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Pharmacology

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https://www.readbyqxmd.com/read/28521325/effect-of-high-salt-diet-on-age-related-high-blood-pressure-and-hypothalamic-redox-signaling
#1
Bilgen Basgut, Melissa A Whidden, Nataliya Kirichenko, Mary Woods, Benedek Erdos, Philip J Scarpace, Nihal Tümer
AIM: The aim of this study was to investigate the effect of a high salt (HS) diet on age-related changes in blood pressure (BP) and the possible role played by regulatory central mechanisms. METHODS: Young (5 months) and old (27 months) male Fischer 344 × Brown Norway (F344/BN) rats were fed standard chow or 8% HS diet for 12 days. BP and heart rate (HR) were measured by telemetry. RESULTS: Mean arterial BP (MAP) was significantly elevated in old rats during the day and night when compared with young animals...
May 19, 2017: Pharmacology
https://www.readbyqxmd.com/read/28494454/acceleration-of-apoptosis-by-extracellular-basic-ph-in-a-3d-human-skin-equivalent-system
#2
Gunhyuk Park, Dal-Seok Oh, Yong-Ung Kim, Moon Ki Park
Previously, we have shown that extracellular basic pH plays a significant role in both the direct and indirect regulation of cellular processes in a wound; this in turn affects the wound-healing process. Several studies have demonstrated the importance of apoptosis modulation in the wound-healing process, especially in removing inflammatory cells and in inhibiting scar formation. However, the effects of extracellular basic pH on wound healing-related skin damage are yet to be examined. Therefore, we investigated the induction of accelerated apoptosis by extracellular basic pH in skin...
May 12, 2017: Pharmacology
https://www.readbyqxmd.com/read/28494448/effects-of-cyp2c19-variants-on-fluoxetine-metabolism-in-vitro
#3
Ping Fang, Jia-Yang He, Ai-Xia Han, Tian Lan, Da-Peng Dai, Jian-Ping Cai, Guo-Xin Hu
AIMS: CYP2C19 is an important member of the cytochrome P450 enzyme superfamily. We recently identified 31 CYP2C19 alleles in the Han Chinese population. The aim of this study was to assess the catalytic activities of these allelic isoforms and their effects on the metabolism of fluoxetine in vitro. METHODS: The wild-type and 30 CYP2C19 variants were expressed in insect cells and each variant was characterized using fluoxetine as the substrate. Reactions were performed at 37°C with 20-1,000 µmol/L substrate for 30 min...
May 12, 2017: Pharmacology
https://www.readbyqxmd.com/read/28501872/a-mechanism-study-underlying-the-protective-effects-of-cyclosporine-a-on-lung-ischemia-reperfusion-injury
#4
Jian''an Li, Zhongya Yan, Qianjin Fang
AIM: This study is aimed at validating the hypothesis that administration of cyclosporine-A (CsA) would be protective in lung ischemia-reperfusion (I/R) injury and in exploring the underlying mechanism. METHODS: Rabbits were divided into 4 groups: the control, sham operation, I/R, and I/R with CsA treatment. Flow cytometry was used to measure the mitochondrial membrane potential. Laser scanning confocal microscope was used to analyze mitochondrion permeability transition pore (MPTP)...
May 10, 2017: Pharmacology
https://www.readbyqxmd.com/read/28486232/osthole-a-coumadin-analog-from-cnidium-monnieri-l-cusson-ameliorates-nucleus-pulposus-induced-radicular-inflammatory-pain-by-inhibiting-the-activation-of-extracellular-signal-regulated-kinase-in-rats
#5
Hai-Xuan Wu, Yi-Min Wang, Hui Xu, Ming Wei, Qiu-Lan He, Mei-Na Li, Lai-Bao Sun, Ming-Hui Cao
AIM: This study was aimed at assessing the role of extracellular signal regulated kinase (ERK) in mechanical allodynia resulting from lumbar disc herniation (LDH) and exploring the osthole's anti-nociceptive effect on ERK activation. METHODS: Radicular pain was generated by applying nucleus pulposus (NP) to the L5 dorsal root ganglion (DRG). Allodynia was measured using Von Frey filaments to calculate the mechanical pain threshold. Phosphorylated ERK and total ERK protein in the lumbar spinal dorsal horn was detected by using the Western blot technique...
May 10, 2017: Pharmacology
https://www.readbyqxmd.com/read/28482342/pioglitazone-attenuates-injury-induced-neointima-formation-in-mouse-femoral-artery-partially-through-the-activation-of-amp-activated-protein-kinase
#6
Islam Osman, Arwa Fairaq, Lakshman Segar
BACKGROUND/AIMS: Pioglitazone (PIO), an antidiabetic drug, has been shown to attenuate vascular smooth muscle cell (VSMC) proliferation, which is a major event in atherosclerosis and restenosis after angioplasty. Till date, the likely contributory role of AMP-activated protein kinase (AMPK) toward PIO inhibition of VSMC proliferation has not been examined in vivo. This study is aimed at determining whether pharmacological inhibition of AMPK would prevent the inhibitory effect of PIO on neointima formation in a mouse model of arterial injury...
May 9, 2017: Pharmacology
https://www.readbyqxmd.com/read/28467994/making-the-case-for-power-abuse-disorder-as-a-nosologic-entity
#7
Gerald Zernig, Christoph Hiemke
The development of societies and cultures arguably is based on the ability of human primates to form hierarchies in which some individuals acquire and wield power, that is, control resources and influence and control the behavior of their conspecifics. In the following, we focus on the type of human primate power wielding that (a) harms and (b) produces excessive negative emotions in (1) the victim(s) of the power wielder and (2) the power wielder her/himself. If such a harmful behavior of the power wielder is not accompanied by an ethically justifiable benefit for the involved human primate groups, it can be considered "power abuse...
May 4, 2017: Pharmacology
https://www.readbyqxmd.com/read/28467992/rutin-attenuates-oxidative-stress-and-proinflammatory-cytokine-level-in-adjuvant-induced-rheumatoid-arthritis-via-inhibition-of-nf-%C3%AE%C2%BAb
#8
Chong-Ling Sun, Jun Wei, Li-Qi Bi
The present study was intended to elucidate the effect of rutin, a flavonoid, on arthritis in complete Freund's adjuvant-induced arthritic rats. The present study showed that more pronounced effect has been observed in the case of 15 mg/kg dose of rutin, with significant reduction in paw diameter together with positive modulation of hematological parameters as compared to 2 other tested doses. A significant upsurge in the level of superoxide dismutase, glutathione peroxidase and glutathione were observed together with decrease in the level of malondialdehyde after treatment with rutin in a dose-dependent manner...
May 4, 2017: Pharmacology
https://www.readbyqxmd.com/read/28441657/involvement-of-the-multidrug-and-toxic-compound-extrusion-transporter-in-testosterone-release-from-cultured-pig-leydig-cells
#9
Mitsuhiro Goda, Kana Oda, Atsuko Oda, Naoki Kobayashi, Masato Otsuka
Testosterone is considered to be released from Leydig cells via passive diffusion because of its hydrophobicity; however, the exact mechanism underlying testosterone secretion and the transporter involved are both unknown. Multidrug and toxic compound extrusion (MATE) transporters are predominantly found in the kidneys and liver and are thought to function in the elimination of metabolic organic cations during the final step of excretion in the kidney. In contrast, mMATE2 has been shown to be predominantly expressed in testicular Leydig cells...
April 26, 2017: Pharmacology
https://www.readbyqxmd.com/read/28346918/5-ht1a-receptors-mediate-analgesia-induced-by-emulsified-sevoflurane-in-thermal-nociception-but-have-little-effect-on-chemical-nociception
#10
Chen Yan, Dai Ti-Jun, Li Xin, Cao Gao, Jiang Shen, Tao Hong, Meng Zhi-Xiu
OBJECTIVE: The study aimed to investigate the relationship between the analgesic effect of sevoflurane and 5-serotonin receptor 1A (5-HT1A R) in the spinal cords of mice. METHODS: Analgesic mouse models were established by intraperitoneal injection of emulsified sevoflurane, and the influence of p-MPPF (a specific antagonist of 5-HT1A Rs) intrathecal injection on the changes in tail-flick latency in tail-withdrawal test, pain threshold in hot-plate test (HPPT), and writhing times in acetic acid-induced writhing test were recorded...
March 28, 2017: Pharmacology
https://www.readbyqxmd.com/read/28334726/preparation-characterization-and-anti-ulcer-efficacy-of-sanguinarine-loaded-solid-lipid-nanoparticles
#11
Qing Sun, Weifeng Li, Huani Li, Xiumei Wang, Yu Wang, Xiaofeng Niu
AIM: This study was designed to develop sanguinarine-loaded solid lipid nanoparticles (SG-SLNs) and investigate its gastroprotective effect on ethanol-induced gastric mucosal lesions in mice. METHODS: SG-SLNs were prepared by high temperature melt-cool solidification method using glycerol monostearate as the lipid and a combination of lecithin with poloxamer 188 as the surfactants. Solid lipid nanoparticles (SLNs) were designed at varying lipid concentrations (5, 10, 15, and 20 mg/mL), surfactant mixture concentrations (6, 12, and 18 mg/mL), and drug contents (5, 10, 15, and 20 mg/mL) in "one factor at a time" fashion...
March 24, 2017: Pharmacology
https://www.readbyqxmd.com/read/28329747/influence-of-dipeptidyl-peptidase-iv-inhibitor-sitagliptin-on-extracellular-signal-regulated-kinases-1-2-signaling-in-rats-with-diabetic-nephropathy
#12
Xiaojun Ren, Gaohong Liu, Yanhong Wang, Wan Zhang, Fuping Xue, Rongshan Li, Weimin Yu
The protective effects of sitagliptin on the kidneys of rats with diabetic nephropathy (DN) and its influence on extracellular signal-regulated kinases 1/2 (ERK1/2) signaling were investigated. Male Wistar rats (n = 40) were randomly assigned to normal control, DN, low-dose sitagliptin intervention (ST1), or high-dose sitagliptin intervention (ST2) groups. Animals were euthanized after a 16-week treatment, and blood glucose (BG), glycosylated hemoglobin (HbA1c), urinary albumin excretion rate (AER), serum creatinine (Scr), creatinine clearance rate (Ccr), active glucagon-like peptide-1 (GLP-1) levels, kidney hypertrophy index, and renal pathohistology were determined...
March 23, 2017: Pharmacology
https://www.readbyqxmd.com/read/28268217/a-phenanthrene-derivative-5-7-dimethoxy-1-4-phenanthrenequinone-inhibits-cell-adhesion-molecule-expression-and-migration-in-vascular-endothelial-and-smooth-muscle-cells
#13
Huey-Ming Lo, Tsong-Long Hwang, Wen-Bin Wu
The activation of endothelial cells (ECs) and migration of vascular smooth muscle cells (VSMCs) have played a crucial role in monocyte chemotaxis/adhesion and intima thickening during vascular injury and atherosclerosis, respectively. Several phenanthrenes isolated from plants and natural products have been shown to possess different bioactivities such as anti-platelet aggregation and anti-inflammation. The current study was designated to investigate the effects of a phenanthrene derivative, 5,7-dimethoxy-1,4-phenanthrenequinone (DMPQ), on cell adhesion molecule (CAM) expression in vascular ECs and migration in VSMCs...
2017: Pharmacology
https://www.readbyqxmd.com/read/28253499/repeated-cold-stress-reduces-cyclophosphamide-induced-cystitis-bladder-pain-and-macrophage-activity-in-mice
#14
Maho Tsubota, Tomoyoshi Miyamoto, Saki Hiruma, Haruka Saeki, Takaya Miyazaki, Fumiko Sekiguchi, Yoshinori Funakami, Atsufumi Kawabata
We examined the effect of repeated cold (RC) stress on cyclophosphamide (CPA)-induced cystitis/bladder pain in mice, in relation to macrophage activity. CPA, given i.p. at 400 mg/kg, caused bladder pain symptoms accompanying cystitis in both unstressed and RC-stressed mice, which were prevented by the macrophage inhibitor minocycline. A low dose, that is, 200 mg/kg, of CPA still produced bladder pain symptoms in unstressed but not RC-stressed mice. Lipopolysaccharide-induced cytokine production in peritoneal macrophages from RC-stressed mice was less than that from unstressed mice...
2017: Pharmacology
https://www.readbyqxmd.com/read/28253495/tacrolimus-triggers-transient-receptor-potential-vanilloid-1-dependent-relapse-of-pancreatitis-related-pain-in-mice
#15
Yuka Terada, Maho Tsubota, Hiiragi Sugo, Kohei Wakitani, Fumiko Sekiguchi, Kyoichi Wada, Mitsutaka Takada, Akira Oita, Atsufumi Kawabata
Transient receptor potential vanilloid-1 (TRPV1) expressed in nociceptors is directly phosphorylated and activated by protein kinase C, and involved in the signaling of pancreatic pain. On the other hand, Cav3.2 T-type Ca2+ channels expressed in nociceptors are functionally upregulated by phosphorylation with protein kinase A and also play a role in pancreatitis-related pain. Calcineurin, a phosphatase, negatively regulates various channel functions including TRPV1, and calcineurin inhibitor-induced pain syndrome by tacrolimus, a calcineurin inhibitor, used as an immunosuppressant, has been a clinical problem...
2017: Pharmacology
https://www.readbyqxmd.com/read/28249288/responsiveness-of-coronary-arteries-to-nitroglycerin-under-hypoxia-the-importance-of-the-endothelium
#16
Masashi Tawa, Takashi Shimosato, Hiroshi Sakonjo, Tomio Okamura
BACKGROUND/AIMS: Nitroglycerin is widely used as a coronary vasodilator in the treatment of ischemic heart diseases. This study investigated the influence of hypoxia on nitroglycerin-induced relaxation in endothelium-intact and -denuded rabbit, monkey, and porcine coronary arteries. METHODS: Helically cut strips of coronary arteries were suspended in organ chambers, and isometric tension was recorded. RESULTS: Nitroglycerin concentration dependently relaxed endothelium-intact rabbit coronary arteries, which were not different under normoxic and hypoxic conditions...
2017: Pharmacology
https://www.readbyqxmd.com/read/28219076/effect-of-n-benzylpiperazine-its-metabolite-n-benzylethylenediamine-and-its-disubstituted-analogue-n-n-dibenzylpiperazine-on-the-acquisition-formation-and-consolidation-of-memory-in-mice
#17
Juan Carlos Castillo-Hernández, Josué A Velázquez-Moyado, Adelfo Reyes-Ramírez, Elena G Ramírez-López, Martín González-Andrade, Andrés Navarrete
BACKGROUND: N-benzylpiperazine (BZP) belongs to a class of piperazine derivatives (PZDs) that have emerged as recreational drugs. These compounds increase the release of dopamine and serotonin. BZP mimics the psychoactive effects of 3,4-methylenedioxymethylamphetamine. BZP is metabolized to N-benzylethylenediamine (BEDA) and benzylamine. The compound N,N'-dibenzylpiperazine (DBZP) is obtained as a byproduct during the synthesis of BZP. Some PZDs have shown effects on memory; however, there are no previous reports on the activity of BZP, BEDA, and DBZP on memory or on a description of their neuropharmacological profile...
2017: Pharmacology
https://www.readbyqxmd.com/read/28214870/the-inhibitory-effect-of-s-777469-a-cannabinoid-type-2-receptor-agonist-on-skin-inflammation-in-mice
#18
Takayo Haruna, Masahiko Soga, Yasuhide Morioka, Kinichi Imura, Yoko Furue, Mina Yamamoto, Jun Hayakawa, Masashi Deguchi, Akinori Arimura, Kiyoshi Yasui
We investigated the effects of S-777469 (1-[[6-Ethyl-1-[4-fluorobenzyl]-5-methyl-2-oxo-1, 2-dihydropyridine-3-carbonyl]amino]-cyclohexanecarboxylic acid), a novel cannabinoid type 2 receptor (CB2) agonist, on 1-fluoro-2,4-dinitrobenzene (DNFB)-induced ear inflammation and mite antigen-induced dermatitis in mice. The oral administration of S-777469 significantly suppressed DNFB-induced ear swelling in a dose-dependent manner. In addition, S-777469 significantly alleviated mite antigen-induced atopic dermatitis-like skin lesions in NC/Nga mice...
2017: Pharmacology
https://www.readbyqxmd.com/read/28208135/abcb1-and-slco1b3-gene-polymorphisms-and-their-impact-on-digoxin-pharmacokinetics-in-atrial-fibrillation-patients-among-the-tunisian-population
#19
Nejia Tounsi, Imen Trabelsi, Emna Kerkeni, Mohamed Habib Grissa, Nizar Fredj, Adel Sekma, Malek Mzali, Ilhem Hellara, Kamel Monastiri, Wahiba Douki, Semir Nouira
BACKGROUND: Digoxin is a substrate of P-glycoprotein (P-gp) and organic anion transporting polypeptide transporters that are encoded by ABCB1 and SLCO1B3 genes. Genetic polymorphisms in both genes may explain inter-individual variability of serum digoxin concentration (SDC). This study evaluates the possible effect of the most common ABCB1 and SLCO1B3 polymorphisms on SDC after a single oral dose of digoxin in Tunisian atrial fibrillation (AF) patients. METHODS: ABCB1 and SLCO1B3 genotypes were analyzed in 102 patients with AF who received digoxin (0...
2017: Pharmacology
https://www.readbyqxmd.com/read/28147362/hochuekkito-a-japanese-herbal-medicine-restores-metabolic-homeostasis-between-mitochondrial-and-glycolytic-pathways-impaired-by-influenza-a-virus-infection
#20
Keita Takanashi, Katsuaki Dan, Sho Kanzaki, Hideki Hasegawa, Kenji Watanabe, Kaoru Ogawa
BACKGROUND: Hochuekkito (HKT), a traditional Japanese herbal medicine (Kampo), has been used to treat symptoms of several diseases. In a recent clinical study, HKT was shown to be protective against the influenza virus infection. However, the underlying mechanism of the prophylactic effect is not clear. Mitochondrial and glycolytic pathways play important roles in cellular energy metabolism to maintain biological functions. These metabolic pathways are affected by the influenza virus infection...
2017: Pharmacology
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