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https://www.readbyqxmd.com/read/27915415/exendin-4-protects-huvecs-from-tunicamycin-induced-apoptosis-via-inhibiting-the-ire1a-jnk-caspase-3-pathway
#1
Li Wu, XiaoYing Liu, LinXi Wang, YanPing Wang, LiJing Wang, BinBin Guan, Zhou Chen, LiBin Liu
PURPOSE: The abnormal increase of apoptosis of endothelial cells induced by endoplasmic reticulum stress is a significant factor for vascular disease, especially for atherosclerosis. Protecting endothelial cells from endoplasmic reticulum stress is a crucial strategies to combate these diseases. The goal of this study was to explore the effect of Exendin-4, a glucagon-like peptide-1 receptor agonist, on tunicamycin-induced apoptosis in human umbilical vein endothelial cells. METHODS: All studies were performed in primary human umbilical vein endothelial cells treated with tunicamycin with or without Exendin-4 pretreatment...
December 3, 2016: Endocrine
https://www.readbyqxmd.com/read/27915399/naringenin-interferes-with-the-anti-diabetic-actions-of-pioglitazone-via-pharmacodynamic-interactions
#2
Hiroki Yoshida, Rika Tsuhako, Toshiyuki Atsumi, Keiko Narumi, Wataru Watanabe, Chihiro Sugita, Masahiko Kurokawa
Pioglitazone is a peroxisome proliferator-activated receptor gamma (PPARγ) full agonist and useful for the treatment of type 2 diabetes mellitus. Naringenin is a citrus flavonoid with anti-inflammatory actions, which has been shown to prevent obesity-related diseases and to activate PPARγ. The aim of this study was to investigate whether dietary naringenin affects the actions of pioglitazone. We administered naringenin (100 mg/kg) and pioglitazone (10 mg/kg) to Tsumura Suzuki Obese Diabetes (TSOD) mice for 4 weeks and then conducted an oral glucose tolerance test...
December 3, 2016: Journal of Natural Medicines
https://www.readbyqxmd.com/read/27915193/metabolic-fate-and-detectability-of-the-new-psychoactive-substances-2-4-bromo-2-5-dimethoxyphenyl-n-2-methoxyphenyl-methyl-ethanamine-25b-nbome-and-2-4-chloro-2-5-dimethoxyphenyl-n-2-methoxyphenyl-methyl-ethanamine-25c-nbome-in-human-and-rat-urine-by-gc-ms
#3
Achim T Caspar, Simon D Brandt, Andreas E Stoever, Markus R Meyer, Hans H Maurer
25B-NBOMe and 25C-NBOMe are potent 5-HT2A receptor agonists that have been associated with inducing hallucinogenic effects in drug users and severe intoxications. This paper describes the identification of their metabolites in rat and human urine by liquid chromatography (LC)-high resolution (HR)-MS/MS, the comparison of metabolite formation in vitro and in vivo and in different species, the general involvement of human cytochrome-P450 (CYP) isoenzymes on their metabolism steps, and their detectability by standard urine screening approaches (SUSAs) using GC-MS, LC-MS(n), or LC-HR-MS/MS...
November 27, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27915186/role-of-the-purinergic-signaling-in-epilepsy
#4
REVIEW
Marek Cieślak, Andrzej Wojtczak, Michał Komoszyński
Adenine nucleotides and adenosine are signaling molecules that activate purinergic receptors P1 and P2. Activation of A1 adenosine receptors has an anticonvulsant action, whereas activation of A2A receptors might initiate seizures. Therefore, a significant limitation to the use of A1 receptor agonists as drugs in the CNS might be their peripheral side effects. The anti-epileptic activity of adenosine is related to its increased concentration outside the cell. This increase might result from the inhibition of the equilibrative nucleoside transporters (ENTs)...
September 22, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27914999/dual-therapy-for-refractory-overactive-bladder-in-children-a-prospective-open-label-study
#5
Fannie Morin, Anne-Sophie Blais, Geneviève Nadeau, Katherine Moore, Lucie Genois, Stéphane Bolduc
PURPOSE: Mirabegron (β3-adrenoreceptor agonist) is a new molecule with a distinct mechanism of action from antimuscarinics. Combination therapy with solifenacin was recently studied in adult population. Our objective was to evaluate the efficacy and safety of mirabegron as add-on therapy, to treat urinary incontinence in children with idiopathic OAB, refractory/intolerant to antimuscarinics. MATERIALS AND METHODS: A prospective off-label study using add-on regimens of mirabegron was conducted with pediatric patients presenting no symptom improvement under intensive behavioural and medical therapies and/or significant side effects (S/E) on antimuscarinic dose escalation...
November 30, 2016: Journal of Urology
https://www.readbyqxmd.com/read/27914963/hypothermia-in-mouse-is-caused-by-adenosine-a1-and-a3-receptor-agonists-and-amp-via-three-distinct-mechanisms
#6
Jesse Lea Carlin, Shalini Jain, Elizabeth Gizewski, Tina C Wan, Dilip K Tosh, Cuiying Xiao, John A Auchampach, Kenneth A Jacobson, Oksana Gavrilova, Marc L Reitman
Small mammals have the ability to enter torpor, a hypothermic, hypometabolic state, allowing impressive energy conservation. Administration of adenosine or adenosine 5'-monophosphate (AMP) can trigger a hypothermic, torpor-like state. We investigated the mechanisms for hypothermia using telemetric monitoring of body temperature in wild type and receptor knock out (Adora1(-/-)-/-, Adora3(-/-)) mice. Confirming prior data, stimulation of the A3 adenosine receptor (AR) induced hypothermia via peripheral mast cell degranulation, histamine release, and activation of central histamine H1 receptors...
November 30, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27914945/effects-of-zacopride-a-moderate-ik1-channel-agonist-on-triggered-arrhythmia-and-contractility-in-human-ventricular-myocardium
#7
Mohammad T Elnakish, Benjamin D Canan, Ahmet Kilic, Peter J Mohler, Paul M L Janssen
Ventricular tachycardia is the leading cause of sudden arrhythmic death in the U.S. Recently, the moderate IK1 channel activator, zacopride, was shown to suppress triggered ventricular tachycardia in rats. Nonetheless, concerns were raised about the possibility of pro-arrhythmic activity after IK1 channel stimulation based on the promising anti-arrhythmic strategy of IK1 blockade in other animal models. Therefore, the goal of the current study was to investigate the ex-vivo effects of zacopride on triggered arrhythmia and contractility in ventricular human myocardium in order to validate data that was solely obtained from animal models...
November 30, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27914812/protective-effects-of-gomisin-n-against-hepatic-steatosis-through-ampk-activation
#8
Ye-Rang Yun, Ji-Hyun Kim, Ji Ha Kim, Myeong Ho Jung
Gomisin N (GN) is a phytochemical derived from Schisandra chinensis. It has been reported to exert a protective effect against hepatic steatosis by attenuating endoplasmic recticulum (ER) stress. However, the detailed mechanism by which GN inhibits hepatic steatosis remains to be elucidated. In this study, we examined whether GN activates AMP-activated protein kinase (AMPK) and exerts therapeutic effects on liver X receptor (LXR)- or palmitic acid (PA)-induced triglyceride (TG) accumulation in HepG2 cells. Furthermore, in vivo protective effects of GN against hepatic steatosis were assessed in high-fat diet (HFD)-induced obese mice...
November 30, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27914700/microvesicle-transfer-of-kinin-b1-receptors-is-a-novel-inflammatory-mechanism-in-vasculitis
#9
Robin Kahn, Maria Mossberg, Anne-Lie Ståhl, Karl Johansson, Ingrid Lopatko Lindman, Caroline Heijl, Mårten Segelmark, Matthias Mörgelin, L M Fredrik Leeb-Lundberg, Diana Karpman
During vasculitis, activation of the kinin system induces inflammation, whereby the kinin B1-receptor is expressed and activated after ligand binding. Additionally, activated blood cells release microvesicles into the circulation. Here we determined whether leukocyte-derived microvesicles bear B1-kinin receptors during vasculitis, and if microvesicles transfer functional B1-receptors to recipient cells, thus promoting inflammation. By flow cytometry, plasma from patients with vasculitis were found to contain high levels of leukocyte-derived microvesicles bearing B1-receptors...
November 30, 2016: Kidney International
https://www.readbyqxmd.com/read/27914516/leukotriene-b4-induces-emt-and-vimentin-expression-in-panc-1-pancreatic-cancer-cells-involvement-of-blt2-via-erk2-activation
#10
You Ri Kim, Mi Kyung Park, Gyeong Jin Kang, Hyun Ji Kim, Eun Ji Kim, Hyun Jung Byun, Moo-Yeol Lee, Chang Hoon Lee
Leukotriene B4 (LTB4) is a leukocyte chemoattractant and plays a major role controlling inflammatory responses including pancreatitis. LTB4 is known to be correlated with cancer progression. LTB4 induces keratin phosphorylation and reorganization by activating extracellular regulated kinase (ERK) in PANC-1 pancreatic cancer cell lines. However, the role of LTB4 in epithelial mesenchymal transition (EMT) and vimentin expression in pancreatic cancer cells is unknown. We examined whether LTB4 induces EMT and vimentin expression by Western blot, si-RNA, and RT-PCR...
December 2016: Prostaglandins, Leukotrienes, and Essential Fatty Acids
https://www.readbyqxmd.com/read/27914450/mechanisms-of-inflammatory-injury-of-renal-tubular-cells-in-a-cellular-model-of-pyelonephritis
#11
M A Morosanova, E Y Plotnikov, L D Zorova, I B Pevzner, V A Popkov, D N Silachev, S S Jankauskas, V A Babenko, D B Zorov
Previously, we have assembled a cellular model of pyelonephritis which contains a primary culture of renal tubular epithelial cells, mononuclear leukocytes, and bacterial lysate or lipopolysaccharide. After cocultivation of renal cells with leukocytes and bacterial lysate, proinflammatory changes were observed in the renal cells, followed by nitrosative and oxidative stress and cell death. The interaction of bacterial antigens not only with leukocytes, but also with epithelial cells of the renal tubules, was partially mediated by signaling pathways involving Toll-like receptors (TLR2 and TLR4)...
November 2016: Biochemistry. Biokhimii︠a︡
https://www.readbyqxmd.com/read/27914294/selective-agonism-of-mglu8-receptors-by-s-3-4-dicarboxyphenylglycine-does-not-affect-sleep-stages-in-the-rat
#12
María Cavas, Gianluigi Scesa, Mercedes Martín-López, José Francisco Navarro
BACKGROUND: Metabotropic glutamate receptors (mGlu) play a role in a number of physiological processes and behaviors, as well as in certain pathological conditions and diseases. New drugs targetting mGlu receptors are being developed with treatment purposes. Recent data indicates that glutamate is involved in sleep, and pharmacological manipulation of distinct subtypes of mGlu receptors affect sleep. Here the consequences of selective pharmacological agonism of mGlu8 receptor upon sleep and wakefulness are explored for the first time...
September 22, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27914122/design-synthesis-and-structure-activity-relationships-of-bavachinin-analogues-as-peroxisome-proliferator-activated-receptor-%C3%AE-agonists
#13
Guoxin Du, Yuanyuan Zhao, Li Feng, Zhuo Yang, Jiye Shi, Cheng Huang, Bo Li, Fujiang Guo, Weiliang Zhu, Yiming Li
Bavachinin analogues with systematic modifications at the A-, B-, and C-rings were designed, synthesized, and subjected to in vitro bioevaluation as peroxisome proliferator-activated receptor γ (PPAR-γ) agonists. In total, 30 molecules, including flavanone and flavone analogues, were evaluated by reporter gene assays for the PPAR-γ agonist activity. Preliminary structure-activity relationships of PPAR-γ agonist activity of bavachinin analogues were initially summarized and analogues 2b, 3, 4a, 4b, 11c, 11d, and 12b were found with higher PPAR-γ agonist activities compared to bavachinin...
December 3, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27914036/prolactin-regulatory-element-binding-protein-is-involved-in-suppression-of-the-adiponectin-gene-in-vivo
#14
X Z Zhang, H Imachi, J Y Lyu, K Fukunaga, S Sato, T Ibata, T Kobayashi, T Yoshimoto, F Kikuchi, T Dong, K Murao
PURPOSE: Prolactin regulatory element-binding protein (PREB), a member of the WD-repeat protein family, has been recognized as a transcriptional factor that regulates prolactin promoter activity in the anterior pituitary of rats. PREB is expressed not only in the pituitary but also in various other tissues, including the adipose tissue. Previous studies have shown that PREB acts as a transcriptional regulator and suppresses the expression of the adiponectin gene in cultured 3T3L1 preadipocytes...
December 2, 2016: Journal of Endocrinological Investigation
https://www.readbyqxmd.com/read/27914011/activation-of-alpha-7-nicotinic-acetylcholine-receptor-reduces-brain-edema-in-mice-with-ischemic-stroke-and-bone-fracture
#15
Dingquan Zou, Man Luo, Zhenying Han, Lei Zhan, Wan Zhu, Shuai Kang, Chen Bao, Zhao Li, Jeffrey Nelson, Rui Zhang, Hua Su
Stroke is an important risk factor for bone fracture. We showed previously that bone fracture at the acute stage of ischemic stroke worsens, and activation of α-7 nicotinic acetylcholine receptor (α-7 nAchR) improves, stroke recovery by attenuating inflammation. We hypothesized that activation of α-7 nAchR also improves the blood-brain barrier (BBB) integrity. Permanent distal middle cerebral artery occlusion (pMCAO) was performed on C57BL/6J mice followed by tibia fracture 1 day later. Mice were treated with 0...
December 2, 2016: Molecular Neurobiology
https://www.readbyqxmd.com/read/27913935/regulation-of-contractile-responses-of-vascular-smooth-muscle-cells-under-conditions-of-hypoxia-reoxygenation
#16
S V Gusakova, Yu G Birulina, L V Smagliy, I V Kovalev, I V Petrova, A V Nosarev, S N Orlov
We analyzed the effects of hypoxia and reoxygenation on changes in contractile activity in rat aortic smooth muscles. Both hypoxia and reoxygenation induced relaxation of smooth muscle cells precontracted with high-potassium Krebs solution (30 mM KCl) or α1-adrenoceptor agonist phenylephrine. Vasodilation resulted from enhancement of potassium permeability of smooth muscle cell membranes caused by activation of voltage-gated potassium channels (triggered by both precontracting agents) or by opening of ATP-sensitive potassium channels (phenylephrine)...
December 2, 2016: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/27913621/identification-of-hepatic-lysophosphatidylcholine-acyltransferase-3-as-a-novel-target-gene-regulated-by-peroxisome-proliferator-activated-receptor-%C3%AE
#17
Amar Bahadur Singh, Jingwen Liu
Peroxisome proliferator-activated receptor δ (PPARδ) regulates many genes involved in lipid metabolism. Hepatic lysophosphatidylcholine acyltransferase 3 (LPCAT3) has critical functions in triglycerides transport and ER stress response due to its unique ability to catalyze the incorporation of polyunsaturated fatty acids into phospholipids. Previous studies identified liver X receptor as the transcription factor controlling LPCAT3 expression in mouse liver tissue. Here we show that the hepatic LPCAT3 gene is transcriptionally regulated by PPARδ...
December 2, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27913575/lowest-glucose-variability-and-hypoglycemia-are-observed-with-the-combination-of-a-glp-1-receptor-agonist-and-basal-insulin-variation-study
#18
Harpreet S Bajaj, Karri Venn, Chenglin Ye, Avril Patrick, Shivani Kalra, Hasnain Khandwala, Nadeem Aslam, David Twum-Barima, Ronnie Aronson
OBJECTIVE: There is a dearth of published literature comparing glucose variability (GV) between different insulin regimens in type 2 diabetes. This cohort study compares GV using continuous glucose monitoring (CGM) in patients with well-controlled type 2 diabetes using four common insulin regimens: basal insulin + oral drugs (BO), basal insulin + glucagon-like peptide 1 receptor agonist (GLP-1 RA) (BGLP), premixed insulin (PM), and basal-bolus insulin (BB). RESEARCH DESIGN AND METHODS: Consecutive patients from three endocrinology clinics who met study criteria-type 2 diabetes, age 18 to 80 years, BMI ≤ 45 kg/m(2), stable insulin regimen for a minimum of 6 months, and stable A1C value ≤7...
December 2, 2016: Diabetes Care
https://www.readbyqxmd.com/read/27913423/bronchodilatory-effect-of-deep-inspiration-in-freshly-isolated-sheep-lungs
#19
William D Wong, Lu Wang, Peter D Paré, Chun Y Seow
Taking a big breath is known to reverse bronchoconstriction induced by bronchochallenge in healthy subjects; this bronchodilatory effect of deep inspiration (DI) is diminished in asthmatics. The mechanism underlying the DI effect is not clear. Observations from experiments using isolated airway smooth muscle (ASM) preparations and airway segments suggest that straining of ASM due to DI could lead to bronchodilation, possibly due to strain-induced reduction in ASM contractility. However, factors external to the lung cannot be excluded as potential causes for the DI effect...
December 2, 2016: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/27913408/neurophysiological-mechanisms-of-cortical-plasticity-impairments-in-schizophrenia-and-modulation-by-the-nmda-receptor-agonist-d-serine
#20
Joshua T Kantrowitz, Michael L Epstein, Odeta Beggel, Stephanie Rohrig, Jonathan M Lehrfeld, Nadine Revheim, Nayla P Lehrfeld, Jacob Reep, Emily Parker, Gail Silipo, Merav Ahissar, Daniel C Javitt
Schizophrenia is associated with deficits in cortical plasticity that affect sensory brain regions and lead to impaired cognitive performance. Here we examined underlying neural mechanisms of auditory plasticity deficits using combined behavioural and neurophysiological assessment, along with neuropharmacological manipulation targeted at the N-methyl-D-aspartate type glutamate receptor (NMDAR). Cortical plasticity was assessed in a cohort of 40 schizophrenia/schizoaffective patients relative to 42 healthy control subjects using a fixed reference tone auditory plasticity task...
December 2016: Brain: a Journal of Neurology
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