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https://www.readbyqxmd.com/read/28918320/in-silico-interaction-analysis-of-cannabinoid-receptor-interacting-protein-1b-crip1b-cb1-cannabinoid-receptor
#1
Pratishtha Singh, Anjali Ganjiwale, Allyn C Howlett, Sudha M Cowsik
Cannabinoid Receptor Interacting Protein isoform 1b (CRIP1b) is known to interact with the CB1 receptor. Alternative splicing of the CNRIP1 gene produces CRIP1a and CRIP1b with a difference in the third exon only. Exons 1 and 2 encode for a functional domain in both proteins. CRIP1a is involved in regulating CB1 receptor internalization, but the function of CRIP1b is not very well characterized. Since there are significant identities in functional domains of these proteins, CRIP1b is a potential target for drug discovery...
September 6, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28917977/the-role-of-the-endocannabinoid-system-in-the-antihyperalgesic-effect-of-cedrus-atlantica-essential-oil-inhalation-in-a-mouse-model-of-postoperative-pain
#2
Aline Armiliato Emer, Nathalia Nahas Donatello, Ana Paula Batisti, Luiz Augusto de Oliveira Belmonte, Adair R S Santos, Daniel F Martins
ETHNOPHARMACOLOGICAL RELEVANCE: Cedar is part of the phylum of conifers, and it´s essential oil has been used for therapeutic purposes since ancient times. In our previous study, we have demonstrated that the inhalation of the Cedrus atlantica essential oil (CaEO) induces an antihyperalgesic effect in a model of postoperative pain. But the mechanism that underlies this effect is not yet fully known. AIM OF THE STUDY: This study investigates the involvement of the endocannabinoid system in the antihyperalgesic effect produced by the inhalation of CaEO in a post operative pain model...
September 13, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28916833/inhibition-of-wnt-%C3%AE-catenin-pathway-and-histone-acetyltransferase-activity-by-rimonabant-a-therapeutic-target-for-colon-cancer
#3
Maria Chiara Proto, Donatella Fiore, Chiara Piscopo, Silvia Franceschelli, Valentina Bizzarro, Chiara Laezza, Gianluigi Lauro, Alessandra Feoli, Alessandra Tosco, Giuseppe Bifulco, Gianluca Sbardella, Maurizio Bifulco, Patrizia Gazzerro
In a high percentage (≥85%) of both sporadic and familial adenomatous polyposis forms of colorectal cancer (CRC), the inactivation of the APC tumor suppressor gene initiates tumor formation and modulates the Wnt/β-Catenin transduction pathways involved in the control of cell proliferation, adhesion and metastasis. Increasing evidence showed that the endocannabinoids control tumor growth and progression, both in vitro and in vivo. We evaluated the effect of Rimonabant, a Cannabinoid Receptor 1 (CB1) inverse agonist, on the Wnt/β-Catenin pathway in HCT116 and SW48 cell lines carrying the genetic profile of metastatic CRC poorly responsive to chemotherapies...
September 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28914627/antinociceptive-effects-of-jwh015-in-female-and-male-rats
#4
Rebecca M Craft, Nicholas Z Greene, Alexa A Wakley
Despite greater chronic pain prevalence in females compared with males, and the analgesic potential of cannabinoid receptor type 2 (CB2) agonists, CB2 agonists have rarely been tested in females. The aim of the present study was to compare the antinociceptive effects of a CB2-preferring agonist, (2-methyl-1-propyl-1H-indol-3-yl)-1-naphthalenylmethanone (JWH015), in female and male rats against acute pain and persistent inflammatory pain. JWH015 (5-20 mg/kg, intraperitoneally) produced dose-dependent and time-dependent increases in latency to respond on the tail withdrawal and paw pressure tests that did not differ statistically between the sexes...
September 13, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28913816/re-visiting-the-endocannabinoid-system-and-its-therapeutic-potential-in-obesity-and-associated-diseases
#5
REVIEW
Joyce M Richey, Orison Woolcott
PURPOSE OF REVIEW: The purpose of the review was to revisit the possibility of the endocannabinoid system being a therapeutic target for the treatment of obesity by focusing on the peripheral roles in regulating appetite and energy metabolism. RECENT FINDINGS: Previous studies with the global cannabinoid receptor blocker rimonabant, which has both central and peripheral properties, showed that this drug has beneficial effects on cardiometabolic function but severe adverse psychiatric side effects...
September 14, 2017: Current Diabetes Reports
https://www.readbyqxmd.com/read/28903355/anti-proliferative-pro-apoptotic-and-anti-invasive-effect-of-ec-ev-system-in-human-osteosarcoma
#6
Francesca Punzo, Chiara Tortora, Daniela Di Pinto, Iolanda Manzo, Giulia Bellini, Fiorina Casale, Francesca Rossi
Osteosarcoma is the most common and aggressive bone tumor in children. The Endocannabinoid/Endovanilloid system has been proposed as anticancer target in tumor of different origins. This system is composed of two receptors (CB1 and CB2), the Transient Potential Vanilloid 1 (TRPV1) channel and their ligands and enzymes. CB1 is expressed mainly in central nervous system while CB2 predominantly on immune and peripheral cells. We investigated the effects of JWH-133 (CB2 agonist) and RTX (TRPV1 agonist) in six human Osteosarcoma cell lines: MG-63, U-2OS, MNNG/HOS, Saos-2, KHOS/NP, Hs888Lu, by Apoptosis and Migration-Assay...
August 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28901271/the-role-of-cannabinoid-receptors-in-renal-diseases
#7
Hélène François, Lola Lecru
Chronic kidney disease (CKD) remains a major challenge for Public Health systems and corresponds to the replacement of renal functional tissue by extra-cellular matrix proteins such as collagens and fibronectin. There is no efficient treatment to date for CKD except nephroprotective strategies. The cannabinoid system and more specifically the cannabinoid receptors 1 (CB1) and 2 (CB2) may represent a new therapeutic target in CKD. Our review will first focus on the current state of knowledge regarding the cannabinoid system in normal renal physiology and in various experimental nephropathies, especially diabetes...
September 11, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28890367/enhanced-anandamide-signaling-reduces-flight-behavior-elicited-by-an-approaching-robo-beetle
#8
Daniel E Heinz, Andreas Genewsky, Carsten T Wotjak
Our current knowledge of the implications of endocannabinoids in fear and anxiety is largely based on fear conditioning paradigms and approach-avoidance conflicts. Here we establish the ethobehavioral beetle mania task (BMT), which confronts mice with an erratically moving robo-beetle. With the help of this task we demonstrate decreased tolerance yet increased avoidance responses to an approaching beetle in high-anxiety behavior (HAB) and BALBc mice compared to C57BL/6N, CD1 and normal-anxiety behavior (NAB) mice...
September 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28889355/tingenone-a-pentacyclic-triterpene-induces-peripheral-antinociception-due-to-cannabinoid-receptors-activation-in-mice
#9
C C Veloso, R C M Ferreira, V G Rodrigues, L P Duarte, A Klein, I D Duarte, T R L Romero, A C Perez
Several works have shown that triterpenes induce peripheral antinociception by activation of cannabinoid receptors and endocannabinoids; besides, several research groups have reported activation of cannabinoid receptors in peripheral antinociception. The aim of this study was to assess the involvement of the cannabinoid system in the antinociceptive effect induced by tingenone against hyperalgesia evoked by prostaglandin E2 (PGE2) at peripheral level. The paw pressure test was used and the hyperalgesia was induced by intraplantar injection of PGE2 (2 μg/paw)...
September 9, 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/28889197/changes-in-gene-expression-in-the-locus-coeruleus-amygdala-circuitry-in-inhibitory-avoidance-ptsd-model
#10
Esther L Sabban, Lidia I Serova, Elizabeth Newman, Nurit Aisenberg, Irit Akirav
The locus coeruleus (LC)-amygdala circuit is implicated in playing a key role in responses to emotionally arousing stimuli and in the manifestation of post-traumatic stress disorder (PTSD). Here, we examined changes in gene expression of a number of important mediators of the LC-amygdala circuitry in the inhibition avoidance model of PTSD. After testing for basal acoustic startle response (ASR), rats were exposed to a severe footshock (1.5 mA for 10 s) in the inhibitory avoidance apparatus. They were given contextual situational reminders every 5 day for 25 days...
September 9, 2017: Cellular and Molecular Neurobiology
https://www.readbyqxmd.com/read/28880480/monoacylglycerol-signalling-and-abhd6-in-health-and-disease
#11
REVIEW
Pegah Poursharifi, Sri Ramachandra Murthy Madiraju, Marc Prentki
Lipid metabolism dysregulation underlies chronic pathologies such as obesity, diabetes and cancer. Besides their role in structure and energy storage, lipids are also important signalling molecules regulating multiple biological functions. Thus, understanding the precise lipid metabolism enzymatic steps that are altered in some pathological conditions is helpful for designing better treatment strategies. Several monoacylglycerol (MAG) species are only recently being recognized as signalling lipid molecules in different tissues...
September 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28877641/collagen-and-hydroxyapatite-scaffolds-activate-distinct-osteogenesis-signaling-pathways-in-adult-adipose-derived-multipotent-stromal-cells
#12
Wei Duan, Masudul Haque, Michael T Kearney, Mandi Lopez
Osteogenic cell signaling pathway disruption varies among bone diseases. This investigation was designed to identify adipose derived multipotent stromal cell (ASC) and bone graft scaffold combinations for local, targeted restoration of gene expression and extracellular matrix (ECM) deposition. Human ASC osteogenesis on bone graft materials was quantified following culture in stromal (S), osteogenic (O) or osteogenic for 48 hours followed by stromal medium (OS) to test the two-part hypothesis: 1) Identical ASC isolates on distinct bone graft scaffolds demonstrate unique viability, differentiation, ECM production and gene expression in the same culture conditions; 2) Identical ASC-bone graft scaffold combinations have different cell viability, differentiation, ECM production, and gene expression when cultured in S, O or OS medium...
September 6, 2017: Tissue Engineering. Part C, Methods
https://www.readbyqxmd.com/read/28875496/g-protein-coupled-receptor-gpr55-promotes-colorectal-cancer-and-has-opposing-effects-to-cannabinoid-receptor-1
#13
Carina Hasenoehrl, David Feuersinger, Eva M Sturm, Thomas Bärnthaler, Ellen Heitzer, Ricarda Graf, Magdalena Grill, Martin Pichler, Stephan Beck, Lee Butcher, Dominique Thomas, Nerea Ferreirós, Rufina Schuligoi, Caroline Schweiger, Johannes Haybaeck, Rudolf Schicho
The putative cannabinoid receptor GPR55 has been shown to play a tumor-promoting role in various cancers, and is involved in many physiological and pathological processes of the gastrointestinal (GI) tract. While the cannabinoid receptor 1 (CB1 ) has been reported to suppress intestinal tumor growth, the role of GPR55 in the development of GI cancers is unclear. We, therefore, aimed at elucidating the role of GPR55 in colorectal cancer (CRC), the third most common cancer worldwide. Using azoxymethane (AOM)- and dextran sulfate sodium (DSS)-driven CRC mouse models, we found that GPR55 plays a tumor-promoting role that involves alterations of leukocyte populations, i...
September 5, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28874764/natural-%C3%A2-9-thc-and-synthetic-jwh-018-cannabinoids-induce-seizures-by-acting-through-the-cannabinoid-cb1-receptor
#14
Olga Malyshevskaya, Kosuke Aritake, Mahesh K Kaushik, Nahoko Uchiyama, Yoan Cherasse, Ruri Kikura-Hanajiri, Yoshihiro Urade
Natural cannabinoids and their synthetic substitutes are the most widely used recreational drugs. Numerous clinical cases describe acute toxic symptoms and neurological consequences following inhalation of the mixture of synthetic cannabinoids known as "Spice." Here we report that an intraperitoneal administration of the natural cannabinoid Δ(9)-tetrahydrocannabinol (10 mg/kg), one of the main constituent of marijuana, or the synthetic cannabinoid JWH-018 (2.5 mg/kg) triggered electrographic seizures in mice, recorded by electroencephalography and videography...
September 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28869110/anandamide-exerts-a-suppressive-effect-on-sperm-binding-to-oviduct-explants-through-cb1-receptors-in-the-water-buffalo-bubalus-bubalis
#15
Vimlesh Kumar, Arumugam Kumaresan, Puneeth Kumar D S, Sreela Lathika, Samiksha Nayak, Kaustubh Kishor Saraf, Pradeep Nag B S, Shivani Chhillar, Tirtha Kumar Datta, Tushar Kumar Mohanty
An endocannabinoid system comprising of Anandamide (AEA) and its receptor has been shown to play a role in sperm acquisition of fertilizing potential and sperm-oviduct interaction. In the present study, we assessed the effect of sperm pre-treatment with AEA or co-incubation of sperm-oviduct explants with AEA in the presence or absence of CB1 receptor antagonist (SR141716A) on sperm-oviduct binding in the water buffalo. Cryopreserved spermatozoa from 3 Murrah buffalo bulls (3 ejaculates from each bull) were utilized for the study...
October 2017: Animal Reproduction Science
https://www.readbyqxmd.com/read/28867485/mechanisms-of-action-of-cannabidiol-in-adoptively-transferred-experimental-autoimmune-encephalomyelitis
#16
Coral González-García, Irene Moreno Torres, Ruth García-Hernández, Lucía Campos-Ruíz, Luis Rodríguez Esparragoza, María José Coronado, Aranzazu García Grande, Antonio García-Merino, Antonio J Sánchez López
Cannabidiol (CBD) is one of the most important compounds in Cannabis sativa, lacks psychotropic effects, and possesses a high number of therapeutic properties including the amelioration of experimental autoimmune encephalomyelitis (EAE). The aim of this study was to analyse the relative efficacy of CBD in adoptively transferred EAE (at-EAE), a model that allows better delineation of the effector phase of EAE. Splenocytes and lymph nodes from mice with actively induced EAE were cultured in the presence of MOG35-55 and IL-12 and inoculated intraperitoneally in recipient female C57BL/6J mice...
September 1, 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28866072/changes-in-the-cannabinoids-receptors-in-rats-following-treatment-with-antidepressants
#17
Irena Smaga, Magdalena Zaniewska, Dawid Gawliński, Agata Faron-Górecka, Przemysław Szafrański, Marek Cegła, Małgorzata Filip
The endocannabinoid (eCB) system plays a significant role in the pathophysiology of depression. The potential participation of this system in the mechanism of action of antidepressants has been highlighted in recent years. The aim of this study was to investigate the expression of cannabinoid (CB) receptors using Western blot and CB1 receptor density using autoradiography after acute or chronic administration of antidepressant drugs [imipramine (IMI, 15mg/kg), escitalopram (ESC, 10mg/kg) and tianeptine (TIA, 10mg/kg)]...
September 1, 2017: Neurotoxicology
https://www.readbyqxmd.com/read/28862250/cb1-receptors-signaling-in-the-brain-extracting-specificity-from-ubiquity
#18
Arnau Busquets-Garcia, Jaideep Bains, Giovanni Marsicano
Endocannabinoids (eCBs) are amongst the most ubiquitous signaling molecules in the nervous system. Over the past few decades, observations based on a large volume of work, first examining the pharmacological effects of exogenous cannabinoids, and then the physiological functions of eCBs, have directly challenged long-held and dogmatic views about communication, plasticity and behavior in the Central Nervous System (CNS). The eCBs and their cognate cannabinoid receptors exhibit a number of unique properties that distinguish them from the widely studied classical amino acid transmitters, neuropeptides and catecholamines...
September 1, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28861508/affinity-and-efficacy-studies-of-tetrahydrocannabinolic-acid-a-at-cannabinoid-receptor-types-one-and-two
#19
John M McPartland, Christa MacDonald, Michelle Young, Phillip S Grant, Daniel P Furkert, Michelle Glass
Introduction:Cannabis biosynthesizes Δ(9)-tetrahydrocannabinolic acid (THCA-A), which decarboxylates into Δ(9)-tetrahydrocannabinol (THC). There is growing interest in the therapeutic use of THCA-A, but its clinical application may be hampered by instability. THCA-A lacks cannabimimetic effects; we hypothesize that it has little binding affinity at cannabinoid receptor 1 (CB1). Materials and Methods: Purity of certified reference standards were tested with high performance liquid chromatography (HPLC). Binding affinity of THCA-A and THC at human (h) CB1 and hCB2 was measured in competition binding assays, using transfected HEK cells and [(3)H]CP55,940...
2017: Cannabis and Cannabinoid Research
https://www.readbyqxmd.com/read/28861507/a-conversion-of-oral-cannabidiol-to-delta9-tetrahydrocannabinol-seems-not-to-occur-in-humans
#20
Gerhard Nahler, Franjo Grotenhermen, Antonio Waldo Zuardi, José A S Crippa
Cannabidiol (CBD), a major cannabinoid of hemp, does not bind to CB1 receptors and is therefore devoid of psychotomimetic properties. Under acidic conditions, CBD can be transformed to delta9-tetrahydrocannabinol (THC) and other cannabinoids. It has been argued that this may occur also after oral administration in humans. However, the experimental conversion of CBD to THC and delta8-THC in simulated gastric fluid (SGF) is a highly artificial approach that deviates significantly from physiological conditions in the stomach; therefore, SGF does not allow an extrapolation to in vivo conditions...
2017: Cannabis and Cannabinoid Research
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