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https://read.qxmd.com/read/30738036/increased-expression-of-cannabinoid-cb-2-and-serotonin-5-ht-1a-heteroreceptor-complexes-in-a-model-of-newborn-hypoxic-ischemic-brain-damage
#1
REVIEW
Rafael Franco, María Villa, Paula Morales, Irene Reyes-Resina, Ana Gutiérrez-Rodríguez, Jasmina Jiménez, Nadine Jagerovic, José Martínez-Orgado, Gemma Navarro
Preclinical work shows cannabidiol as a promising drug to manage neonatal hypoxic-ischemic brain damage (NHIBD). The molecular mechanism is not well defined but the beneficial effects of this phytocannabinoid are blocked by antagonists of both cannabinoid CB2 (CB2 R) and serotonin 5-HT1A (5-HT1AR) receptors that, in addition, may form heteromers in a heterologous expression system. Using bioluminescence energy transfer, we have shown a direct interaction of the two receptors that leads to a particular signaling in a heterologous system...
February 6, 2019: Neuropharmacology
https://read.qxmd.com/read/30733293/therapeutic-targeting-of-her2-cb-2-r-heteromers-in-her2-positive-breast-cancer
#2
Sandra Blasco-Benito, Estefanía Moreno, Marta Seijo-Vila, Isabel Tundidor, Clara Andradas, María M Caffarel, Miriam Caro-Villalobos, Leyre Urigüen, Rebeca Diez-Alarcia, Gema Moreno-Bueno, Lucía Hernández, Luis Manso, Patricia Homar-Ruano, Peter J McCormick, Lucka Bibic, Cristina Bernadó-Morales, Joaquín Arribas, Meritxell Canals, Vicent Casadó, Enric I Canela, Manuel Guzmán, Eduardo Pérez-Gómez, Cristina Sánchez
Although human epidermal growth factor receptor 2 (HER2)-targeted therapies have dramatically improved the clinical outcome of HER2-positive breast cancer patients, innate and acquired resistance remains an important clinical challenge. New therapeutic approaches and diagnostic tools for identification, stratification, and treatment of patients at higher risk of resistance and recurrence are therefore warranted. Here, we unveil a mechanism controlling the oncogenic activity of HER2: heteromerization with the cannabinoid receptor CB2 R...
February 7, 2019: Proceedings of the National Academy of Sciences of the United States of America
https://read.qxmd.com/read/30702341/cannabinoids-and-bone-regeneration
#3
Dragos Apostu, Ondine Lucaciu, Alexandru Mester, Horea Benea, Daniel Oltean-Dan, Florin Onisor, Mihaela Baciut, Simion Bran
Bone is a complex tissue of the with unique properties such as high strength and regeneration capabilities while carrying out multiple functions. Bone regeneration occurs both in physiological situations (bone turnover) and pathological situations (e.g. fractures), being performed by osteoblasts and osteoclasts. If this process is inadequate, fracture nonunion or aseptic loosening of implants occurs and requires a complex treatment. Exogenous factors are currently used to increase bone regeneration process when needed, such as bisphosphonates and vitamin D, but limitations do exist...
January 31, 2019: Drug Metabolism Reviews
https://read.qxmd.com/read/30624864/expression-and-preparation-of-a-g-protein-coupled-cannabinoid-receptor-cb-2-for-nmr-structural-studies
#4
Alexei Yeliseev
Cannabinoid receptor type II, or CB2 , is an integral membrane protein that belongs to a large class of G-protein-coupled receptors (GPCR)s. CB2 is a part of the endocannabinoid system, which plays an important role in the regulation of immune response, inflammation, and pain. Information about the structure and function of CB2 is essential for the development of specific ligands targeting this receptor. We present here a methodology for recombinant expression of CB2 and its stable isotope labeling, purification, and reconstitution into liposomes, in preparation for its characterization by nuclear magnetic resonance (NMR)...
January 9, 2019: Current Protocols in Protein Science
https://read.qxmd.com/read/30611802/progress-in-brain-cannabinoid-cb-2-receptor-research-from-genes-to-behavior
#5
REVIEW
Chloe J Jordan, Zheng-Xiong Xi
The type 2 cannabinoid receptor (CB2R) was initially regarded as a peripheral cannabinoid receptor. However, recent technological advances in gene detection, alongside the availability of transgenic mouse lines, indicate that CB2Rs are expressed in both neurons and glial cells in the brain under physiological and pathological conditions, and are involved in multiple functions at cellular and behavioral levels. Brain CB2Rs are inducible and neuroprotective via up-regulation in response to various insults, but display species differences in gene and receptor structures, CB2R expression, and receptor responses to various CB2R ligands...
January 3, 2019: Neuroscience and Biobehavioral Reviews
https://read.qxmd.com/read/30605489/increased-von-willebrand-factor-parameters-in-children-with-febrile-seizures
#6
Astrid Pechmann, Sven Wellmann, Benjamin Stoecklin, Marcus Krüger, Barbara Zieger
INTRODUCTION: Primary blood coagulation and wound sealing are orchestrated by von Willebrand factor (VWF), a large multimeric glycoprotein. Upon release of arginine vasopressin (AVP), VWF containing high molecular weight multimers is secreted. By measuring copeptin, the C-terminal part of the AVP prohormone, we recently found strongly increased AVP levels in children with febrile seizures (FS) as compared to children with fever but without seizures. It is unknown if increased AVP levels in FS are of any biological function...
2019: PloS One
https://read.qxmd.com/read/30591150/n-3-polyunsaturated-n-acylethanolamines-are-cb-2-cannabinoid-receptor-preferring-endocannabinoids
#7
Nahed Alharthi, Peter Christensen, Wafa Hourani, Catherine Ortori, David A Barrett, Andrew J Bennett, Victoria Chapman, Stephen P H Alexander
Anandamide, the first identified endogenous cannabinoid and TRPV1 agonist, is one of a series of endogenous N-acylethanolamines, NAEs. We have generated novel assays to quantify the levels of multiple NAEs in biological tissues and their rates of hydrolysis through fatty acid amide hydrolase. This range of NAEs was also tested in rapid response assays of CB1 , CB2 cannabinoid and TRPV1 receptors. The data indicate that PEA, SEA and OEA are not endocannabinoids or endovanilloids, and that the higher endogenous levels of these metabolites compared to polyunsaturated analogues are a correlate of their slow rates of hydrolysis...
November 2018: Biochimica et biophysica acta. Molecular and cell biology of lipids
https://read.qxmd.com/read/30588600/preclinical-evaluation-of-18-f-ma3-a-cb-2-receptor-agonist-radiotracer-for-positron-emission-tomography
#8
Bala Attili, Sofie Celen, Muneer Ahamed, Michel Koole, Chris Van den Haute, Wim Vanduffel, Guy Bormans
BACKGROUND AND PURPOSE: Non-invasive in vivo imaging of CB2 receptors (CB2 R) using positron emission tomography (PET) is pursued to study neuroinflammation. The purpose of this study is to evaluate the in vivo binding specificity of [18 F]MA3, a CB2 R agonist, in a rat model with local overexpression of human CB2 R (hCB2 R). METHODS: [18 F]MA3 was produced with good radiochemical yield and radiochemical purity. The radiotracer was evaluated in rats with local overexpression of hCB2 R and in a healthy non-human primate using PET...
December 27, 2018: British Journal of Pharmacology
https://read.qxmd.com/read/30583970/benzo-d-thiazol-2-3h-ones-as-new-potent-selective-cb-2-agonists-with-anti-inflammatory-properties
#9
Natascha Leleu-Chavain, Davy Baudelet, Valéria Moas Heloire, Diana Escalante Rocha, Nicolas Renault, Amélie Barczyk, Madjid Djouina, Mathilde Body-Malapel, Pascal Carato, Régis Millet
The high distribution of CB2 receptors in immune cells suggests their important role in the control of inflammation. Growing evidence offers this receptor as an attractive therapeutic target: selective CB2 agonists are able to modulate inflammation without triggering psychotropic effects. In this work, we report a new series of selective CB2 agonists based on a benzo[d]thiazol-2(3H)-one scaffold. This drug design project led to the discovery of compound 9, as a very potent CB2 agonist (Ki  = 13.5 nM) with a good selectivity versus CB1 ...
December 13, 2018: European Journal of Medicinal Chemistry
https://read.qxmd.com/read/30500553/cannabinoid-cb-1-and-cb-2-receptors-antagonists-am251-and-am630-differentially-modulate-the-chronotropic-and-inotropic-effects-of-isoprenaline-in-isolated-rat-atria
#10
Jolanta Weresa, Anna Pędzińska-Betiuk, Rafał Kossakowski, Barbara Malinowska
BACKGROUND: Drugs targeting CB1 and CB2 receptors have been suggested to possess therapeutic benefit in cardiovascular disorders associated with elevated sympathetic tone. Limited data suggest cannabinoid ligands interact with postsynaptic β-adrenoceptors. The aim of this study was to examine the effects of CB1 and CB2 antagonists, AM251 and AM630, respectively, at functional cardiac β-adrenoceptors. METHODS: Experiments were carried out in isolated spontaneously beating right atria and paced left atria where inotropic and chronotropic increases were induced by isoprenaline and selective agonists of β1 and β2 -adrenergic receptors...
September 17, 2018: Pharmacological Reports: PR
https://read.qxmd.com/read/30447588/household-solid-fuel-burning-emission-characterization-and-activity-levels-in-india
#11
Shamsh Pervez, Madhuri Verma, Suresh Tiwari, Rajan K Chakrabarty, John G Watson, Judith C Chow, Abhilash S Panicker, Manas Kanti Deb, Mohammad Nahid Siddiqui, Yasmeen Fatima Pervez
Emission factors (EFs) of PM2.5, carbon fractions, major ionic (K+ , Ca2+ , NH4 + , SO4 2- , NO3 - and Cl- ) and elemental (Al, Cr, Cu and Fe) species from combustion of commonly used household solid fuel were determined in 10 different states in India during cooking practices. The study involved sampling during actual household cooking involving use of a variety of fuels including coal balls (CB), fuel wood (FW), dung cakes (DC), crop residues (CR), mixed fuels (MF: dung cakes + fuel woods). Species-wise highest EFs (g·kg-1 ) were: 34...
November 4, 2018: Science of the Total Environment
https://read.qxmd.com/read/30243065/anandamide-inhibits-fc%C3%AE%C2%B5ri-dependent-degranulation-and-cytokine-synthesis-in-mast-cells-through-cb-2-and-gpr55-receptor-activation-possible-involvement-of-cb-2-gpr55-heteromers
#12
Silvia L Cruz, Elizabeth Sánchez-Miranda, Jorge Ivan Castillo-Arellano, Rodolfo Daniel Cervantes-Villagrana, Alfredo Ibarra-Sánchez, Claudia González-Espinosa
Activation of high affinity receptor for IgE (FcεRI) by IgE/antigen complexes in mast cells (MCs) leads to the release of preformed pro-inflammatory mediators stored in granules by a Ca2+ -dependent process known as anaphylactic degranulation. Degranulation inhibition has been proposed as a strategy to control allergies and chronic inflammation conditions. Cannabinoids are important inhibitors of inflammatory reactions but their effects on IgE/Ag-mediated MCs responses are not well described. In this study, we analyzed the effect of the endocannabinoid anandamide (AEA), the selective CB2 receptor agonist HU308, and the GPR55 receptor agonist lysophosphatidylinositol (LPI) on FcεRI-induced activation in murine bone marrow-derived mast cells (BMMCs)...
September 19, 2018: International Immunopharmacology
https://read.qxmd.com/read/30232034/inflammation-and-cb-2-signaling-drive-novel-changes-in-the-ocular-lipidome-and-regulate-immune-cell-activity-in-the-eye
#13
J T Toguri, E Leishman, A M Szczesniak, R B Laprairie, O Oehler, A J Straiker, M E M Kelly, H B Bradshaw
Uveitis is inflammation of the uvea which consists of the iris, ciliary body and the choroid of the eye. Uveitis can lead to impaired vision and is responsible for 10% of all cases of blindness globally. Using an endotoxin-induced uveitis (EIU) rodent model, our previous data implicated the endogenous cannabinoid system (ECS) in the amelioration of many of the components of the inflammatory response. Here, we test the hypothesis that the reduction in inflammatory mediators in the EIU model by the CB2 agonist, HU308, is associated with changes in ECS endogenous ligands as well as related lipids, prostaglandins (PGs), 2-acyl glycerols, and lipoamines...
September 16, 2018: Prostaglandins & Other Lipid Mediators
https://read.qxmd.com/read/30217464/synthesis-of-oxidative-metabolites-of-cra13-and-their-analogs-identification-of-cra13-active-metabolites-and-analogs-thereof-with-selective-cb-2-r-affinity
#14
Ahmed H E Hassan, Min Chang Cho, Hye In Kim, Ji Seul Yang, Kyung Tae Park, Ji Young Hwang, Choon-Gon Jang, Ki Duk Park, Yong Sup Lee
CRA13; a peripheral dual CB1 R/CB2 R agonist with clinically proven analgesic properties, infiltrates into CNS producing adverse effects due to central CB1 R agonism. Such adverse effects might be circumvented by less lipophilic compounds with attenuated CB1 R affinity. Metabolism produces less lipophilic metabolites that might be active metabolites. Some CRA13 oxidative metabolites and their analogues were synthesized as less lipophilic CRA13 analogues. Probing their CB1 R and CB2 R activity revealed the alcohol metabolite 8c as a more potent and more effective CB2 R ligand with attenuated CB1 R affinity relative to CRA13...
September 6, 2018: Bioorganic & Medicinal Chemistry
https://read.qxmd.com/read/30197863/simultaneous-biosynthesis-of-r-acetoin-and-ethylene-glycol-from-d-xylose-through-in-vitro-metabolic-engineering
#15
Xiaojing Jia, Robert M Kelly, Yejun Han
( R )-acetoin is a four-carbon platform compound used as the precursor for synthesizing novel optically active materials. Ethylene glycol (EG) is a large-volume two-carbon commodity chemical used as the anti-freezing agent and building-block molecule for various polymers. Currently established microbial fermentation processes for converting monosaccharides to either ( R )-acetoin or EG are plagued by the formation of undesirable by-products. We show here that a cell-free bioreaction scheme can generate enantiomerically pure acetoin and EG as co-products from biomass-derived D-xylose...
December 2018: Metabolic Engineering Communications
https://read.qxmd.com/read/30194918/cannabidiol-skews-biased-agonism-at-cannabinoid-cb-1-and-cb-2-receptors-with-smaller-effect-in-cb-1-cb-2-heteroreceptor-complexes
#16
Gemma Navarro, Irene Reyes-Resina, Rafael Rivas-Santisteban, Verónica Sánchez de Medina, Paula Morales, Salvatore Casano, Carlos Ferreiro-Vera, Alejandro Lillo, David Aguinaga, Nadine Jagerovic, Xavier Nadal, Rafael Franco
Currently, biased agonism is at the center stage of drug development approaches. We analyzed effects of a battery of cannabinoids plus/minus cannabidiol (CBD) in four functional parameters (cAMP levels, phosphorylation of extracellular signal-regulated kinases (ERK1/2), β-arrestin recruitment and label-free/DMR) in HEK-293T cells expressing cannabinoid receptors, CB1 or CB2 , or CB1 -CB2 heteroreceptor complexes. In all cases two natural agonists plus two selective synthetic agonists were used. Furthermore, the effect of cannabidiol, at a dose (100 nM) that does not allow significant binding to the orthosteric center of either receptor, was measured...
September 6, 2018: Biochemical Pharmacology
https://read.qxmd.com/read/30090996/second-generation-cryoballoon-ablation-for-recurrent-atrial-fibrillation-after-an-index-cryoballoon-procedure-a-staged-strategy-with-variable-balloon-size
#17
Sjoerd W Westra, Stijn P G van Vugt, Sümeyye Sezer, Reinder Evertz, Martin E Hemels, Rypko J Beukema, Carlo de Asmundis, Marc A Brouwer, Gian-Battista Chierchia
PURPOSE: Currently, information on the optimal approach of redo procedures for paroxysmal atrial fibrillation (PAF) is limited. Radiofrequency ablation is the preferred technique, with reported success rates of 50-70% at 1-2 years, whereas only few reports exist on redo cryoballoon (CB) ablations. We describe outcomes on a systematic approach of repeat procedures with a second-generation cryoballoon (CB-2) after a successful index CB ablation. METHODS: Cohort study of 40 consecutive patients with recurrent PAF (55% male), median CHA2 DS2 -VASc score 1 (IQR 0-3)...
August 8, 2018: Journal of Interventional Cardiac Electrophysiology: An International Journal of Arrhythmias and Pacing
https://read.qxmd.com/read/30055149/emerging-strategies-targeting-cb-2-cannabinoid-receptor-biased-agonism-and-allosterism
#18
REVIEW
Paula Morales, Pilar Goya, Nadine Jagerovic
During these last years, the CB2 cannabinoid receptor has emerged as a potential anti-inflammatory target in diseases such as multiple sclerosis, amyotrophic lateral sclerosis, Huntington's disease, ischemic stroke, autoimmune diseases, osteoporosis, and cancer. However, the development of clinically useful CB2 agonists reveals to be very challenging. Allosterism and biased-signaling mechanisms at CB2 receptor may offer new avenues for the development of improved CB2 receptor-targeted therapies. Although there has been some exploration of CB1 receptor activation by new CB1 allosteric or biased-signaling ligands, the CB2 receptor is still at initial stages in this domain...
July 26, 2018: Biochemical Pharmacology
https://read.qxmd.com/read/30033591/vce-004-3-a-cannabidiol-aminoquinone-derivative-prevents-bleomycin-induced-skin-fibrosis-and-inflammation-through-ppar%C3%AE-and-cb-2-receptor-dependent-pathways
#19
Carmen Del Rio, Irene Cantarero, Belén Palomares, María Gómez-Cañas, Javier Fernández-Ruiz, Carolina Pavicic, Adela García-Martín, Maria Luz Bellido, Rafaela Ortega-Castro, Carlos Pérez-Sánchez, Chary López-Pedrera, Giovanni Appendino, Marco A Calzado, Eduardo Muñoz
BACKGROUND AND PURPOSE: The endocannabinoid system and PPARγ are important targets for the development of novel compounds against fibrotic diseases such as systemic sclerosis (SSc), also called scleroderma. The aim of this study was to characterize VCE-004.3, a novel cannabidiol derivative, and study its anti-inflammatory and anti-fibrotic activities. EXPERIMENTAL APPROACH: The binding of VCE-004.3 to CB1 and CB2 receptors and PPARγ and its effect on their functional activities were studied in vitro and in silico...
October 2018: British Journal of Pharmacology
https://read.qxmd.com/read/29990428/identification-of-the-first-synthetic-allosteric-modulator-of-the-cb-2-receptors-and-evidence-of-its-efficacy-for-neuropathic-pain-relief
#20
Francesca Gado, Lorenzo Di Cesare Mannelli, Elena Lucarini, Simone Bertini, Elena Cappelli, Maria Digiacomo, Lesley A Stevenson, Marco Macchia, Tiziano Tuccinardi, Carla Ghelardini, Roger G Pertwee, Clementina Manera
The direct activation of cannabinoid receptors (CBRs) results in several beneficial effects; therefore several CBRs ligands have been synthesized and tested in vitro and in vivo. However, none of them reached an advanced phase of clinical development due mainly to side effects on the CNS. Medicinal chemistry approaches are now engaged to develop allosteric modulators that might offer a novel therapeutic approach to achieve potential therapeutic benefits avoiding inherent side effects of orthosteric ligands...
July 23, 2018: Journal of Medicinal Chemistry
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