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https://www.readbyqxmd.com/read/28821005/anticonvulsant-effect-of-cannabidiol-in-the-pentylenetetrazole-model-pharmacological-mechanisms-electroencephalographic-profile-and-brain-cytokine-levels
#1
Luciano R Vilela, Isabel V Lima, Érica B Kunsch, Hyorrana Priscila P Pinto, Aline S de Miranda, Érica Leandro M Vieira, Antônio Carlos P de Oliveira, Marcio Flávio D Moraes, Antônio L Teixeira, Fabricio A Moreira
Cannabidiol (CBD), the main nonpsychotomimetic compound from Cannabis sativa, inhibits experimental seizures in animal models and alleviates certain types of intractable epilepsies in patients. Its pharmacological profile, however, is still uncertain. Here we tested the hypothesis that CBD anticonvulsant mechanisms are prevented by cannabinoid (CB1 and CB2) and vanilloid (TRPV1) receptor blockers. We also investigated its effects on electroencephalographic (EEG) activity and hippocampal cytokines in the pentylenetetrazole (PTZ) model...
August 15, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28814985/activation-of-endocannabinoid-receptor-2-as-a-mechanism-of-propofol-pretreatment-induced-cardioprotection-against-ischemia-reperfusion-injury-in-rats
#2
Hai-Jing Sun, Yan Lu, Hao-Wei Wang, Hao Zhang, Shuang-Ran Wang, Wen-Yun Xu, Hai-Long Fu, Xue-Ya Yao, Feng Yang, Hong-Bin Yuan
Propofol pretreatment before reperfusion, or propofol conditioning, has been shown to be cardioprotective, while its mechanism is unclear. The current study investigated the roles of endocannabinoid signaling in propofol cardioprotection in an in vivo model of myocardial ischemia/reperfusion (I/R) injury and in in vitro primary cardiomyocyte hypoxia/reoxygenation (H/R) injury. The results showed that propofol conditioning increased both serum and cell culture media concentrations of endocannabinoids including anandamide (AEA) and 2-arachidonoylglycerol (2-AG) detected by LC-MS/MS...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28805944/suppression-of-acute-and-anticipatory-nausea-by-peripherally-restricted-faah-inhibitor-in-animal-models-role-of-ppar%C3%AE-and-cb1-receptors
#3
Erin M Rock, Guillermo Moreno-Sanz, Cheryl L Limebeer, Gavin N Petrie, Roberto Angelini, Daniele Piomelli, Linda A Parker
To evaluate the ability of the peripherally restricted fatty acid amide hydrolase (FAAH) inhibitor, URB937 (cyclohexylcarbamic acid 3'-carbamoyl-6-hydroxybiphenyl-3-yl ester) to suppress acute and anticipatory nausea in rats, and to examine the pharmacological mechanism of such an effect. EXPERIMENTAL APPROACH: We investigated the potential of URB937 to reduce the establishment of lithium chloride (LiCl)-induced conditioned gaping (a model of acute nausea) and to reduce the expression of contextually elicited conditioned gaping (a model of anticipatory nausea) in rats...
August 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28799775/a-review-of-the-therapeutic-antitumor-potential-of-cannabinoids
#4
Višnja Bogdanović, Jasminka Mrdjanović, Ivana Borišev
OBJECTIVES: The aim of this review is to discuss cannabinoids from a preclinical and clinical oncological perspective and provide the audience with a concise, retrospective overview of the most significant findings concerning the potential use of cannabinoids in cancer treatment. METHODS: A literature survey of medical and scientific databases was conducted with a focus on the biological and medical potential of cannabinoids in cancer treatment. RESULTS: Cannabis sativa is a plant rich in more than 100 types of cannabinoids...
August 11, 2017: Journal of Alternative and Complementary Medicine: Research on Paradigm, Practice, and Policy
https://www.readbyqxmd.com/read/28799288/neuroprotective-activity-of-cannabinoid-receptor-2-against-oxidative-stress-and-apoptosis-in-rat-pups-having-experimentally-induced-congenital-hypothyroidism
#5
Mehmet Eray Alcigir, Halef Okan Dogan, Sevil Atalay Vural, Fatma Meriç Yilmaz
In this study, it was aimed to show the cannabinoid receptor-2 (CB2) role, which is a part of neuroprotective endocannabinoidal system, against increasing nitric oxide synthetase (iNOS, eNOS) levels and the apoptotic activity (caspase-3, caspase-9 and DNA in situ fragmentation) within the postnatal critical period in pups of pregnant rats with artificially induced maternal thyroid hormone (TH) deficiency. Each of the 3 groups established comprised 1 male and 2 female rats, and they were coupled. Their pups were used...
August 11, 2017: Developmental Neurobiology
https://www.readbyqxmd.com/read/28792725/pharmacology-of-cumyl-carboxamide-synthetic-cannabinoid-new-psychoactive-substances-nps-cumyl-bica-cumyl-pica-cumyl-5f-pica-cumyl-5f-pinaca-and-their-analogues
#6
Mitchell Longworth, Samuel D Banister, Rochelle Boyd, Richard C Kevin, Mark Connor, Iain S McGregor, Michael Kassiou
Synthetic cannabinoids (SC) are the largest class of new psychoactive substances (NPS), and are increasingly associated with serious adverse effects. The majority of SC NPS are 1,3-disubstituted indoles and indazoles featuring a diversity of subunits at the 1- and 3-positions. Most recently, cumyl-derived indole- and indazole-3-carboxamides have been detected by law enforcement agencies and by emergency departments. Herein we describe the synthesis, characterization, and pharmacology of SCs CUMYL-BICA, CUMYL-PICA, CUMYL-5F-PICA, CUMYL-PINACA, CUMYL-5F-PINACA, and related analogues...
August 11, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28782714/electroacupuncture-inhibits-nlrp3-inflammasome-activation-through-cb2-receptors-in-inflammatory-pain
#7
Fang Gao, Hong-Chun Xiang, Hong-Ping Li, Min Jia, Xiao-Li Pan, Hui-Lin Pan, Man Li
The therapeutic effect of electroacupuncture (EA) on inflammatory pain has been well recognized clinically. The inflammasome promotes the maturation of the inflammatory cytokines, and EA can stimulate cannabinoid CB2 receptors in inflamed tissues. In this study we investigated whether EA inhibits NLRP3 inflammasome activation through CB2 receptors and thus relieving inflammatory pain. Assay of Caspase-1 activity and western blotting revealed that complete Freund's adjuvant (CFA) injection activated the NLRP3 inflammasome in the skin tissue in rats, which was attenuated by EA treatment...
August 3, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28771321/activity-based-detection-of-consumption-of-synthetic-cannabinoids-in-authentic-urine-samples-using-a-stable-cannabinoid-reporter-system
#8
Annelies Cannaert, Florian Franz, Volker Auwärter, Christophe P Stove
Synthetic cannabinoids (SCs) continue to be the largest group of new psychoactive substances (NPS) monitored by the European Monitoring Center of Drugs and Drugs of Abuse (EMCDDA). The identification and subsequent prohibition of single SCs has driven clandestine chemists to produce analogues of increasing structural diversity, intended to evade legislation. That structural diversity, combined with the mostly unknown metabolic profiles of these new SCs, poses a big challenge for the conventional targeted analytical assays, as it is difficult to screen for 'unknown' compounds...
August 3, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28759851/relationship-of-carbohydrates-and-lignin-molecular-structure-spectral-profiles-to-nutrient-profile-in-newly-developed-oats-cultivars-and-barley-grain
#9
Luciana Louzada Prates, Basim Refat, Yaogeng Lei, Mariana Louzada-Prates, Peiqiang Yu
The objectives of this study were to quantify the chemical profile and the magnitude of differences in the oat and barley grain varieties developed by Crop Development Centre (CDC) in terms of Cornell Net Carbohydrate Protein System (CNCPS) carbohydrate sub-fractions: CA4 (sugars), CB1 (starch), CB2 (soluble fibre), CB3 (available neutral detergent fibre - NDF), and CC (unavailable carbohydrate); to estimate the energy values; to detect the lignin and carbohydrate (CHO) molecular structure profiles in CDC Nasser and CDC Seabiscuit oat and CDC Meredith barley grains by using Fourier transform infrared attenuated total reflectance (FTIR-ATR); to develop a model to predict nutrient supply based on CHO molecular profile...
July 24, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28759568/cannabinoid-receptor-2-63-rr-variant-is-independently-associated-with-severe-necroinflammation-in-hiv-hcv-coinfected-patients
#10
Caterina Sagnelli, Caterina Uberti-Foppa, Hamid Hasson, Giulia Bellini, Carmine Minichini, Stefania Salpietro, Emanuela Messina, Diletta Barbanotti, Marco Merli, Francesca Punzo, Nicola Coppola, Adriano Lazzarin, Evangelista Sagnelli, Francesca Rossi
OBJECTIVE: This is the first study to analyze the impact of the rs35761398 variant of the CNR2 gene leading to the substitution of GLN (Q) of codon 63 of the cannabinoid receptor 2 (CB2) with ARG (R) on the clinical presentation of chronic hepatitis in HIV/HCV coinfected patients. METHODS: Enrolled in this study were 166 consecutive HIV/HCV coinfected patients, naïve for HCV treatment. A pathologist unaware of the patients' condition graded liver fibrosis, necroinflammation (Ishak) and steatosis...
2017: PloS One
https://www.readbyqxmd.com/read/28758232/administrations-of-thalidomide-into-the-rostral-ventromedial-medulla-produce-antinociceptive-effects-in-a-rat-model-of-postoperative-pain
#11
Tieying Song, Xiaojing Ma, Pengyu Ma, Kunfeng Gu, Jianhui Zhao, Yunliang Yang, Bo Jiang, Yuxia Li, Chunping Wang
The rostral ventromedial medulla (RVM) is highly involved in pain signal transmissions. Previous studies have shown that thalidomide is anti-nociceptive. Thus, we evaluated the neurobiological mechanisms of thalidomide in the RVM in the regulation of postoperative pain. We used a rat model of postoperative pain to investigate the effects of intra-RVM thalidomide treatments on postoperative pain, and evaluate the role of cannabinoid receptors in the effects of intra-RVM thalidomide treatments on GABAergic neurotransmission in the RVM neurons...
July 31, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28754373/cannabidiol-disrupts-the-consolidation-of-specific-and-generalized-fear-memories-via-dorsal-hippocampus-cb1-and-cb2-receptors
#12
Cristina A J Stern, Thiago R da Silva, Ana M Raymundi, Camila P de Souza, Vinicius A Hiroaki-Sato, Luiza Kato, Francisco S Guimarães, Roberto Andreatini, Reinaldo N Takahashi, Leandro J Bertoglio
Pharmacological interventions able to modulate a fear memory while it is consolidated could have therapeutic value in tempering those maladaptively overconsolidated. Animal and human studies have shown the intensity of unconditioned stimulus delivered during fear conditioning influences qualitative and quantitative aspects of the memory to be established. By varying the shock intensity used for contextual pairing in rats, here we induced specific and more generalized long-term fear memories to investigate whether, how and where in the brain the cannabidiol (CBD; 3...
July 25, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28750813/methods-for-the-development-of-in-silico-gpcr-models
#13
Paula Morales, Dow P Hurst, Patricia H Reggio
The Reggio group has constructed computer models of the inactive and G-protein-activated states of the cannabinoid CB1 and CB2 receptors, as well as, several orphan receptors that recognize a subset of cannabinoid compounds, including GPR55 and GPR18. These models have been used to design ligands, mutations, and covalent labeling studies. The resultant second-generation models have been used to design ligands with improved affinity, efficacy, and subtype selectivity. Herein, we provide a guide for the development of GPCR models using the most recent orphan receptor studied in our lab, GPR3...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28750812/expression-and-nmr-structural-studies-of-isotopically-labeled-cannabinoid-receptor-type-ii
#14
Alexei Yeliseev, Klaus Gawrisch
Cannabinoid receptor type II (CB2) is an integral membrane protein with seven transmembrane helices that belongs to the large superfamily of rhodopsin-like G protein-coupled receptors. The CB2 is a part of the endocannabinoid system that plays a vital role in regulation of immune response, inflammation, pain, and other metabolic processes. Information about the structure and function of CB2 in cell membranes is essential for development of specific pharmaceuticals that target CB2 signaling. Methodology for recombinant expression, stable isotope labeling, purification, reconstitution into liposomes, and NMR characterization of functionally active CB2 is presented...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28750811/mass-spectrometry-analysis-of-human-cb2-cannabinoid-receptor-and-its-associated-proteins
#15
Zhao-Hui Song, Alyssa S Laun, Jian Cai
Studying the assemblies and dynamics of the complex formed by cannabinoid receptors and their associated proteins is important for understanding the molecular basis for the functions of these receptors. In the absence of the crystal structures of these macromolecular complexes, mass spectrometry is a sensitive technique that can be used to study cannabinoid receptors and their associated proteins. In this chapter, three aspects of the work are presented: (1) mass spectrometry analysis of the primary sequence of the human CB2 cannabinoid receptor after affinity chromatography purification of the receptor proteins, (2) functional proteomic analysis of CB2-associated proteins coimmunoprecipitated with CB2, and (3) chemical cross-linking and mass spectrometry analysis of CB2-G protein complex...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28747489/a-novel-selective-inverse-agonist-of-the-cb2-receptor-as-a-radiolabeled-tool-compound-for-kinetic-binding-studies
#16
Andrea Martella, Huub Sijben, Arne Rufer, Juergen Fingerle, Uwe Grether, Christoph Ullmer, Thomas Hartung, Ad IJzerman, Mario van der Stelt, Laura Heitman
The endocannabinoid system (ECS) and in particular the cannabinoid receptor 2 (CB2R), raised the interest of many medicinal chemistry programs for its therapeutic relevance in several (patho)physiological processes. However, the the physico-chemical properties of tool compounds for CB2R (e.g. the radioligand [(3)H]CP55,940) are not optimal, despite the research efforts in developing effective drugs to target this system. At the same time, the importance of drug-target binding kinetics is growing, as the kinetic binding profile of a ligand may provide important insights for the resulting in vivo efficacy...
July 26, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28747360/cannabinoids-and-the-kidney-effects-in-health-and-disease
#17
Frank Park, Praveen K Potukuchi, Hamid Moradi, Csaba P Kovesdy
Consumption of cannabis and various related products (cannabinoids) for both medicinal and recreational use is gaining popularity. Furthermore, regulatory changes are fostering a cultural shift towards increasing liberalization of cannabis use, thereby increasing the likelihood of even larger numbers of individuals being exposed in the future. The two different types of receptors (CB1 and CB2) that are activated by the pharmacologically active ingredients of cannabis are found in numerous tissues, including the kidneys...
July 26, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28743542/the-endocannabinoid-system-expression-in-the-female-reproductive-tract-is-modulated-by-estrogen
#18
J Maia, M Almada, A Silva, G Correia-da-Silva, N Teixeira, S I Sá, B M Fonseca
The endocannabinoid system (ECS) is involved in several physiological events that resulted in a growing interest in its modulation. Moreover, the uterine levels of anandamide (AEA), the major endocannabinoid, must be tightly regulated to create proper embryo implantation conditions. However, there are no evidences about the regulation of AEA in uterus by estrogen. Thus, the aim of this study is to elucidate whether estradiol benzoate (EB) and tamoxifen (TAM) administration to ovariectomized (OVX) rats can induce changes in the expression of cannabinoid receptors and AEA-metabolic enzymes in uterus by evaluating gene transcription and protein levels by qPCR, Western blot and immunohistochemistry...
July 22, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28740313/characterization-of-portuguese-honey-from-castelo-branco-region-according-to-their-pollen-spectrum-physicochemical-characteristics-and-mineral-contents
#19
Luís R Silva, Adriana Sousa, Marcos Taveira
The aim of this work was to evaluate the quality of 16 honey samples from Castelo Branco region (Portugal). Twelve are monofloral from Calluna vulgaris, Erica, Lavandula, Echium and Campanula. The mean values obtained for physicochemical parameters were: 3.82 pH; 16.80% moisture; 81.6°Brix; 0.21% ash; 357.6 μS cm(-1) electrical conductivity; 33.7 meq/kg free acidity; 5.7 meq/kg lactonic acidity; 39.3 meq/kg total acidity; 9.11 mg/kg HMF; 21.3 IN invertase and 9.0° Gothe for diastase activities. The results indicate a good quality, adequate processing, good maturity and freshness of honey...
July 2017: Journal of Food Science and Technology
https://www.readbyqxmd.com/read/28738764/neuroprotection-by-endo-cannabinoids-in-glaucoma-and-retinal-neurodegenerative-diseases
#20
Cinzia Rapino, Daniel Tortolani, Lucia Scipioni, Mauro Maccarrone
Emerging neuroprotective strategies are being explored to preserve the retina from degeneration, that occurs in eye pathologies like glaucoma, diabetic retinopathy, age-related macular degeneration, and retinitis pigmentosa. Incidentally, neuroprotection of retina is a defending mechanism designed to prevent or delay neuronal cell death, and to maintain neural function following an initial insult, thus avoiding loss of vision. Numerous studies have investigated potential neuroprotective properties of plant-derived phytocannabinoids, as well as of their endogenous counterparts collectively termed endocannabinoids (eCBs), in several degenerative diseases of the retina...
July 24, 2017: Current Neuropharmacology
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