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https://www.readbyqxmd.com/read/27920472/anti-inflammatory-effect-of-cannabinoid-agonist-win55-212-on-mouse-experimental-colitis-is-related-to-inhibition-of-p38mapk
#1
Ya-Jing Feng, Yong-Yu Li, Xu-Hong Lin, Kun Li, Ming-Hua Cao
AIM: To investigate the anti-inflammatory effect and the possible mechanisms of an agonist of cannabinoid (CB) receptors, WIN55-212-2 (WIN55), in mice with experimental colitis, so as to supply experimental evidence for its clinical use in future. METHODS: We established the colitis model in C57BL/6 mice by replacing the animals' water supply with 4% dextran sulfate sodium (DSS) for 7 consecutive days. A colitis scoring system was used to evaluate the severity of colon local lesion...
November 21, 2016: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/27914737/targeted-proteomics-of-cannabinoid-receptor-cb1-and-the-cb1b-isoform
#2
Soumita Ghosh, Isabel González-Mariscal, Josephine M Egan, Ruin Moaddel
Cannabinoid receptors (CBR), including CB1 and CB2 have been therapeutic targets for a number of conditions. Recently, splice variants of the CB1R have been identified in humans. The isoforms differ in their N-terminus sequence and pharmacological activity relative to the CB1R, as a result, the differentiation between the CB1 receptor and its isoform is required. As a result, a selected reaction monitoring mass spectrometry (SRM-MS) method was developed for the quantitation of CB1 and the CB1b isoform in CHO cells transduced with CB1 and CB1b...
November 11, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27909504/long-term-evolution-of-patients-treated-for-paroxysmal-atrial-fibrillation-with-first-and-second-generation-cryoballoon-catheter-ablation-with-a-prospective-protocol-guided-by-complete-bidirectional-left-atrium-pulmonary-veins-disconnection-after-adenosine
#3
Jesus M Paylos Md PhD, Aracelis Morales Md, Luis Azcona Md, Marisol Paradela Md, Raquel Yagüe Md, Fernando Gómez-Guijarro Md, Lourdes Lacal Md, Clara Ferrero Rn, Octavio Rodríguez Md
INTRODUCTION: Cryoballoon ablation (CB) has proven effective for treating patients with paroxysmal atrial fibrillation (PAF). We analyzed our seven year follow-up of patients, treated for PAF with first (CB1) and second generation (CB2), with demonstration of LA-PV disconnection with bidirectional block (BB) after adenosine (AD). METHODS: Since November 2008 to May 2015, 128 patients, 97 male (58±7 years), without heart disease, highly symptomatic, refractory to antiarrhythmic drugs (AAD) were treated, and follow-up (1411 ±727 days)...
April 2016: Journal of Atrial Fibrillation
https://www.readbyqxmd.com/read/27909503/first-and-second-generation-cryoballoon-ablation-efficacy-restoring-and-maintaining-sinus-rhythm-in-patients-electrically-selected-and-treated-for-long-standing-persistent-atrial-fibrillation-after-acute-complete-electrical-disconnection-of-pulmonary-veins
#4
Jesus M Paylos Md PhD, Luis Azcona Md, Lourdes Lacal Md, Marisol Paradela Md, Carmen Cilleros Md, Ildefonso Del Campo Md, Clara Ferrero Rn Carlos Martínez Md PhD, Aracelis Morales Md
Introduction Cryoballoon ablation (CB) has proven effective to treatment of patients (pts) with atrial fibrillation (AF). However, the isolated efficacy of CB to treat pts with long-standing persistent atrial fibrillation (LSPAF) is less know. We analyzed the acute results and the long-term follow-up of our pts suffering LSPAF and initially treated with CB. Methods A cohort of 44 pts, 37 male (84%) mean age (60±10 year) suffering LSPAF were treated with first (CB1): 15pts, and second (CB2): 29 pts, generation CB...
April 2016: Journal of Atrial Fibrillation
https://www.readbyqxmd.com/read/27908562/ontogeny-of-sensorimotor-gating-and-short-term-memory-processing-throughout-the-adolescent-period-in-rats
#5
Anja A Goepfrich, Chris M Friemel, Sabina Pauen, Miriam Schneider
Adolescence and puberty are highly susceptible developmental periods during which the neuronal organization and maturation of the brain is completed. The endocannabinoid (eCB) system, which is well known to modulate cognitive processing, undergoes profound and transient developmental changes during adolescence. With the present study we were aiming to examine the ontogeny of cognitive skills throughout adolescence in male rats and clarify the potential modulatory role of CB1 receptor signalling. Cognitive skills were assessed repeatedly every 10th day in rats throughout adolescence...
November 19, 2016: Developmental Cognitive Neuroscience
https://www.readbyqxmd.com/read/27906750/role-of-orexin-2-and-cb1-receptors-within-the-periaqueductal-gray-matter-in-lateral-hypothalamic-induced-antinociception-in-rats
#6
Mohammad-Hossein Esmaeili, Zahra Reisi, Somayeh Ezzatpanah, Abbas Haghparast
Orexin plays an important role in pain modulation. Orexin-1 and orexin-2 receptors (Ox1r and Ox2r) are found at high density in the ventrolateral periaqueductal gray matter (vlPAG). Our previous study showed that chemical stimulation of the lateral hypothalamus with carbachol induces antinociception in the tail-flick test, a model of acute pain, and Ox1r-mediated antinociception in the vlPAG is modulated by the activity of vlPAG CB1 receptors. In the current study, TCS OX2 29, an Ox2r antagonist (5, 15, 50, 150, and 500 nmol/l), was microinjected into the vlPAG 5 min before the administration of carbachol (125 nmol/l)...
November 30, 2016: Behavioural Pharmacology
https://www.readbyqxmd.com/read/27905022/neurophysiology-of-space-travel-energetic-solar-particles-cause-cell-type-specific-plasticity-of-neurotransmission
#7
Sang-Hun Lee, Barna Dudok, Vipan K Parihar, Kwang-Mook Jung, Miklós Zöldi, Young-Jin Kang, Mattia Maroso, Allyson L Alexander, Gregory A Nelson, Daniele Piomelli, István Katona, Charles L Limoli, Ivan Soltesz
In the not too distant future, humankind will embark on one of its greatest adventures, the travel to distant planets. However, deep space travel is associated with an inevitable exposure to radiation fields. Space-relevant doses of protons elicit persistent disruptions in cognition and neuronal structure. However, whether space-relevant irradiation alters neurotransmission is unknown. Within the hippocampus, a brain region crucial for cognition, perisomatic inhibitory control of pyramidal cells (PCs) is supplied by two distinct cell types, the cannabinoid type 1 receptor (CB1)-expressing basket cells (CB1BCs) and parvalbumin (PV)-expressing interneurons (PVINs)...
November 30, 2016: Brain Structure & Function
https://www.readbyqxmd.com/read/27905004/ocular-disposition-of-%C3%A2-8-tetrahydrocannabinol-from-various-topical-ophthalmic-formulations
#8
Nagendra S Punyamurthula, Goutham R Adelli, Waseem Gul, Michael A Repka, Mahmoud A ElSohly, Soumyajit Majumdar
The purposes of this project are to enhance the trans-membrane penetration of Δ(8)-Tetrahydrocannabinol (Δ(8)-THC) and to study the effect of various lipid based systems in delivering the compound, non-invasively, to anterior and posterior ocular chambers. Solid lipid nanoparticles (SLNs), fast gelling films were manufactured using high pressure homogenization and melt cast techniques, respectively. The formulations were characterized for drug content, entrapment efficiency, particle size and subsequently evaluated in vitro for trans-corneal permeation...
November 30, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27900261/targeting-the-endocannabinoid-cb1-receptor-system-for-treating-obesity-in-prader-willi-syndrome
#9
Ibrahim Knani, Brian J Earley, Shiran Udi, Alina Nemirovski, Rivka Hadar, Asaad Gammal, Resat Cinar, Harry J Hirsch, Yehuda Pollak, Itai Gross, Talia Eldar-Geva, Daniela P Reyes-Capo, Joan C Han, Andrea M Haqq, Varda Gross-Tsur, Rachel Wevrick, Joseph Tam
OBJECTIVE: Extreme obesity is a core phenotypic feature of Prader-Willi syndrome (PWS). Among numerous metabolic regulators, the endocannabinoid (eCB) system is critically involved in controlling feeding, body weight, and energy metabolism, and a globally acting cannabinoid-1 receptor (CB1R) blockade reverses obesity both in animals and humans. The first-in-class CB1R antagonist rimonabant proved effective in inducing weight loss in adults with PWS. However, it is no longer available for clinical use because of its centrally mediated, neuropsychiatric, adverse effects...
December 2016: Molecular Metabolism
https://www.readbyqxmd.com/read/27899885/interacting-cannabinoid-and-opioid-receptors-in-the-nucleus-accumbens-core-control-adolescent-social-play
#10
Antonia Manduca, Olivier Lassalle, Marja Sepers, Patrizia Campolongo, Vincenzo Cuomo, Giovanni Marsicano, Brigitte Kieffer, Louk J M J Vanderschuren, Viviana Trezza, Olivier J J Manzoni
Social play behavior is a highly rewarding, developmentally important form of social interaction in young mammals. However, its neurobiological underpinnings remain incompletely understood. Previous work has suggested that opioid and endocannabinoid neurotransmission interact in the modulation of social play. Therefore, we combined behavioral, pharmacological, electrophysiological, and genetic approaches to elucidate the role of the endocannabinoid 2-arachidonoylglycerol (2-AG) in social play, and how cannabinoid and opioid neurotransmission interact to control social behavior in adolescent rodents...
2016: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/27899300/role-of-the-endocannabinoid-system-in-the-control-of-mouse-myometrium-contractility-during-the-menstrual-cycle
#11
Ester Pagano, Pierangelo Orlando, Stefania Finizio, Antonietta Rossi, Lorena Buono, Fabio Arturo Iannotti, Fabiana Piscitelli, Angelo A Izzo, Vincenzo Di Marzo, Francesca Borrelli
Cannabis and cannabinoids are known to affect female reproduction. However, the role of the endocannabinoid system in mouse uterine contractility in the dioestrus and oestrus phases has not been previously investigated. The present study aimed at filling this gap. Endocannabinoid (anandamide and 2-arachidonoylglycerol) levels were measured in mouse uterus at dioestrus and oestrus phases by liquid chromatography-mass spectrometry; quantitative reverse transcription-PCR measured mRNA expression of cannabinoid receptors and enzymes involved in the metabolism of endocannabinoids...
November 26, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27895162/cannabinoid-receptor-interacting-protein-crip-1a-competition-with-%C3%AE-arrestin-for-cb1-receptor-binding-sites
#12
Lawrence C Blume, Theresa Patten, Khalil Eldeeb, Sandra Leone-Kabler, Alexander A Ilyasov, Bradley M Keegan, Jeremy E O'Neal, Caroline E Bass, Roy R Hantgan, W Todd Lowther, Dana E Selley, Allyn C Howlett
Cannabinoid Receptor Interacting Protein1a (CRIP1a) is a CB1 receptor (CB1R) distal C-terminus-associated protein that alters CB1R interactions with G-proteins (Blume et al.,2015; Smith et al.,2015). We tested the hypothesis that CRIP1a is capable of also altering CB1R interactions with β-arrestin proteins that interact with the CB1R at the C-terminal. Co-immunoprecipitation studies indicated that CB1R associates in complexes with either CRIP1a or β-arrestin, but CRIP1a and β-arrestin fail to co-immunoprecipitate with each other...
November 28, 2016: Molecular Pharmacology
https://www.readbyqxmd.com/read/27891602/cannabimimetic-phytochemicals-in-the-diet-an-evolutionary-link-to-food-selection-and-metabolic-stress-adaptation
#13
REVIEW
Jürg Gertsch
The endocannabinoid system (ECS) is a major lipid signaling network that plays important pro-homeostatic (allostatic) roles not only in the nervous system but in peripheral organs. Increasing evidence points towards a dietary component in the modulation of the ECS. Cannabinoid receptors in hominids co-evolved with diet and the ECS constitutes a feedback loop for food selection and energy metabolism. Here it is postulated that the mismatch of ancient lipid genes of hunter-gatheres and pastoralists with the high carbohydrate diet introduced by agriculture could be compensated via dietary modulation of the ECS...
November 27, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27891077/presynaptic-g-protein-coupled-receptors-gatekeepers-of-addiction
#14
REVIEW
Kari A Johnson, David M Lovinger
Drug abuse and addiction cause widespread social and public health problems, and the neurobiology underlying drug actions and drug use and abuse is an area of intensive research. Drugs of abuse alter synaptic transmission, and these actions contribute to acute intoxication as well as the chronic effects of abused substances. Transmission at most mammalian synapses involves neurotransmitter activation of two receptor subtypes, ligand-gated ion channels that mediate fast synaptic responses and G protein-coupled receptors (GPCRs) that have slower neuromodulatory actions...
2016: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/27890818/the-anabolic-steroid-nandrolone-alters-cannabinoid-self-administration-and-brain-cb1-receptor-density-and-function
#15
Dicky Struik, Paola Fadda, Tamara Zara, Erica Zamberletti, Tiziana Rubino, Daniela Parolaro, Walter Fratta, Liana Fattore
Clinical and pre-clinical observations indicate that anabolic-androgenic steroids can induce neurobiological changes that alter the rewarding effects of drugs of abuse. In this study, we investigated the effect of the anabolic steroid nandrolone on the rewarding properties of the cannabinoid CB1 receptor agonist WIN55,212-2 (WIN) in rats. Lister Hooded male rats were treated intramuscularly with nandrolone (15mg/kg) or vehicle for 14 consecutive days, and then allowed to self-administer WIN (12.5μg/kg/infusion) intravenously...
November 24, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27890711/the-endogenous-lipid-n-arachidonoyl-glycine-is-hypotensive-and-nitric-oxide-cgmp-dependent-vasorelaxant
#16
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)...
November 24, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27884725/endocannabinoid-system-in-sexual-motivational-processes-is-it-a-novel-therapeutic-horizon
#17
REVIEW
Renata Androvicova, Jiri Horacek, Tibor Stark, Filippo Drago, Vincenzo Micale
The endocannabinoid system (ECS), which is composed of the cannabinoid receptors types 1 and 2 (CB1 and CB2) for marijuana's psychoactive ingredient Δ(9)-tetrahydrocannabinol (Δ(9)-THC), the endogenous ligands (AEA and 2-AG) and the enzymatic systems involved in their biosynthesis and degradation, recently emerged as important modulator of emotional and non-emotional behaviors. For centuries, in addition to its recreational actions, several contradictory claims regarding the effects of Cannabis use in sexual functioning and behavior (e...
November 21, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27879006/allosteric-modulation-an-alternate-approach-targeting-the-cannabinoid-cb1-receptor
#18
REVIEW
Thuy Nguyen, Jun-Xu Li, Brian F Thomas, Jenny L Wiley, Terry P Kenakin, Yanan Zhang
The cannabinoid CB1 receptor is a G protein coupled receptor and plays an important role in many biological processes and physiological functions. A variety of CB1 receptor agonists and antagonists, including endocannabinoids, phytocannabinoids, and synthetic cannabinoids, have been discovered or developed over the past 20 years. In 2005, it was discovered that the CB1 receptor contains allosteric site(s) that can be recognized by small molecules or allosteric modulators. A number of CB1 receptor allosteric modulators, both positive and negative, have since been reported and importantly, they display pharmacological characteristics that are distinct from those of orthosteric agonists and antagonists...
November 23, 2016: Medicinal Research Reviews
https://www.readbyqxmd.com/read/27875353/cannabinoid-receptor-2-functional-variant-contributes-to-the-risk-for-pediatric-inflammatory-bowel-disease
#19
Caterina Strisciuglio, Giulia Bellini, Erasmo Miele, Massimo Martinelli, Sabrina Cenni, Chiara Tortora, Carlo Tolone, Emanuele Miraglia Del Giudice, Francesca Rossi
GOALS: We conducted a case-control association analysis to establish the role of a common CB2 functional variant, Q63R, in the susceptibility to inflammatory bowel disease (IBD). BACKGROUND: Endocannabinoids may limit intestinal inflammation through cannabinoid receptor 1 and/or 2 (CB1, CB2). STUDY: We genotyped 217 pediatric IBD patients [112 Crohn's disease (CD), 105 ulcerative colitis (UC)] and 600 controls for the CB2-Q63R variant by Taqman assay...
November 21, 2016: Journal of Clinical Gastroenterology
https://www.readbyqxmd.com/read/27867358/biased-agonism-of-three-different-cannabinoid-receptor-agonists-in-mouse-brain-cortex
#20
Rebeca Diez-Alarcia, Inés Ibarra-Lecue, Ángela P Lopez-Cardona, Javier Meana, Alfonso Gutierrez-Adán, Luis F Callado, Ekaitz Agirregoitia, Leyre Urigüen
Cannabinoid receptors are able to couple to different families of G proteins when activated by an agonist drug. It has been suggested that different intracellular responses may be activated depending on the ligand. The goal of the present study was to characterize the pattern of G protein subunit stimulation triggered by three different cannabinoid ligands, Δ(9)-THC, WIN55212-2, and ACEA in mouse brain cortex. Stimulation of the [(35)S]GTPγS binding coupled to specific immunoprecipitation with antibodies against different subtypes of G proteins (Gαi1, Gαi2, Gαi3, Gαo, Gαz, Gαs, Gαq/11, and Gα12/13), in the presence of Δ(9)-THC, WIN55212-2 and ACEA (submaximal concentration 10 μM) was determined by scintillation proximity assay (SPA) technique in mouse cortex of wild type, CB1 knock-out, CB2 knock-out and CB1/CB2 double knock-out mice...
2016: Frontiers in Pharmacology
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