytes
#18
Dipanjan Chanda, Yvonne Oligschlaeger, Ilvy Geraets, Yilin Liu, Xiaoqing Zhu, Jieyi Li, Miranda Nabben, Will Coumans, Joost J F P Luiken, Jan F C Glatz, Dietbert Neumann
Several studies have linked impaired glucose uptake and insulin resistance (IR) to functional impairment of the heart. Recently, endocannabinoids have been implicated in cardiovascular disease. However, the mechanisms involving endocannabinoid signaling, glucose uptake and IR in cardiomyocytes are understudied. Here, we report the endocannabinoid 2-Arachidonoylglycerol (2-AG) via stimulation of cannabinoid type-1 (CB1) receptor and Ca2+/Calmodulin-dependent protein kinase β (CaMKKβ) activates AMPK leading to increased glucose uptake...
March 20, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28315398/hepatic-expression-of-cannabinoid-receptors-cb1-and-cb2-correlate-with-fibrogenesis-in-patients-with-chronic-hepatitis-b
#19
Erhei Dai, Lianshan Zhang, Lihong Ye, Shiqing Wan, Lulu Feng, Qi Qi, Fang Yao, Zhen Li
BACKGROUND: The endocannabinoid system is involved in the pathogenesis of liver fibrosis. However, most of the findings in this area have come from experimental studies in animal models or clinical trials on chronic hepatitis C. The roles of cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2) in hepatofibrosis in patients with chronic hepatitis B (CHB) have not been studied fully. This study aimed to explore the relationship between liver fibrosis and the expression of CB1 and CB2 in patients with CHB...
March 15, 2017: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/28289947/in-vivo-and-in-vitro-identification-of-endocannabinoid-signaling-in-periodontal-tissues-and-their-potential-role-in-local-pathophysiology
#20
Anna Konermann, Andreas Jäger, Stefanie A E Held, P Brossart, Anne Schmöle
The endocannabinoid system (ECS) with its binding receptors CB1 and CB2 impacts multiple pathophysiologies not only limited to neuronal psychoactivity. CB1 is assigned to cerebral neuron action, whereas CB2 is mainly expressed in different non-neuronal tissues and associated with immunosuppressive effects. Based on these tissue-selective CB receptor roles, it was the aim of this study to analyze potential expression in periodontal tissues under physiological conditions and inflammatory states. In vivo, CB receptor expression was investigated on human periodontal biopsies with or without bacterial inflammation and on rat maxillae with or without sterile inflammation...
March 14, 2017: Cellular and Molecular Neurobiology
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