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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 (1 mg/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 (3 mg/kg)...
November 24, 2016: European Journal of Pharmacology
Robert B Laprairie, Amina M Bagher, Eileen M Denovan-Wright
The G protein-coupled cannabinoid receptors CB1, CB2, GPR18, and GPR55 regulate neurotransmission, pain, and inflammation and have been intensively investigated as potential drug targets. Each of these GPCRs is coupled to multiple effector proteins mediating divergent cellular signals. The ligand bias of cannabinoid-targeted compounds is only beginning to be quantified. Research into cannabinoid bias is now revealing correlations between bias in cell culture and functional outcomes in vivo. We present an example study of cannabinoid bias in the context of Huntington disease...
November 8, 2016: Current Opinion in Pharmacology
Aine M McKillop, Brian M Moran, Yasser H A Abdel-Wahab, Noella M Gormley, Peter R Flatt
AIMS/HYPOTHESIS: Abnormal cannabidiol (Abn-CBD) and AS-1269574 are potent selective agonists for GPR55 and GPR119, respectively. The present study evaluated the actions and ability of these small-molecule agonists to counteract experimental diabetes in mice. METHODS: Diabetes was induced in NIH Swiss mice by five consecutive daily intraperitoneal injections of 40 mg/(kg body weight) streptozotocin. Diabetic mice received daily oral administration of Abn-CBD or AS-1269574 (0...
September 27, 2016: Diabetologia
Brian M Moran, Aine M McKillop, Finbarr Pm O'Harte
Incretin based glucagon-like peptide-1 receptor (GLP-1R) agonists which target a G-protein coupled receptor (GPCR) are currently used in the treatment of type 2 diabetes. This review focuses on GPCRs from pancreatic β-cells, including GLP-1, glucose-dependent insulinotropic polypeptide (GIP), glucagon, somatostatin, pancreatic polypeptide (PP), cholecystokinin (CCK), peptide YY (PYY), oxyntomodulin (OXM) and ghrelin receptors. In addition, fatty acids GPCRs are thought to have an increasing role in regulating peptide secretions namely short fatty acids GPCR (GPR41, GPR43), medium chain fatty acid GPCR (GPR84), long chain fatty acid GPCR (GPR40, GPR120) and cannabinoid-like GPCR (GPR55, GPR119)...
September 5, 2016: Current Opinion in Pharmacology
Juan Zhou, Ian Burkovskiy, Hyewon Yang, Joel Sardinha, Christian Lehmann
The endocannabinoid system (ECS) is involved in many physiological processes and has been suggested to play a critical role in the immune response and the central nervous system (CNS). Therefore, ECS modulation has potential therapeutic effects on immune dysfunctional disorders, such as sepsis and CNS injury-induced immunodeficiency syndrome (CIDS). In sepsis, excessive release of pro- and anti-inflammatory mediators results in multi-organ dysfunction, failure, and death. In CIDS, an acute CNS injury dysregulates a normally well-balanced interplay between CNS and the immune system, leading to increased patients' susceptibility to infections...
2016: Frontiers in Pharmacology
Agnieszka Gęgotek, Jacek Nikliński, Neven Žarković, Kamelija Žarković, Georg Waeg, Wojciech Łuczaj, Radosław Charkiewicz, Elżbieta Skrzydlewska
BACKGROUND: The oxidative modifications of bioactive macromolecules have important roles in carcinogenesis. Of particular interest are lipid peroxidation products, which are involved in the activation of Nrf2 and endocannabinoids that affect cancer progression. METHODS: In lung cancer tissues (squamous cell lung carcinoma - SCC and adenocarcinoma - AC), the glutathione peroxidase and catalase activity and glutathione level, together with the expression of Nrf2 and its activators/inhibitors were estimated...
August 20, 2016: Redox Biology
Bo Liu, Shuang Song, Inmaculada Ruz-Maldonado, Attilio Pingitore, Guo C Huang, David Baker, Peter M Jones, Shanta J Persaud
AIMS: The novel cannabinoid receptor GPR55 is expressed by rodent islets and it has been implicated in β-cell function in response to a range of ligands. This study evaluated the effects of GPR55 ligands on intracellular calcium ([Ca(2+) ]i ) levels and insulin secretion from islets isolated from GPR55 knockout (GPR55 (-/-) ) mice, age-matched wildtype (WT) mice and human pancreas. MATERIALS AND METHODS: GPR55 expression was determined by Western blotting and fluorescent immunohistochemistry...
December 2016: Diabetes, Obesity & Metabolism
C Hasenoehrl, U Taschler, M Storr, R Schicho
BACKGROUND: In ancient medicine, extracts of the marijuana plant Cannabis sativa were used against diseases of the gastrointestinal (GI) tract. Today, our knowledge of the ingredients of the Cannabis plant has remarkably advanced enabling us to use a variety of herbal and synthetic cannabinoid (CB) compounds to study the endocannabinoid system (ECS), a physiologic entity that controls tissue homeostasis with the help of endogenously produced CBs and their receptors. After many anecdotal reports suggested beneficial effects of Cannabis in GI disorders, it was not surprising to discover that the GI tract accommodates and expresses all the components of the ECS...
December 2016: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
Michał Biernacki, Elżbieta Skrzydlewska
Endocannabinoids belong to a group of ester, ether and amide derivatives of fatty acids, which are endogenous ligands of receptors CB1, CB2, TRPV1 and GPR55 that are included in the endocannabinoid system of the animal organism. The best known endocannabinoids are: N-arachidonylethanolamide called anandamide (AEA) and 2-arachidonoylglycerol (2-AG). They occur in all organisms, and their highest level is observed in the brain. In this review the mechanisms of synthesis and degradation of both AEA and 2-AG are shown...
2016: Postȩpy Higieny i Medycyny Doświadczalnej
Bruno A Marichal-Cancino, Alfonso Fajardo-Valdéz, Alejandra E Ruiz-Contreras, Mónica Méndez-Díaz, Oscar Prospéro-García
The G protein-coupled receptor 55 (GPR55) is a mammalian orphan receptor whose functions in the central nervous system (CNS) have been scarcely elucidated. Several endogenous lipids (cannabinoids and non-cannabinoid) may activate GPR55; these facts have raised a discussion about its nature as a putative cannabinoid receptor. Lysophosphatidylinositol (LPI) is a non-endocannabinoid lipid with activity as a full and potent agonist of GPR55. Beyond this controversy, it is known the endocannabinoid system and GPR55 are highly related both in anatomical localization and function...
July 29, 2016: Current Neuropharmacology
Maria Pyszniak, Jacek Tabarkiewicz, Jarogniew J Łuszczki
The endocannabinoid system (ECS) comprises cannabinoid receptors (CBs), endogenous cannabinoids, and enzymes responsible for their synthesis, transport, and degradation of (endo)cannabinoids. To date, two CBs, CB1 and CB2, have been characterized; however, orphan G-protein-coupled receptor GPR55 has been suggested to be the third putative CB. Several different types of cancer present abnormal expression of CBs, as well as other components of ECS, and this has been shown to correlate with the clinical outcome...
2016: OncoTargets and Therapy
Joseph Bouskila, Vanessa Harrar, Pasha Javadi, Christian Casanova, Yoshio Hirabayashi, Ichiro Matsuo, Jyunpei Ohyama, Jean-François Bouchard, Maurice Ptito
The endogenous cannabinoid system plays important roles in the retina of mice and monkeys via their classic CB1 and CB2 receptors. We have previously reported that the G protein-coupled receptor 55 (GPR55), a putative cannabinoid receptor, is exclusively expressed in rod photoreceptors in the monkey retina, suggesting its possible role in scotopic vision. To test this hypothesis, we recorded full-field electroretinograms (ERGs) after the intravitreal injection of the GPR55 agonist lysophosphatidylglucoside (LPG) or the selective GPR55 antagonist CID16020046 (CID), under light- and dark-adapted conditions...
January 2016: Visual Neuroscience
Fabrizio Montecucco, Alexander I Bondarenko, Sébastien Lenglet, Fabienne Burger, Fabiana Piscitelli, Federico Carbone, Aline Roth, Luca Liberale, Franco Dallegri, Karim J Brandt, Rodrigo A Fraga-Silva, Nikolaos Stergiopulos, Vincenzo Di Marzo, François Mach
Endocannabinoids modulate atherogenesis by triggering different receptors. Recently, orphan G protein-coupled receptors (GPRs) were suggested to be activated by endocannabinoids, possibly regulating vasorelaxation. Here, we investigated whether GPR55 antagonism with CID16020046 would impact on atherosclerotic size and inflammation in two mouse models of early and more advanced atherogenesis. Eleven-week old ApoE-/- mice were fed either a normal diet ([ND] for 16 weeks) or a high-cholesterol diet ([HD] for 11 weeks), resulting in different degrees of hypercholesterolaemia and size of atherosclerosis...
July 28, 2016: Thrombosis and Haemostasis
Cornelius Hess, Clara T Schoeder, Thanigaimalai Pillaiyar, Burkhard Madea, Christa E Müller
In recent years, many synthetic cannabinoid (CB) receptor agonists have appeared on the market as constituents of herbal incense mixtures known as "spice". Contrary to the declared use, they are perorally consumed as a replacement for marijuana to get "high". In many cases, detailed information on the physicochemical and pharmacological properties of the synthetic compounds found in spice preparations is lacking. We have now evaluated a large series of heterocyclic compounds, 1,3-disubstituted indole and 2-azaindole derivatives known or assumed to be CB1 receptor agonists, many of which have previously been identified in forensic samples...
2016: Forensic Toxicology
Nagendra S Singh, Michel Bernier, Irving W Wainer
G protein-coupled receptor 55 (GPR55) possesses pro-oncogenic activity and its function can be competitively inhibited with (R,R')-4'-methoxy-1-naphthylfenoterol (MNF) through poorly defined signaling pathways. Here, the anti-tumorigenic effect of MNF was investigated in the human pancreatic cancer cell line, PANC-1, by focusing on the expression of known cancer biomarkers and the expression and function of multidrug resistance (MDR) exporters such as P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP)...
September 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Mellar P Davis
Cannabinoids bind not only to classical receptors (CB1 and CB2) but also to certain orphan receptors (GPR55 and GPR119), ion channels (transient receptor potential vanilloid), and peroxisome proliferator-activated receptors. Cannabinoids are known to modulate a multitude of monoamine receptors. Structurally, there are 3 groups of cannabinoids. Multiple studies, most of which are of moderate to low quality, demonstrate that tetrahydrocannabinol (THC) and oromucosal cannabinoid combinations of THC and cannabidiol (CBD) modestly reduce cancer pain...
July 2016: Journal of the National Comprehensive Cancer Network: JNCCN
Clara Andradas, Sandra Blasco-Benito, Sonia Castillo-Lluva, Patricia Dillenburg-Pilla, Rebeca Diez-Alarcia, Alba Juanes-García, Elena García-Taboada, Rodrigo Hernando-Llorente, Joaquim Soriano, Sigrid Hamann, Antonia Wenners, Ibrahim Alkatout, Wolfram Klapper, Christoph Rocken, Maret Bauer, Norbert Arnold, Miguel Quintanilla, Diego Megías, Miguel Vicente-Manzanares, Leyre Urigüen, J Silvio Gutkind, Manuel Guzmán, Eduardo Pérez-Gómez, Cristina Sánchez
The orphan G protein-coupled receptor GPR55 has been directly or indirectly related to basic alterations that drive malignant growth: uncontrolled cancer cell proliferation, sustained angiogenesis, and cancer cell adhesion and migration. However, little is known about the involvement of this receptor in metastasis. Here, we show that elevated GPR55 expression in human tumors is associated with the aggressive basal/triple-negative breast cancer population, higher probability to develop metastases, and therefore poor patient prognosis...
June 21, 2016: Oncotarget
Natalia Malek, Magdalena Kostrzewa, Wioletta Makuch, Agnieszka Pajak, Mateusz Kucharczyk, Fabiana Piscitelli, Barbara Przewlocka, Vincenzo Di Marzo, Katarzyna Starowicz
There is considerable evidence to support the role of anandamide (AEA), an endogenous ligand of cannabinoid receptors, in neuropathic pain modulation. AEA also produces effects mediated by other biological targets, of which the transient receptor potential vanilloid type 1 (TRPV1) has been the most investigated. Both, inhibition of AEA breakdown by fatty acid amide hydrolase (FAAH) and blockage of TRPV1 have been shown to produce anti-nociceptive effects. Recent research suggests the usefulness of dual-action compounds, which may afford greater anti-allodynic efficacy...
September 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Sharon Anavi-Goffer, Ruth A Ross
AlphaScreen(®) SureFire(®) assay is a novel technology that combines luminescent oxygen channeling technology, nano-beads, and monocloncal antibodies to detect the level of a selected protein in a volume lower than 5 μl. This method is more sensitive compared with the traditional enzyme-linked immunosorbent assays (ELISA), and can detect an increasing number of new targets. Here, we described a method for AlphaScreen(®) SureFire(®) assay that targets ERK1/2 phosphorylation, a primary downstream signaling pathway that conveys activation of GPR55 by L-α-lysophosphatidylinositol (LPI) and certain cannabinoids...
2016: Methods in Molecular Biology
Christopher M Henstridge, Andrew J Brown, Maria Waldhoer
Since the discovery of the lysophospholipid-sensitive receptor GPR55, hopes have been raised that targeting this G protein-coupled receptor (GPCR) may represent a novel approach for the treatment of metabolic disorders. We discuss conflicting evidence surrounding GPR55 physiology and highlight its potential as a novel target for the treatment of obesity and diabetes.
September 2016: Trends in Endocrinology and Metabolism: TEM
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