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https://www.readbyqxmd.com/read/30099006/selective-up-regulation-of-cannabinoid-cb-1-receptor-coupling-to-go-proteins-in-suicide-victims-with-mood-disorders
#1
Susana Mato, Fuencisla Pilar-Cuéllar, Elsa M Valdizán, Javier González-Maeso, Rafael Rodríguez-Puertas, Javier Meana, Joan Sallés, Benedicto Crespo-Facorro, Ángel Pazos
Brain endocannabinoid system is proposed to play a role in the pathogenesis of affective disorders. In the present study, we analyzed the functionality of the cannabinoid receptor type 1 (CB1 receptor) at different transduction levels in prefrontal cortex (PFC) of depressed suicide victims. We examined stimulation of [35 S]GTPγS binding, activation Gα protein subunits and inhibition of adenylyl cyclase by the cannabinoid agonist WIN55,212-2, as well as [3 H]CP55,940 binding, in PFC homogenates from suicide victims with major depression (MD) and matched control subjects...
August 9, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30096288/genetic-deletion-of-cb-1-cannabinoid-receptors-exacerbates-the-alzheimer-like-symptoms-in-a-transgenic-animal-model
#2
Ester Aso, Pol Andrés-Benito, Isidre Ferrer
Activating CB1 cannabinoid receptor has been demonstrated to produce certain therapeutic effects in animal models of Alzheimer's disease (AD). In this study, we evaluated the specific contribution of CB1 receptor to the progression of AD-like pathology in double transgenic APP/PS1 mice. A new mouse strain was generated by crossing APP/PS1 transgenic mice with CB1 knockout mice. Genetic deletion of CB1 drastically reduced the survival of APP/PS1 mice. In spite that CB1 mutant mice bearing the APP/PS1 transgene developed normally, they suddenly died within the first two months of life likely due to spontaneous seizures...
August 7, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30090996/second-generation-cryoballoon-ablation-for-recurrent-atrial-fibrillation-after-an-index-cryoballoon-procedure-a-staged-strategy-with-variable-balloon-size
#3
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://www.readbyqxmd.com/read/30073165/neuronal-calcium-and-camp-cross-talk-mediated-by-cannabinoid-cb-1-receptor-and-ef-hand-calcium-sensor-interactions
#4
Edgar Angelats, Marta Requesens, David Aguinaga, Michael R Kreutz, Rafael Franco, Gemma Navarro
Endocannabinoids are important players in neural development and function. They act via receptors, whose activation inhibits cAMP production. The aim of the paper was to look for calcium- and cAMP-signaling cross-talk mediated by cannabinoid CB1 receptors (CB1 R) and to assess the relevance of EF-hand CaM-like calcium sensors in this regard. Using a heterologous expression system, we demonstrated that CB1 R interacts with calneuron-1 and NCS1 but not with caldendrin. Furthermore, interaction motives were identified in both calcium binding proteins and the receptor, and we showed that the first two sensors competed for binding to the receptor in a Ca2+ -dependent manner...
2018: Frontiers in Cell and Developmental Biology
https://www.readbyqxmd.com/read/30002493/cb-1-receptor-activation-induces-intracellular-ca-2-mobilization-and-2-arachidonoylglycerol-release-in-rodent-spinal-cord-astrocytes
#5
Zoltán Hegyi, Tamás Oláh, Áron Kőszeghy, Fabiana Pisticelli, Krisztina Holló, Balázs Pál, László Csernoch, Vincenzo Di Marzo, Miklós Antal
Accumulating evidence supports the role of astrocytes in endocannabinoid mediated modulation of neural activity. It has been reported that some astrocytes express the cannabinoid type 1 receptor (CB1 -R), the activation of which is leading to Ca2+ mobilization from internal stores and a consecutive release of glutamate. It has also been documented that astrocytes have the potential to produce the endocannabinoid 2-arachidonoylglycerol, one of the best known CB1 -R agonist. However, no relationship between CB1 -R activation and 2-arachidonoylglycerol production has ever been demonstrated...
July 12, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29977202/cannabigerol-action-at-cannabinoid-cb-1-and-cb-2-receptors-and-at-cb-1-cb-2-heteroreceptor-complexes
#6
Gemma Navarro, Katia Varani, Irene Reyes-Resina, Verónica Sánchez de Medina, Rafael Rivas-Santisteban, Carolina Sánchez-Carnerero Callado, Fabrizio Vincenzi, Salvatore Casano, Carlos Ferreiro-Vera, Enric I Canela, Pier Andrea Borea, Xavier Nadal, Rafael Franco
Cannabigerol (CBG) is one of the major phytocannabinoids present in Cannabis sativa L. that is attracting pharmacological interest because it is non-psychotropic and is abundant in some industrial hemp varieties. The aim of this work was to investigate in parallel the binding properties of CBG to cannabinoid CB1 (CB1 R) and CB2 (CB2 R) receptors and the effects of the compound on agonist activation of those receptors and of CB1 -CB2 heteroreceptor complexes. Using [3 H]-CP-55940, CBG competed with low micromolar K i values the binding to CB1 R and CB2 R...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29967454/cannabinoid-cb-1-receptor-neutral-antagonist-am4113-inhibits-heroin-self-administration-without-depressive-side-effects-in-rats
#7
Xiang-Hu He, Chloe J Jordan, Kiran Vemuri, Guo-Hua Bi, Jia Zhan, Eliot L Gardner, Alexandros Makriyannis, Yan-Lin Wang, Zheng-Xiong Xi
Cannabinoid CB1 receptors (CB1 Rs) have been shown to be a promising target in medication development for the treatment of addiction. However, clinical trials with SR141716A (rimonabant, a selective CB1 R antagonist/inverse agonist) for the treatment of obesity and smoking cessation failed due to unwanted side effects, such as depression, anxiety, and suicidal tendencies. Recent preclinical studies suggest that the neutral CB1 R antagonist AM4113 may retain the therapeutic anti-addictive effects of SR141716A in nicotine self-administration models and possibly has fewer unwanted side effects...
July 2, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29958285/molecular-identification-and-functional-characterization-of-the-cathepsin-b-gene-ab-cb-1-in-the-plant-parasitic-nematode-aphelenchoides-besseyi
#8
Hong-Le Wang, Xi Cheng, Shan-Wen Ding, Dong-Wei Wang, Chun Chen, Chun-Ling Xu, Hui Xie
The rice white tip nematode, Aphelenchoides besseyi, is widely distributed in rice planting areas worldwide and causes serious economic losses. Cathepsin genes have been demonstrated to have importance in studying the reproduction, development, pathogenicity, and control methods of plant nematodes. In this paper, a novel cathepsin B gene, Ab-cb-1, was found and cloned. The Ab-cb-1 gene was 1347 bp in length and encodes 369 amino acids. The Ab-CB-1 protein contains characteristic occluding loops but no signal peptide...
2018: PloS One
https://www.readbyqxmd.com/read/29902669/effects-of-central-rvd-hemopressin-%C3%AE-administration-on-anxiety-feeding-behavior-and-hypothalamic-neuromodulators-in-the-rat
#9
Lucia Recinella, Annalisa Chiavaroli, Claudio Ferrante, Adriano Mollica, Giorgia Macedonio, Azzurra Stefanucci, Marilisa Pia Dimmito, Szabolcs Dvorácskó, Csaba Tömböly, Luigi Brunetti, Giustino Orlando, Sheila Leone
BACKGROUND: The endocannabinoid (eCB) system is strongly involved in the regulation of anxiety and feeding behavior. RVD-hemopressin(α) [RVD-hp(α)], a N-terminally extended form of hemopressin, is a negative allosteric modulator of the cannabinoid (CB) 1 receptor and a positive allosteric modulator of CB2 receptor which has been recently reported to exert anxiolytic/antidepressant and anorexigenic effects after peripheral administration in rats. Pharmacological evidences reported a possible link between brain hypocretin/orexin, monoamine and eCB systems, as regards appetite and emotional behavior control...
February 2, 2018: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29802957/increased-risk-of-respiratory-diseases-in-adults-with-type-1-and-type-2-diabetes
#10
Chelsey George, Alan M Ducatman, Baqiyyah N Conway
AIMS: Diabetes is linked with decreases in lung elasticity and in capacity to transfer carbon monoxide. Systemic inflammation, a common concern with diabetes, may contribute to airflow obstruction. We examined the association of self-reported diabetes with self-reported respiratory diseases (RDs) among 53,146 adults from the C8 Health Project. METHODS: Participants were categorized into three groups: Type 1 (T1D, n = 781), Type 2 (T2D, n = 4277), or no diabetes (n = 48,088)...
May 24, 2018: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/29792186/involvement-of-the-cb-2-cannabinoid-receptor-in-cell-growth-inhibition-and-g0-g1-cell-cycle-arrest-via-the-cannabinoid-agonist-win-55-212-2-in-renal-cell-carcinoma
#11
Mohammed I Khan, Anna A Sobocińska, Klaudia K Brodaczewska, Katarzyna Zielniok, Malgorzata Gajewska, Claudine Kieda, Anna M Czarnecka, Cezary Szczylik
BACKGROUND: The anti-tumor properties of cannabinoids have been investigated in many in vitro and in vivo studies. Many of these anti-tumor effects are mediated via cannabinoid receptor types 1 and 2 (CB1 and CB2 ), comprising the endocannabinoid system (ECS). In this study, we investigated the ECS based on CB 1 and CB 2 receptor gene and protein expression in renal cell carcinoma (RCC) cell lines. In view of their further use for potential treatments, we thus investigated the roles of CB1 and CB2 receptors in the anti-proliferative action and signal transduction triggered by synthetic cannabinoid agonists [such as JWH-133 and WIN 55,212-2 (WIN-55)] in RCC cell lines...
May 23, 2018: BMC Cancer
https://www.readbyqxmd.com/read/29790591/synthesis-of-13-c-6-labeled-dual-target-inhibitor-of-cannabinoid-1-receptor-cb-1-r-and-inducible-nitric-oxide-synthase-inos
#12
Malliga R Iyer, Resat Cinar, Nathan J Coffey, George Kunos
Cannabinoid-1 receptor (CB1 R) antagonists/inverse agonists have great potential in the treatment of metabolic disorders like dyslipidemia, type 2 diabetes, and nonalcoholic steatohepatitis. Cannabinoid-1 receptor inverse agonists have also been reported to be effective in mitigating fibrotic disorders in murine models. Inducible nitric oxide synthase is another promising target implicated in fibrotic and inflammatory disorders. We have disclosed MRI-1867 as a potent and selective, peripherally acting dual-target inhibitor of the CB1 R and inducible nitric oxide synthase (iNOS)...
May 23, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29779943/astroglial-cb-1-receptors-determine-synaptic-d-serine-availability-to-enable-recognition-memory
#13
Laurie M Robin, José F Oliveira da Cruz, Valentin C Langlais, Mario Martin-Fernandez, Mathilde Metna-Laurent, Arnau Busquets-Garcia, Luigi Bellocchio, Edgar Soria-Gomez, Thomas Papouin, Marjorie Varilh, Mark W Sherwood, Ilaria Belluomo, Georgina Balcells, Isabelle Matias, Barbara Bosier, Filippo Drago, Ann Van Eeckhaut, Ilse Smolders, Francois Georges, Alfonso Araque, Aude Panatier, Stéphane H R Oliet, Giovanni Marsicano
Bidirectional communication between neurons and astrocytes shapes synaptic plasticity and behavior. D-serine is a necessary co-agonist of synaptic N-methyl-D-aspartate receptors (NMDARs), but the physiological factors regulating its impact on memory processes are scantly known. We show that astroglial CB1 receptors are key determinants of object recognition memory by determining the availability of D-serine at hippocampal synapses. Mutant mice lacking CB1 receptors from astroglial cells (GFAP-CB1 -KO) displayed impaired object recognition memory and decreased in vivo and in vitro long-term potentiation (LTP) at CA3-CA1 hippocampal synapses...
June 6, 2018: Neuron
https://www.readbyqxmd.com/read/29667549/advances-in-the-understanding-of-the-cannabinoid-receptor-1-focusing-on-the-inverse-agonists-interactions
#14
Silvana Russo, Walter Filgueira De Azevedo
BACKGROUND: Cannabinoid Receptor 1 (CB1) is a membrane protein prevalent in the central nervous system, whose crystallographic structure has recently been solved. Studies will be needed to investigate CB1 complexes with its ligands and its role in the development of new drugs. OBJECTIVE: Our goal here is to review the studies on CB1, starting with general aspects and focusing on the recent structural studies, with emphasis on the inverse agonists bound structures...
April 17, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29575501/liquid-chromatography-isotope-ratio-mass-spectrometry-analysis-of-halogenated-benzoates-for-characterization-of-the-underlying-degradation-reaction-in-thauera-chlorobenzoica-cb-1-t
#15
Steffi Franke, Steffen Kümmel, Ivonne Nijenhuis
RATIONALE: Halogenated benzoic acids occur in the environment due to their widespread agricultural and pharmaceutical use. Compound-specific stable isotope analysis (CSIA) has developed over the last decades for investigation of in situ transformation and reaction mechanisms of environmental pollutants amenable by gas chromatography (GC). As polar compounds are unsuitable for GC analysis we developed a method to perform liquid chromatography (LC)/CSIA for halogenated benzoates. METHODS: LC/isotope ratio mass spectrometry (IRMS) utilizing a LC-Surveyor pump coupled to a MAT 253 isotope ratio mass spectrometer via a LC-Isolink interface was applied...
June 15, 2018: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/29501084/the-inhibition-of-cb-1-receptor-accelerates-the-onset-and-development-of-eae-possibly-by-regulating-microglia-macrophages-polarization
#16
Zhi-Yin Lou, Jie Cheng, Xiao-Rong Wang, Yong-Fei Zhao, Jing Gan, Guo-Yu Zhou, Zhen-Guo Liu, Bao-Guo Xiao
Cannabinoid 1 receptor (CB1 R) regulates the neuro-inflammatory and neurodegenerative damages of experimental autoimmune encephalomyelitis (EAE) and of multiple sclerosis (MS). The mechanism by which CB1 R inhibition exerts inflammatory effects is still unclear. Here, we explored the cellular and molecular mechanisms of CB1 R in the treatment of EAE by using a specific and selective CB1 R antagonist SR141716A. Our study demonstrated that SR141716A accelerated the clinical onset and development of EAE, accompanied by body weight loss...
April 15, 2018: Journal of Neuroimmunology
https://www.readbyqxmd.com/read/29454037/melatonin-attenuates-%C3%AE-9-tetrahydrocannabinol-induced-reduction-in-rat-sperm-motility-and-kinematics-in-vitro
#17
Isiaka Abdullateef Alagbonsi, Luqman Aribidesi Olayaki
The use of Cannabis sativa (CS) has been widely demonstrated to have detrimental effect on male reproductive functions. Despite the well-known existence of endocannabinoid and melatonergic systems in semen, the physiological significance of their interaction is not understood. We recently showed that melatonin exacerbates the CS-induced gonadotoxicity in-vivo. To overcome the limitations associated with our in-vivo studies and further understand the role of cannabinoid-melatonin relationship in sperm functions, this study investigated the in-vitro effect of tetrahydrocannabinol (THC) and/or melatonin on motility and kinematics of capacitating rat sperms...
April 2018: Reproductive Toxicology
https://www.readbyqxmd.com/read/29454025/early-alteration-of-distribution-and-activity-of-hippocampal-type-1-cannabinoid-receptor-in-alzheimer-s-disease-like-mice-overexpressing-the-human-mutant-amyloid-precursor-protein
#18
Mauro Maccarrone, Antonio Totaro, Alessandro Leuti, Giacomo Giacovazzo, Lucia Scipioni, Dalila Mango, Roberto Coccurello, Robert Nisticò, Sergio Oddi
Besides its involvement in Alzheimer's disease (AD) as precursor of the neurotoxic amyloid peptides, the pathophysiological impact of brain accumulation of amyloid precursor protein (APP) is not yet well understood. Recent studies reported that APP interacts with other membrane proteins, including G protein coupled receptors, affecting their biological functions. Here, we focused on the study of the potential impact of human mutant APP on expression, distribution and activity of type-1 cannabinoid (CB1 ) receptor in the hippocampus of Tg2576 mice, an AD-like mice model...
April 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/29450258/the-cannabinoids-%C3%AE-8-thc-cbd-and-hu-308-act-via-distinct-receptors-to-reduce-corneal-pain-and-inflammation
#19
Dinesh Thapa, Elizabeth A Cairns, Anna-Maria Szczesniak, James T Toguri, Meggie D Caldwell, Melanie E M Kelly
Background and Purpose: Corneal injury can result in dysfunction of corneal nociceptive signaling and corneal sensitization. Activation of the endocannabinoid system has been reported to be analgesic and anti-inflammatory. The purpose of this research was to investigate the antinociceptive and anti-inflammatory effects of cannabinoids with reported actions at cannabinoid 1 (CB1 R) and cannabinoid 2 (CB2 R) receptors and/or noncannabinoid receptors in an experimental model of corneal hyperalgesia. Methods: Corneal hyperalgesia (increased pain response) was generated using chemical cauterization of the corneal epithelium in wild-type (WT) and CB2 R knockout (CB2 R-/- ) mice...
2018: Cannabis and Cannabinoid Research
https://www.readbyqxmd.com/read/29156899/modulating-the-endocannabinoid-pathway-as-treatment-for-peripheral-neuropathic-pain-a-selected-review-of-preclinical-studies
#20
Shannon O'Hearn, Patrick Diaz, Bo Angela Wan, Carlo DeAngelis, Nicholas Lao, Leila Malek, Edward Chow, Alexia Blake
Chemotherapy-induced neuropathic pain is a distressing and commonly occurring side effect of many commonly used chemotherapeutic agents, which in some cases may prevent cancer patients from being able to complete their treatment. Cannabinoid based therapies have the potential to manage or even prevent pain associated with this syndrome. Pre-clinical animal studies that investigate the modulation of the endocannabinoid system (endogenous cannabinoid pathway) are being conducted to better understand the mechanisms behind this phenomenon...
December 2017: Annals of Palliative Medicine
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