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https://www.readbyqxmd.com/read/28088085/new-pyridazinone-4-carboxamides-as-new-cannabinoid-receptor-type-2-inverse-agonists-synthesis-pharmacological-data-and-molecular-docking
#1
Giulio Ragusa, María Gómez-Cañas, Paula Morales, Carmen Rodríguez-Cueto, María R Pazos, Battistina Asproni, Elena Cichero, Paola Fossa, Gerard A Pinna, Nadine Jagerovic, Javier Fernández-Ruiz, Gabriele Murineddu
In the last few years, cannabinoid type-2 receptor (CB2R) selective ligands have shown a great potential as novel therapeutic drugs in several diseases. With the aim of discovering new selective cannabinoid ligands, a series of pyridazinone-4-carboxamides was designed and synthesized, and the new derivatives tested for their affinity toward the hCB1R and hCB2R. The 6-(4-chloro-3-methylphenyl)-2-(4-fluorobenzyl)-N-(cis-4-methylcyclohexyl)-3-oxo-2,3-dihydropyridazine-4-carboxamide (9) displayed high CB2-affinity (KiCB2 = 2...
January 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28087785/thermolytic-degradation-of-synthetic-cannabinoids-chemical-exposures-and-pharmacological-consequences
#2
Brian F Thomas, Timothy W Lefever, Ricardo A Cortes, Alexander L Kovach, Anderson O Cox, Purvi R Patel, Gerald T Pollard, Julie A Marusich, Richard A Kevin, Thomas F Gamage, Jenny L Wiley
Synthetic cannabinoids are manufactured clandestinely with little quality control and are distributed as herbal "Spice" for smoking or as bulk compound for mixing with a solvent and inhalation via electronic vaporizers. Intoxication with synthetic cannabinoids has been associated with seizure, excited delirium, coma, kidney damage, and other disorders. The chemical alterations produced by heating these structurally novel compounds for consumption are largely unknown. Here we show that heating synthetic cannabinoids containing tetramethylcyclopropyl-ring substituents produced thermal degradants with pharmacological activity that varied considerably from their parent compounds...
January 13, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28087250/pharmacology-of-cannabinoids-in-the-treatment-of-epilepsy
#3
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/28079433/pet-imaging-of-cannabinoid-type-2-receptors-with-11-c-a-836339-did-not-evidence-changes-following-neuroinflammation-in-rats
#4
Geraldine Pottier, Vanessa Gómez-Vallejo, Daniel Padro, Raphaël Boisgard, Frédéric Dollé, Jordi Llop, Alexandra Winkeler, Abraham Martín
Cannabinoid type 2 receptors (CB2R) have emerged as promising targets for the diagnosis and therapy of brain pathologies. However, no suitable radiotracers for accurate CB2R mapping have been found to date, limiting the investigation of the CB2 receptor expression using positron emission tomography (PET) imaging. In this work, we report the evaluation of the in vivo expression of CB2R with [(11)C]A-836339 PET after cerebral ischemia and in two rat models of neuroinflammation, first by intrastriatal LPS and then by AMPA injection...
January 1, 2017: Journal of Cerebral Blood Flow and Metabolism
https://www.readbyqxmd.com/read/28069688/up-regulation-of-cb2-receptors-in-reactive-astrocytes-in-canine-degenerative-myelopathy-a-disease-model-of-amyotrophic-lateral-sclerosis
#5
María Fernández-Trapero, Francisco Espejo-Porras, Carmen Rodríguez-Cueto, Joan R Coates, Carmen Pérez-Díaz, Eva de Lago, Javier Fernández-Ruiz
Targeting the CB2 receptor afforded neuroprotection in SOD1(G93A) mutant mice, a model of amyotrophic lateral sclerosis (ALS). The neuroprotective effects of CB2 receptors were facilitated by their up-regulation in the spinal cord in SOD1(G93A) mutant mice. Herein, we have investigated whether a similar CB2 receptor up-regulation, as well as parallel changes in other endocannabinoid elements, are evident in the spinal cord of dogs with degenerative myelopathy (DM), caused from mutations in the superoxide dismutase 1 gene (SOD1)...
January 9, 2017: Disease Models & Mechanisms
https://www.readbyqxmd.com/read/28063111/comparison-of-catheter-ablation-for-paroxysmal-atrial-fibrillation-between-cryoballoon-and-radiofrequency-a-meta-analysis
#6
REVIEW
Chao-Feng Chen, Xiao-Fei Gao, Xu Duan, Bin Chen, Xiao-Hua Liu, Yi-Zhou Xu
PURPOSE: The present systematic review and meta-analysis aimed to assess and compare the safety and efficacy of radiofrequency (RF) and cryoballoon (CB) ablation for paroxysmal atrial fibrillation (PAF). RF and CB ablation are two frequently used methods for pulmonary vein isolation in PAF, but which is a better choice for PAF remains uncertain. METHODS: A systematic review was conducted in Medline, PubMed, Embase, and Cochrane Library. All trials comparing RF and CB ablation were screened and included if the inclusion criteria were met...
January 7, 2017: Journal of Interventional Cardiac Electrophysiology: An International Journal of Arrhythmias and Pacing
https://www.readbyqxmd.com/read/28045021/cannabinoid-cb2-receptor-ligand-profiling-reveals-biased-signalling-and-off-target-activity
#7
Marjolein Soethoudt, Uwe Grether, Jürgen Fingerle, Travis W Grim, Filomena Fezza, Luciano de Petrocellis, Christoph Ullmer, Benno Rothenhäusler, Camille Perret, Noortje van Gils, David Finlay, Christa MacDonald, Andrea Chicca, Marianela Dalghi Gens, Jordyn Stuart, Henk de Vries, Nicolina Mastrangelo, Lizi Xia, Georgios Alachouzos, Marc P Baggelaar, Andrea Martella, Elliot D Mock, Hui Deng, Laura H Heitman, Mark Connor, Vincenzo Di Marzo, Jürg Gertsch, Aron H Lichtman, Mauro Maccarrone, Pal Pacher, Michelle Glass, Mario van der Stelt
The cannabinoid CB2 receptor (CB2R) represents a promising therapeutic target for various forms of tissue injury and inflammatory diseases. Although numerous compounds have been developed and widely used to target CB2R, their selectivity, molecular mode of action and pharmacokinetic properties have been poorly characterized. Here we report the most extensive characterization of the molecular pharmacology of the most widely used CB2R ligands to date. In a collaborative effort between multiple academic and industry laboratories, we identify marked differences in the ability of certain agonists to activate distinct signalling pathways and to cause off-target effects...
January 3, 2017: Nature Communications
https://www.readbyqxmd.com/read/28041663/potent-immunomodulatory-activity-of-a-highly-selective-cannabinoid-cb2-agonist-on-immune-cells-from-healthy-subjects-and-patients-with-multiple-sclerosis
#8
Pasquale Annunziata, Chiara Cioni, Claudia Mugnaini, Federico Corelli
COR167, a novel CB2-selective high affinity agonist, was found to significantly inhibit, in a dose-dependent manner, the proliferation of both peripheral blood mononuclear cells and myelin basic protein-reactive T cell lines from normal healthy subjects and patients with relapsing-remitting multiple sclerosis (MS). In MS, a significantly higher inhibition was observed in patients on treatment with disease modifying drugs compared to those naive to treatment. The inhibitory activity of COR167 was exerted through a mixed mechanism involving atypical and incomplete shift of Th1 phenotype towards Th2 phenotype associated with slight reduction of IL-4 and IL-5 as well as strongly reduced levels of Th17-related cytokines...
December 23, 2016: Journal of Neuroimmunology
https://www.readbyqxmd.com/read/28035344/dietary-olive-oil-induces-cannabinoid-cb2-receptor-expression-in-adipose-tissue-of%C3%A2-apc-min-transgenic-mice
#9
Maria Notarnicola, Valeria Tutino, Angela Tafaro, Giusy Bianco, Emilia Guglielmi, Maria Gabriella Caruso
BACKGROUND: Cannabinoid- 2 (CB2) receptor is known for its anti-obesity effects silencing the activated immune cells that are key drivers of metabolic syndrome and inflammation. Nutritional interventions in experimental models of carcinogenesis have been demonstrated to modulate tissue inflammation state and proliferation. OBJECTIVE: Aim of this study was to test, in Apc(Min/+) mice, whether a diet enriched with olive oil, omega- 3 and omega-6- PUFAs affects the adipose tissue inflammation status. METHODS: Four groups of animal were studied: ST group, receiving a standard diet; OO group, receiving the standard diet in which soybean oil (source of fats) was replaced with olive oil; OM-3 group, receiving the standard diet in which soybean oil was replaced with salmon oil; OM-6 group, receiving the standard diet in which soybean oil was replaced with oenothera oil...
October 27, 2016: Nutr Healthy Aging
https://www.readbyqxmd.com/read/28026135/protective-effects-of-trans-caryophyllene-on-maintaining-osteoblast-function
#10
Jinghua Shan, Lixia Chen, Keliang Lu
Age-related osteoblast dysfunction is the main cause of age-related bone loss. Trans-caryophyllene (TC) is an important constituent of the essential oils derived from several species of medicinal plants. In this study, we investigated the effects of TC on osteoblast function in osteoblastic MC3T3-E1 cells. The results indicate that TC caused a significant elevation in collagen content, alkaline phosphatase activity, osteocalcin production, and mineralization, which are the four markers that account for the various stages of osteoblastic differentiation...
January 2017: IUBMB Life
https://www.readbyqxmd.com/read/28012093/pharmacological-and-toxicological-effects-of-synthetic-cannabinoids-and-their-metabolites
#11
Sherrica Tai, William E Fantegrossi
Commercial preparations containing synthetic cannabinoids (SCBs) are rapidly emerging as drugs of abuse. Although often assumed to be "safe" and "legal" alternatives to cannabis, reports indicate that SCBs induce toxicity not often associated with the primary psychoactive component of marijuana, Δ9-tetrahydrocannabinol (Δ(9)-THC). This chapter will summarize the evidence that use of SCBs poses greater health risks relative to marijuana and suggest that distinct pharmacological properties and metabolism of SCBs relative to Δ(9)-THC may contribute to this increased toxicity...
December 24, 2016: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28010996/pharmacological-characterization-of-rat-vd-hemopressin-%C3%AE-an-%C3%AE-hemoglobin-derived-peptide-exhibiting-cannabinoid-agonist-like-effects-in-mice
#12
Ting Zheng, Ting Zhang, Run Zhang, Zi-Long Wang, Zheng-Lan Han, Ning Li, Xu-Hui Li, Meng-Na Zhang, Biao Xu, Xiong-Li Yang, Quan Fang, Rui Wang
Hemopressin and related peptides have shown to function as the endogenous ligands or the regulator of cannabinoid receptors. Moreover, hemopressin and its truncated peptides were also reported to produce a slight modulatory effect on opioid system. In the present work, based on the amino acid sequence analyses of hemoglobin subunit α, rat VD-hemopressin(α) [(r)VD-Hpα] was predicted as a cannabinoid peptide derived from rat α-hemoglobin. Furthermore, (r)VD-Hpα was synthesized and characterized in a series of in vitro and in vivo assays...
December 16, 2016: Neuropeptides
https://www.readbyqxmd.com/read/28007501/synergistic-attenuation-of-chronic-pain-using-mu-opioid-and-cannabinoid-receptor-2-agonists
#13
Shaness A Grenald, Madison A Young, Yue Wang, Michael H Ossipov, Mohab M Ibrahim, Tally M Largent-Milnes, Todd W Vanderah
The misuse of prescription opiates is on the rise with combination therapies (e.g. acetaminophen or NSAIDs) resulting in severe liver and kidney damage. In recent years, cannabinoid receptors have been identified as potential modulators of pain and rewarding behaviors associated with cocaine, nicotine and ethanol in preclinical models. Yet, few studies have identified whether mu opioid agonists and CB2 agonists act synergistically to inhibit chronic pain while reducing unwanted side effects including reward liability...
December 20, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27994006/attenuation-of-cocaine-induced-conditioned-place-preference-and-motor-activity-via-cannabinoid-cb2-receptor-agonism-and-cb1-receptor-antagonism-in-rats
#14
Foteini Delis, Alexia Polissidis, Nafsika Poulia, Zuzana Justinova, George G Nomikos, Steven R Goldberg, Katerina Antoniou
BACKGROUND: Studies have shown the involvement of cannabinoid (CB) receptors in the behavioral and neurobiological effects of psychostimulants. Most of these studies have focused on the role of CB1 receptors in the psychostimulant effects of cocaine, while very few have investigated the respective role of CB2 receptors. Further studies are warranted to elucidate the extent of CB receptor involvement in the expression of cocaine-induced effects. METHODS: The role of CB1 and CB2 receptors in the rewarding and motor properties of cocaine was assessed in conditioned place preference, conditioned motor activity, and open field activity in rats...
December 19, 2016: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27993113/the-role-of-mifamurtide-in-chemotherapy-induced-osteoporosis-of-children-with-osteosarcoma
#15
Bellini Giulia, Di Pinto Daniela, Tortora Chiara, Manzo Iolanda, Punzo Francesca, Casale Fiorina, Rossi Francesca
BACKGROUND: Osteosarcoma is the most frequent malignant bone tumor in childhood and young adulthood. Long-term survivors of OS patients show high prevalence of osteoporosis and fractures. The immunomodulatory mifamurtide, which modulates macrophages activity, improves disease outcome. OBJECTIVE: To evaluate the role of mifamurtide on macrophage component of bone, the osteoclasts, during chemotherapy in children with osteosarcoma. METHOD: Osteoclasts, obtained from peripheral blood cells of healthy donors were harvested in presence or not of mifamurtide...
December 15, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27992060/cb2-receptors-regulate-natural-killer-cells-that-limit-allergic-airway-inflammation-in-a-murine-model-of-asthma
#16
M E Ferrini, S Hong, A Stierle, D Stierle, N Stella, K Roberts, Z Jaffar
BACKGROUND: Allergic asthma is a chronic airway inflammatory disease involving the complementary actions of innate and adaptive immune responses. Endogenously generated cannabinoids, acting via CB2 receptors play important roles in both homeostatic and inflammatory processes. However, the contribution of CB2-acting eicosanoids to the innate events preceding sensitization to the common house dust mite (HDM) allergen, remain to be elucidated. We investigated the role of CB2 activation during allergen-induced pulmonary inflammation and NK cell effector function...
December 19, 2016: Allergy
https://www.readbyqxmd.com/read/27989582/expression-of-cannabinoid-type-1-receptors-in%C3%A2-human-odontoblast-cells
#17
Kehua Que, Dan He, Ying Jin, Ligeng Wu, Fang Wang, Zhiying Zhao, Jing Yang, Jiayin Deng
INTRODUCTION: The aim of this study was to investigate the functional expression of cannabinoid type 1 (CB1) receptors in human odontoblasts (HODs) and the possible internal mechanism. METHODS: In the present study, we examined the molecular and functional expression of the CB1 receptors in cultured HOD-like cells and native HODs obtained from healthy wisdom teeth. RESULTS: Immunohistochemistry and immunofluorescence revealed that CB1 receptors localize to native HODs and HOD-like cells, respectively...
December 15, 2016: Journal of Endodontics
https://www.readbyqxmd.com/read/27960161/cannabinoid-2-receptor-agonist-improves-systemic-sensitivity-to-insulin-in-high-fat-diet-streptozotocin-induced-diabetic-mice
#18
Xiuyuan Zhang, Shan Gao, Jinfeng Niu, Pan Li, Juan Deng, Shixin Xu, Zhihong Wang, Weiwei Wang, Deling Kong, Chen Li
BACKGROUND/AIMS: The endocannabinoid signalling (ECS) system has been known to regulate glucose homeostasis. Previous studies have suggested that the cannabinoid 2 (CB2) receptor may play a regulatory role on insulin secretion, immune modulation and insulin resistance. Given that diabetes and insulin resistance are attributable to elevated inflammatory tone, we investigated the role of CB2 receptor on glucose tolerance and insulin sensitivity in high-fat diet (HFD)/streptozotocin (STZ)-induced mice...
2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27940994/compensatory-activation-of-cannabinoid-cb2-receptor-inhibition-of-gaba-release-in-the-rostral-ventromedial-medulla-rvm-in-inflammatory-pain
#19
Ming-Hua Li, Katherine L Suchland, Susan L Ingram
: The rostral ventromedial medulla (RVM) is a relay in the descending pain modulatory system and an important site of endocannabinoid modulation of pain. Endocannabinoids inhibit GABA release in the RVM but it is not known if this effect persists in chronic pain states. In the present studies, persistent inflammation induced by complete Freund's adjuvant (CFA) increased GABAergic miniature inhibitory postsynaptic currents (mIPSCs). Endocannabinoid activation of cannabinoid (CB1) receptors known to inhibit presynaptic GABA release was significantly reduced in the RVM of CFA-treated rats compared to naïve rats...
December 9, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27935269/from-adolescent-to-elder-rats-motivation-for-palatable-food-and-cannabinoids-receptors
#20
Octavio Amancio-Belmont, Antonio Romano-López, Alejandra Evelin Ruiz-Contreras, Mónica Méndez-Díaz, Oscar Prospéro-García
To analyze motivation, food self-administration and decision-making was evaluated in adolescent, adult and aged rats. Subjects were trained to press a lever (fixed ratio, FR1 and FR5) in an operant chamber, to obtain chocolate flavor pellets. We assessed the progressive ratio (PR), extinction and reinstatement of the behavior. To estimate decision-making for food, rats were trained in the conditioned place preference (CPP) paradigm: a) associating one compartment with lab chow (LCh) one day and the other compartment with rice krisspies (RK), the next day...
December 9, 2016: Developmental Neurobiology
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