keyword
MENU ▼
Read by QxMD icon Read
search

GPR55

keyword
https://www.readbyqxmd.com/read/28087250/pharmacology-of-cannabinoids-in-the-treatment-of-epilepsy
#1
REVIEW
Tyler E Gaston, Daniel Friedman
The use of cannabis products in the treatment of epilepsy has long been of interest to researchers and clinicians alike; however, until recently very little published data were available to support its use. This article summarizes the available scientific data of pharmacology from human and animal studies on the major cannabinoids which have been of interest in the treatment of epilepsy, including ∆9-tetrahydrocannabinol (∆9-THC), cannabidiol (CBD), ∆9-tetrahydrocannabivarin (∆9-THCV), cannabidivarin (CBDV), and ∆9-tetrahydrocannabinolic acid (Δ9-THCA)...
January 10, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28064014/gpr55-agonist-lysophosphatidylinositol-and-lysophosphatidylcholine-inhibit-endothelial-cell-hyperpolarization-via-gpr-independent-suppression-of-na-ca-2-exchanger-and-endoplasmic-reticulum-ca-2-refilling
#2
Alexander I Bondarenko, Fabrizio Montecucco, Olga Panasiuk, Vadim Sagach, Nataliya Sidoryak, Karim J Brandt, François Mach
Lysophosphatidylinositol (LPI) and lysophosphatidylcholine (LPC) are lipid signaling molecules that induce endothelium-dependent vasodilation. In addition, LPC suppresses acetylcholine (Ach)-induced responses. We aimed to determine the influence of LPC and LPI on hyperpolarizing responses in vitro and in situ endothelial cells (EC) and identify the underlying mechanisms. Using patch-clamp method, we show that LPI and LPC inhibit EC hyperpolarization to histamine and suppress Na(+)/Ca(2+) exchanged (NCX) currents in a concentration-dependent manner...
January 4, 2017: Vascular Pharmacology
https://www.readbyqxmd.com/read/28029647/peptide-guided-targeting-of-gpr55-for-anti-cancer-therapy
#3
Maria Mangini, Enrico Iaccino, Maria Giovanna Mosca, Selena Mimmi, Rosa D'Angelo, Ileana Quinto, Giuseppe Scala, Stefania Mariggiò
Expression of the lysophosphatidylinositol receptor GPR55 correlates with invasive potential of metastatic cells and bone metastasis formation of different types of tumors. These findings suggest a role for GPR55 signaling in cancer progression, including in lymphoproliferative diseases. Here, we screened a M13-phage-displayed random library using the bait of HEK293 cells that heterologously expressed full-length HA-GPR55. We selected a set of phagotopes that carried 7-mer insert peptides flanked by a pair of cysteine residues, which resulted in cyclized peptides...
December 23, 2016: Oncotarget
https://www.readbyqxmd.com/read/28005346/identification-of-crucial-amino-acid-residues-involved-in-agonist-signaling-at-the-gpr55-receptor
#4
Mary A Lingerfelt, Pingwei Zhao, Haleli P Sharir, Dow P Hurst, Patricia H Reggio, Mary E Abood
GPR55 is a newly deorphanized class A G-protein-coupled receptor that has been implicated in inflammatory pain, neuropathic pain, metabolic disorder, bone development, and cancer. Few potent GPR55 ligands have been identified to date. This is largely due to an absence of information about salient features of GPR55, such as residues important for signaling and residues implicated in the GPR55 signaling cascade. The goal of this work was to identify residues that are key for the signaling of the GPR55 endogenous ligand, l-α-lysophosphatidylinositol (LPI), as well as the signaling of the GPR55 agonist, ML184 {CID 2440433, 3-[4-(2,3-dimethylphenyl)piperazine-1-carbonyl]-N,N-dimethyl-4-pyrrolidin-1-ylbenzenesulfonamide}...
January 11, 2017: Biochemistry
https://www.readbyqxmd.com/read/27941994/deletion-of-gpr55-results-in-subtle-effects-on-energy-metabolism-motor-activity-and-thermal-pain-sensation
#5
Mikael Bjursell, Erik Ryberg, Tingting Wu, Peter J Greasley, Mohammad Bohlooly-Y, Stephan Hjorth
The G-protein coupled receptor 55 (GPR55) is activated by cannabinoids and non-cannabinoid molecules and has been speculated to play a modulatory role in a large variety of physiological and pathological processes, including in metabolically perturbed states. We therefore generated male mice deficient in the gene coding for the cannabinoid/lysophosphatidylinositol (LPI) receptor Gpr55 and characterized them under normal dietary conditions as well as during high energy dense diet feeding followed by challenge with the CB1 receptor antagonist/GPR55 agonist rimonabant...
2016: PloS One
https://www.readbyqxmd.com/read/27890711/the-endogenous-lipid-n-arachidonoyl-glycine-is-hypotensive-and-nitric-oxide-cgmp-dependent-vasorelaxant
#6
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 (1mg/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 (3mg/kg)...
January 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27835801/cannabinoid-receptor-ligand-bias-implications-in-the-central-nervous-system
#7
REVIEW
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
https://www.readbyqxmd.com/read/27677765/metabolic-effects-of-orally-administered-small-molecule-agonists-of-gpr55-and-gpr119-in-multiple-low-dose-streptozotocin-induced-diabetic-and-incretin-receptor-knockout-mice
#8
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
https://www.readbyqxmd.com/read/27607913/development-of-novel-ligands-for-peptide-gpcrs
#9
REVIEW
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)...
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27597829/cb2-and-gpr55-receptors-as-therapeutic-targets-for-systemic-immune-dysregulation
#10
REVIEW
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
https://www.readbyqxmd.com/read/27567474/lipid-mediators-involved-in-the-oxidative-stress-and-antioxidant-defence-of-human-lung-cancer-cells
#11
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
https://www.readbyqxmd.com/read/27561953/gpr55-dependent-stimulation-of-insulin-secretion-from-isolated-mouse-and-human-islets-of-langerhans
#12
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
https://www.readbyqxmd.com/read/27561826/the-gastrointestinal-tract-a-central-organ-of-cannabinoid-signaling-in-health-and-disease
#13
REVIEW
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
https://www.readbyqxmd.com/read/27516570/metabolism-of-endocannabinoids
#14
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
https://www.readbyqxmd.com/read/27488130/advances-in-the-physiology-of-gpr55-in-the-central-nervous
#15
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
https://www.readbyqxmd.com/read/27486335/endocannabinoid-system-as-a-regulator-of-tumor-cell-malignancy-biological-pathways-and-clinical-significance
#16
REVIEW
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
https://www.readbyqxmd.com/read/27485069/scotopic-vision-in-the-monkey-is-modulated-by-the-g-protein-coupled-receptor-55
#17
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
https://www.readbyqxmd.com/read/27465665/treatment-with-the-gpr55-antagonist-cid16020046-increases-neutrophil-activation-in-mouse-atherogenesis
#18
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
https://www.readbyqxmd.com/read/27429655/pharmacological-evaluation-of-synthetic-cannabinoids-identified-as-constituents-of-spice
#19
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
https://www.readbyqxmd.com/read/27423937/selective-gpr55-antagonism-reduces-chemoresistance-in-cancer-cells
#20
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
keyword
keyword
11049
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"