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https://www.readbyqxmd.com/read/29238589/cannabidiol-restores-intestinal-barrier-dysfunction-and-inhibits-the-apoptotic-process-induced-by-clostridium-difficile-toxin-a-in-caco-2-cells
#1
Stefano Gigli, Luisa Seguella, Marcella Pesce, Eugenia Bruzzese, Alessandra D'Alessandro, Rosario Cuomo, Luca Steardo, Giovanni Sarnelli, Giuseppe Esposito
Background: Clostridium difficile toxin A is responsible for colonic damage observed in infected patients. Drugs able to restore Clostridium difficile toxin A-induced toxicity have the potential to improve the recovery of infected patients. Cannabidiol is a non-psychotropic component of Cannabis sativa, which has been demonstrated to protect enterocytes against chemical and/or inflammatory damage and to restore intestinal mucosa integrity. Objective: The purpose of this study was to evaluate (a) the anti-apoptotic effect and (b) the mechanisms by which cannabidiol protects mucosal integrity in Caco-2 cells exposed to Clostridium difficile toxin A...
December 2017: United European Gastroenterology Journal
https://www.readbyqxmd.com/read/29238581/a-spicy-status-synthetic-cannabinoid-spice-use-and-new-onset-refractory-status-epilepticus-a-case-report-and-review-of-the-literature
#2
Marc-Alain Babi, Christopher P Robinson, Carolina B Maciel
Synthetic cannabinoids refer to a wide variety of chemicals engineered to bind cannabinoid receptors (CB1 and CB2) and mimic the effects of delta-9-tetrahydrocanabinol. The potential for severe toxicity and limited in vivo data make synthetic cannabinoid intake an important public health and safety concern. Neurologic toxidromes associated with their use include mental status changes, panic attacks, memory distortions, acute psychosis (e.g. paranoia, delusional thoughts), disorganized behavior, and suicidal and homicidal thoughts...
2017: SAGE Open Medical Case Reports
https://www.readbyqxmd.com/read/29237478/am404-paracetamol-metabolite-prevents-prostaglandin-synthesis-in-activated-microglia-by-inhibiting-cox-activity
#3
Soraya Wilke Saliba, Ariel R Marcotegui, Ellen Fortwängler, Johannes Ditrich, Juan Carlos Perazzo, Eduardo Muñoz, Antônio Carlos Pinheiro de Oliveira, Bernd L Fiebich
BACKGROUND: N-arachidonoylphenolamine (AM404), a paracetamol metabolite, is a potent agonist of the transient receptor potential vanilloid type 1 (TRPV1) and low-affinity ligand of the cannabinoid receptor type 1 (CB1). There is evidence that AM404 exerts its pharmacological effects in immune cells. However, the effect of AM404 on the production of inflammatory mediators of the arachidonic acid pathway in activated microglia is still not fully elucidated. METHOD: In the present study, we investigated the effects of AM404 on the eicosanoid production induced by lipopolysaccharide (LPS) in organotypic hippocampal slices culture (OHSC) and primary microglia cultures using Western blot, immunohistochemistry, and ELISA...
December 13, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29232588/bioactive-products-from-singlet-oxygen-photooxygenation-of-cannabinoids
#4
Ahmed Galal Osman, Khaled M Elokely, Vivek K Yadav, Paulo Carvalho, Mohamed Radwan, Desmond Slade, Waseem Gul, Shabana Khan, Olivia R Dale, Afeef S Husni, Michael L Klein, Stephen J Cutler, Samir A Ross, Mahmoud A ElSohly
Photooxygenation of Δ8 tetrahydrocannabinol (Δ8-THC), Δ9 tetrahydrocannabinol (Δ9-THC), Δ9 tetrahydrocannabinolic acid (Δ9-THCA) and some derivatives (acetate, tosylate and methyl ether) yielded 24 oxygenated derivatives, 18 of which were new and 6 were previously reported, including allyl alcohols, ethers, quinones, hydroperoxides, and epoxides. Testing these compounds for their modulatory effect on cannabinoid receptors CB1 and CB2 led to the identification of 7 and 21 as CB1 partial agonists with Ki values of 0...
November 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29229226/novel-sulfenamides-and-sulfonamides-based-on-pyridazinone-and-pyridazine-scaffolds-as-cb1-receptor-ligand-antagonists
#5
Gabriele Murineddu, Francesco Deligia, Giulio Ragusa, Laura García-Toscano, María Gómez-Cañas, Battistina Asproni, Valentina Satta, Elena Cichero, Ruth Pazos, Paola Fossa, Giovanni Loriga, Javier Fernández-Ruiz, Gerard A Pinna
A series of sulfenamide and sulfonamide derivatives was synthesized and evaluated for the affinity at CB1 and CB2 receptors. The N-bornyl-S-(5,6-di-p-tolylpyridazin-3-yl)-sulfenamide, compound 11, displayed good affinity and high selectivity for CB1 receptors (Ki values of 44.6 nM for CB1 receptors and >40 μM for CB2 receptors, respectively). The N-isopinocampheyl-sulfenamide 12 and its sulfonamide analogue 22 showed similar selectivity for CB1 receptors with Ki values of 75.5 and 73.2 nM, respectively...
December 2, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29225042/endogenous-dopamine-and-endocannabinoid-signaling-mediate-cocaine-induced-reversal-of-ampar-synaptic-potentiation-in-the-nucleus-accumbens-shell
#6
Anna E Ingebretson, Matthew C Hearing, Ethan D Huffington, Mark J Thomas
Repeated exposure to drugs of abuse alters the structure and function of neural circuits mediating reward, generating maladaptive plasticity in circuits critical for motivated behavior. Within meso-corticolimbic dopamine circuitry, repeated exposure to cocaine induces progressive alterations in AMPAR-mediated glutamatergic synaptic transmission. During a 10-14 day period of abstinence from cocaine, AMPAR signaling is potentiated at synapses on nucleus accumbens (NAc) medium spiny neurons (MSNs), promoting a state of heightened synaptic excitability...
December 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29225040/differential-neuromodulatory-role-of-endocannabinoids-in-the-rodent-trigeminal-sensory-ganglion-and-cerebral-cortex-relevant-to-pain-processing
#7
Francesca Eroli, Inge C M Loonen, Arn M J M van den Maagdenberg, Else A Tolner, Andrea Nistri
Endocannabinoids are suggested to control pain, even though their clinical use is not fully validated and the underlying mechanisms are incompletely understood. To clarify the targets of endocannabinoid actions, we studied how activation of the endocannabinoid CB1 receptor (CB1R) affects neuronal responses in two in vitro preparations of rodents, namely the trigeminal sensory ganglion (TG) in culture and a coronal slice of the cerebral cortex. On TG small-medium size neurons, we tested whether submicromolar concentrations of the endogenous CB1R agonist anandamide (AEA) modulated inhibitory GABAA receptors and excitatory ATP-gated P2X3 receptors...
December 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29218862/the-presence-and-distribution-of-cannabinoid-type-1-and-2-receptors-in-the-mandibular-gland-the-influence-of-different-physical-forms-of-diets-on-their-expression-in-piglets
#8
C Pirino, M G Cappai, M Maranesi, D Tomassoni, A Giontella, W Pinna, C Boiti, J Kamphues, C Dall'Aglio
We explored the expression and cell type distribution of cannabinoid receptors type 1 (CB1) and cannabinoid receptors type 2 (CB2) in the mandibular glands of pigs in relation to different physical forms of the diet. Thirty-two crossbred growing pigs (ages 5-6 weeks) were randomly allotted to four experimental groups (eight pigs/group) and fed four different physical types of the same diet for 4 weeks: finely ground pellet (FP), coarsely ground meal (CM), coarsely ground pellet (CP) and coarsely ground extruded (CE) with dMEAN of 0...
December 7, 2017: Journal of Animal Physiology and Animal Nutrition
https://www.readbyqxmd.com/read/29216450/endocannabinoid-actions-on-cortical-terminals-orchestrate-local-modulation-of-dopamine-release-in-the-nucleus-accumbens
#9
Yolanda Mateo, Kari A Johnson, Dan P Covey, Brady K Atwood, Hui-Ling Wang, Shiliang Zhang, Iness Gildish, Roger Cachope, Luigi Bellocchio, Manuel Guzmán, Marisela Morales, Joseph F Cheer, David M Lovinger
Dopamine (DA) transmission mediates numerous aspects of behavior. Although DA release is strongly linked to firing of DA neurons, recent developments indicate the importance of presynaptic modulation at striatal dopaminergic terminals. The endocannabinoid (eCB) system regulates DA release and is a canonical gatekeeper of goal-directed behavior. Here we report that extracellular DA increases induced by selective optogenetic activation of cholinergic neurons in the nucleus accumbens (NAc) are inhibited by CB1 agonists and eCBs...
December 6, 2017: Neuron
https://www.readbyqxmd.com/read/29205751/lh-21-and-abn-cbd-improve-%C3%AE-cell-function-in-isolated-human-and-mouse-islets-through-gpr55-dependent-and-independent-signalling
#10
Inmaculada Ruz-Maldonado, Attilio Pingitore, Bo Liu, Patricio Atanes, Guo Cai Huang, David Baker, Francisco José Alonso, Francisco Javier Bermúdez-Silva, Shanta J Persaud
AIMS: CB1 and GPR55 are GPCRs expressed by islet β-cells. Pharmacological compounds have been used to investigate their function, but off-target effects of ligands have been reported. This study examined the effects of Abn-CBD (GPR55 agonist) and LH-21 (CB1 antagonist) on human and mouse islet function, and islets from GPR55-/- mice were used to determine signalling via GPR55. MATERIALS AND METHODS: Islets isolated from human organ donors and mice were incubated in the absence or presence of Abn-CBD or LH-21 and insulin secretion, [Ca2+ ]i, cAMP, apoptosis, β-cell proliferation and CREB and AKT phosphorylation were examined by standard techniques...
December 5, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29204742/target-and-tissue-selectivity-prediction-by-integrated-mechanistic-pharmacokinetic-target-binding-and-quantitative-structure-activity-modeling
#11
Anna H C Vlot, Wilhelmus E A de Witte, Meindert Danhof, Piet H van der Graaf, Gerard J P van Westen, Elizabeth C M de Lange
Selectivity is an important attribute of effective and safe drugs, and prediction of in vivo target and tissue selectivity would likely improve drug development success rates. However, a lack of understanding of the underlying (pharmacological) mechanisms and availability of directly applicable predictive methods complicates the prediction of selectivity. We explore the value of combining physiologically based pharmacokinetic (PBPK) modeling with quantitative structure-activity relationship (QSAR) modeling to predict the influence of the target dissociation constant (K D) and the target dissociation rate constant on target and tissue selectivity...
December 4, 2017: AAPS Journal
https://www.readbyqxmd.com/read/29203303/interactive-effects-of-morphine-and-nicotine-on-memory-function-depend-on-the-central-amygdala-cannabinoid-cb1-receptor-function-in-rats
#12
Fatemeh Tirgar, Ameneh Rezayof, Sakineh Alijanpour, Nima Yazdanbakhsh
The present study investigated the possible involvement of the central amygdala (CeA) cannabinoid receptors type-1 (CB1Rs) in the interactive effects of morphine and nicotine on memory formation in a passive avoidance learning task. Our results showed that systemic administration of morphine (3 and 6mg/kg, s.c.) immediately after training phase impaired memory consolidation and induced amnesia. Administration of nicotine (0.3 and 0.6mg/kg, s.c.) before testing phase significantly restored morphine-induced amnesia, suggesting a cross state-dependent learning between morphine and nicotine...
December 1, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29196726/emergence-of-ba9-genotype-of-human-respiratory-syncytial-virus-subgroup-b-in-china-from-2006-to-2014
#13
Jinhua Song, Huiling Wang, Jing Shi, Aili Cui, Yanzhi Huang, Liwei Sun, Xingyu Xiang, Chaofeng Ma, Pengbo Yu, Zifeng Yang, Qi Li, Teresa I Ng, Yan Zhang, Rongbo Zhang, Wenbo Xu
A study was conducted to investigate the circulation of HRSV subgroup B (HRSVB) in China in recent years. HRSVB sequences from 365 samples collected in 1991, 2004 and 2008-2014 in China, together with 332 Chinese HRSVB sequences obtained from GenBank were analyzed to determine the geographic and yearly distribution of HRSVB. Phylogenetic analysis revealed these HRSVB sequences clustered into 4 genotypes with different frequencies: BA (83%), CB1 (11%), SAB (3.0%) and GB3 (0.7%). Between 2005 and 2013, there was a co-circulation of BA and non-BA genotypes in China...
December 1, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29192125/endocannabinoid-specific-impairment-in-synaptic-plasticity-in-striatum-of-huntington-s-disease-mouse-model
#14
Marja D Sepers, Amy Smith-Dijak, Jeff LeDue, Karolina Kolodziejczyk, Ken Mackie, Lynn A Raymond
Huntington's disease (HD) is an inherited neurodegenerative disease affecting predominantly striatum and cortex that results in motor and cognitive disorders. Prior to a motor phenotype, animal models of HD show aberrant cortical-striatal glutamate signaling. Here, we tested synaptic plasticity of cortical excitatory synapses onto striatal spiny projection neurons (SPNs) early in the YAC128 mouse model of HD. High frequency stimulation-induced long-term depression, mediated by the endocannabinoid anandamide and cannabinoid receptor 1 (CB1), was significantly attenuated in male and female YAC128 SPNs...
November 30, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29187590/selective-cannabinoid-2-receptor-stimulation-reduces-tubular-epithelial-cell-damage-following-renal-ischemia-reperfusion-injury
#15
Jeffrey D Pressly, Suni M Mustafa, Ammaar Abidi, Sahar Alghamdi, Pankaj Pandey, Kuldeep K Roy, Robert Doerksen, Bob M Moore, Frank Park
Ischemia-reperfusion injury (IRI) is a common cause of acute kidney injury (AKI), which is an increasing problem in the clinic and has been associated with increased rates of mortality. Currently, therapies to treat AKI are not available, so identification of new targets which, upon diagnosis of AKI, can be modulated to ameliorate renal damage is essential. In this study, a novel cannabinoid receptor 2 (CB2) agonist, SMM-295, was designed, synthesized, and tested in vitro and in silico. In vivo testing of the CB2 agonist was performed using a mouse model of bilateral IRI, which is a common model to mimic human AKI...
November 29, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29176975/targeting-cannabinoid-signaling-in-the-immune-system-high-ly-exciting-questions-possibilities-and-challenges
#16
REVIEW
Attila Oláh, Zoltán Szekanecz, Tamás Bíró
It is well known that certain active ingredients of the plants of Cannabis genus, i.e., the "phytocannabinoids" [pCBs; e.g., (-)-trans-Δ9-tetrahydrocannabinol (THC), (-)-cannabidiol, etc.] can influence a wide array of biological processes, and the human body is able to produce endogenous analogs of these substances ["endocannabinoids" (eCB), e.g., arachidonoylethanolamine (anandamide, AEA), 2-arachidonoylglycerol (2-AG), etc.]. These ligands, together with multiple receptors (e.g., CB1 and CB2 cannabinoid receptors, etc...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/29171003/inhibition-of-monoacylglycerol-lipase-terminates-diazepam-resistant-status-epilepticus-in-mice-and-its-effects-are-potentiated-by-a-ketogenic-diet
#17
Gaetano Terrone, Alberto Pauletti, Alessia Salamone, Massimo Rizzi, Bianca R Villa, Luca Porcu, Mark J Sheehan, Edward Guilmette, Christopher R Butler, Justin R Piro, Tarek A Samad, Annamaria Vezzani
OBJECTIVE: Status epilepticus (SE) is a life-threatening and commonly drug-refractory condition. Novel therapies are needed to rapidly terminate seizures to prevent mortality and morbidity. Monoacylglycerol lipase (MAGL) is the key enzyme responsible for the hydrolysis of the endocannabinoid 2-arachidonoylglycerol (2-AG) and a major contributor to the brain pool of arachidonic acid (AA). Inhibiting of monoacylglycerol lipase modulates synaptic activity and neuroinflammation, 2 mediators of excessive neuronal activation underlying seizures...
November 24, 2017: Epilepsia
https://www.readbyqxmd.com/read/29169961/the-cannabinoid-transporter-inhibitor-omdm-2-reduces-social-interaction-further-evidence-for-transporter-mediated-endocannabinoid-release
#18
Alexandre Seillier, Andrea Giuffrida
Experimental evidence suggests that the transport of endocannabinoids might work bi-directionally. Accordingly, it is possible that pharmacological blockade of the latter affects not only the re-uptake, but also the release of endocannabinoids, thus preventing them from stimulating CB1 receptors. We used biochemical, pharmacological, and behavioral approaches to investigate the effects of the transporter inhibitor OMDM-2 on social interaction, a behavioral assay that requires activation of CB1 receptors. The underlying mechanisms of OMDM-2 were compared with those of the Fatty Acid Amide Hydrolase (FAAH) inhibitor URB597...
November 21, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29169951/regulation-of-noradrenergic-and-serotonergic-systems-by-cannabinoids-relevance-to-cannabinoid-induced-effects
#19
REVIEW
Aitziber Mendiguren, Erik Aostri, Joseba Pineda
The cannabinoid system is composed of Gi/o protein-coupled cannabinoid type 1 receptor (CB1) and cannabinoid type 2 (CB2) receptor and endogenous compounds. The CB1 receptor is widely distributed in the central nervous system (CNS) and it is involved in the regulation of common physiological functions. At the neuronal level, the CB1 receptor is mainly placed at GABAergic and glutamatergic axon terminals, where it modulates excitatory and inhibitory synapses. To date, the involvement of CB2 receptor in the regulation of neurotransmission in the CNS has not been clearly shown...
November 20, 2017: Life Sciences
https://www.readbyqxmd.com/read/29168269/adolescent-ethanol-intake-alters-cannabinoid-type-1-receptor-localization-in-astrocytes-of-the-adult-mouse-hippocampus
#20
Itziar Bonilla-Del Rίo, Nagore Puente, Sara Peñasco, Irantzu Rico, Ana Gutiérrez-Rodrίguez, Izaskun Elezgarai, Almudena Ramos, Leire Reguero, Inmaculada Gerrikagoitia, Brian R Christie, Patrick Nahirney, Pedro Grandes
Cannabinoid type-1 (CB1 ) receptors are widely distributed in the brain and play important roles in astrocyte function and the modulation of neuronal synaptic transmission and plasticity. However, it is currently unknown how CB1 receptor expression in astrocytes is affected by long-term exposure to stressors. Here we examined CB1 receptors in astrocytes of ethanol (EtOH)-exposed adolescent mice to determine its effect on CB1 receptor localization and density in adult brain. 4-8-week-old male mice were exposed to 20 percent EtOH over a period of 4 weeks, and receptor localization was examined after 4 weeks in the hippocampal CA1 stratum radiatum by pre-embedding immunoelectron microscopy...
November 23, 2017: Addiction Biology
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