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https://www.readbyqxmd.com/read/29136335/sii-ang-ii-potentiates-insulin-receptor-signalling-and-glycogen-synthesis-in-hepatocytes
#1
Samra Joke Sanni, Christina Lyngsø, Steen Gammeltoft, Jakob Lerche Hansen
The angiotensin II type I receptor (AT1R) is involved in the regulation of cardiovascular function. Excessive activation of AT1R by angiotensin II (Ang II) leads to cardiovascular disease and may be involved in the development of insulin resistance and diabetes. Functionally selective Ang II analogues, such as the [Sar1, Ile4, Ile8]-angiotensin II (SII Ang II) analogue that only activates a subset of signalling networks have been demonstrated to have beneficial effects on cardiovascular function in certain settings, including lowering blood pressure and increasing cardiac performance...
November 14, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29135287/molecular-modelling-studies-in-explaining-the-higher-gpvi-antagonistic-activity-of-the-racemic-2-4-methoxyphenylsulfonyl-2-3-4-9-tetrahydro-1h-pyrido-3-4-b-indole-3-carboxamide-than-its-enantiomers
#2
S S Bhunia, A K Saxena
The GPVI receptor on the platelets plays a major role in inhibiting arterial thrombosis with limited risk of bleeding and is considered a potential anti-thrombotic target for arterial thrombosis. In the reported anti-thrombotics, tetrahydropyridoindoles, the title compound was the best inhibitor of the collagen mediated platelet aggregation by antagonizing the platelet receptor GPVI. Interestingly, the racemic title compound showed better antagonism (IC50 racemate = 6.7 μM) than either of its enantiomers (IC50 S enantiomer = 25...
November 14, 2017: SAR and QSAR in Environmental Research
https://www.readbyqxmd.com/read/29126194/central-and-peripheral-slow-pressor-mechanisms-contributing-to
#3
Jiao Lu, Hong-Wei Wang, Monir Ahmad, Marzieh Keshtkar-Jahromi, Mordecai P Blaustein, John Hamlyn, Frans H H Leenen
Aims: High salt intake markedly enhances hypertension induced by angiotensin II (Ang II). We explored central and peripheral slow-pressor mechanisms which may be activated by Ang II and salt. Methods and Results: In Protocol I, Wistar rats were infused subcutaneously with low- dose Ang II (150 ng/kg/min) and fed regular (0.4%) or high salt (2%) diet for 14 days. In Protocol II, Ang II -high salt was combined with intracerebroventricular infusion of mineralocorticoid receptor (MR) blockers (eplerenone, spironolactone), epithelial sodium channel (ENaC) blocker (benzamil), angiotensin II type 1 receptor (AT1R) blocker (losartan) or vehicles...
November 8, 2017: Cardiovascular Research
https://www.readbyqxmd.com/read/29122658/endothelium-derived-contraction-in-a-model-of-rheumatoid-arthritis-is-mediated-via-angiotensin-ii-type-1-receptors
#4
Kayleigh Hamilton, Lynette Dunning, William R Ferrell, John C Lockhart, Andrew MacKenzie
A role for endothelium-derived constricting factors (EDCF), and the angiotensin II type 1 receptor (AT1R) pathway, in the vascular impairment found in the rat Freund's complete adjuvant (FCA)-model of rheumatoid arthritis (RA) was examined. FCA arthritis was induced in rats±losartan. Vehicle-treated rats served as controls. Knee-joint swelling and red blood cell (RBC) aggregation were measured as indicators of inflammation and endothelium reactivity assessed by response to acetylcholine (ACh) on aortic rings...
November 6, 2017: Vascular Pharmacology
https://www.readbyqxmd.com/read/29121091/effects-of-four-different-antihypertensive-drugs-on-plasma-metabolomic-profiles-in-patients-with-essential-hypertension
#5
Timo P Hiltunen, Jenni M Rimpelä, Robert P Mohney, Steven M Stirdivant, Kimmo K Kontula
OBJECTIVE: In order to search for metabolic biomarkers of antihypertensive drug responsiveness, we measured >600 biochemicals in plasma samples of subjects participating in the GENRES Study. Hypertensive men received in a double-blind rotational fashion amlodipine, bisoprolol, hydrochlorothiazide and losartan, each as a monotherapy for one month, with intervening one-month placebo cycles. METHODS: Metabolomic analysis was carried out using ultra high performance liquid chromatography-tandem mass spectrometry...
2017: PloS One
https://www.readbyqxmd.com/read/29119534/angiotensin-ii-causes-neuronal-damage-in-stretch-injured-neurons-protective-effects-of-losartan-an-angiotensin-t1-receptor-blocker
#6
P M Abdul-Muneer, Saurav Bhowmick, Nicholas Briski
Angiotensin II (Ang II) is a mediator of oxidative stress via activation/induction of reactive oxygen and nitrogen species-generating enzymes, NADPH oxidase (NOX) and inducible nitric oxide synthase (iNOS). We investigated the hypothesis that overproduction of Ang II during traumatic brain injury (TBI) induces the activation of the oxidative stress, which triggers neuroinflammation and cell apoptosis in a cell culture model of neuronal stretch injury. We first established that stretch injury causes a rapid increase in the level of Ang II, which causes the release of pro-inflammatory cytokines, IL-1β and TNF-α, via the induction of oxidative stress...
November 8, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/29119275/comparison-of-effects-of-losartan-and-metoprolol-on-left-ventricular-and-aortic-function-at-rest-and-during-exercise-in-chronic-aortic-regurgitation
#7
Paul A Roberts, Aaron C W Lin, Brett R Cowan, Alistair A Young, Ralph Stewart
Aortic regurgitation (AR) increases the hemodynamic load on both the left ventricle (LV) and the aorta. Vasodilators and beta-blockers both reduce systemic blood pressure, but their relative effects on the LV and aortic function and aortic regurgitant fraction in chronic AR are uncertain. We aimed to compare short-term effects of losartan and metoprolol on LV and aortic function in asymptomatic patients with chronic moderate to severe AR, both at rest and during exercise, using cardiac magnetic resonance (CMR) imaging...
November 8, 2017: International Journal of Cardiovascular Imaging
https://www.readbyqxmd.com/read/29110325/a-case-of-segmental-stiff-skin-syndrome-treated-with-systemic-losartan
#8
Nicole Maillet-Lebel, Victor Kokta, Jerome Coulombe, Julie Powell
Stiff skin syndrome (SSS) is a rare, autosomal dominant cutaneous disorder with progressive, symmetric, sclerotic skin changes of the shoulders, hips, and thighs. In a recent publication, a distinct segmental variant of SSS was proposed. In this report we discuss the case of a boy with segmental SSS and review the current literature.
November 6, 2017: Pediatric Dermatology
https://www.readbyqxmd.com/read/29109495/a-pitfall-in-suspected-refractory-celiac-disease-losartan-induced-enteropathy
#9
T van Gils, R J Robijn, G Bouma, E A Neefjes-Borst, C J J Mulder
No abstract text is available yet for this article.
November 2017: American Journal of Gastroenterology
https://www.readbyqxmd.com/read/29107090/inhibition-of-angiotensin-ii-and-calpain-attenuates-pleural-fibrosis
#10
Lin-Jie Song, Fei Xiang, Hong Ye, Hai Huang, Jie Yang, Fan Yu, Liang Xiong, Juan-Juan Xu, Peter A Greer, Huan-Zhong Shi, Jian-Bao Xin, Yunchao Su, Wan-Li Ma
Pleural fibrosis is associated with various inflammatory processes such as tuberculous pleurisy and bacterial empyema. There is currently no ideal therapeutic to attenuate pleural fibrosis. Some pro-fibrogenic mediators induce fibrosis through inflammatory processes, suggesting that blockage of these mediators might prevent pleural fibrosis. The MeT-5A human pleural mesothelial cell line (PMC) was used in this study as an in vitro model of fibrosis; and intra-pleural injection of bleomycin with carbon particles was used as an in vivo mouse model of pleural fibrosis...
October 26, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29105106/angiotensin-receptor-blocker-use-and-gastro-oesophageal-cancer-survival-a-population-based-cohort-study
#11
J Busby, Ú McMenamin, A Spence, B T Johnston, C Hughes, C R Cardwell
BACKGROUND: Angiotensin receptor blockers (ARBs; including candesartan, losartan, olmesartan and valsartan) are widely used to treat hypertension, heart failure and diabetic neuropathy. There is considerable pre-clinical evidence that ARBs can reduce cancer progression, particularly for gastric cancer. Despite this, epidemiological studies have yet to assess the impact of ARB use on gastro-oesophageal cancer survival. AIM: To investigate the association between post-diagnosis ARB use and gastro-oesophageal cancer survival...
November 3, 2017: Alimentary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29104158/moderate-salt-restriction-with-or-without-paricalcitol-in-type-2-diabetes-and-losartan-resistant-macroalbuminuria-proceed-a-randomised-double-blind-placebo-controlled-crossover-trial
#12
Aneliya Parvanova, Matias Trillini, Manuel A Podestà, Ilian Petrov Iliev, Barbara Ruggiero, Manuela Abbate, Annalisa Perna, Francesco Peraro, Olimpia Diadei, Nadia Rubis, Flavio Gaspari, Fabiola Carrara, Nadia Stucchi, Antonio Belviso, Antonio C Bossi, Roberto Trevisan, Giuseppe Remuzzi, Martin de Borst, Piero Ruggenenti
BACKGROUND: Macroalbuminuria predicts renal and cardiovascular events in patients with type 2 diabetes. We aimed to assess the albuminuria-lowering effects of salt restriction, paricalcitol therapy, or both, in this population. METHODS: In this randomised, double-blind, placebo-controlled, crossover trial, we recruited adult patients with type 2 diabetes from six diabetology outpatient clinics in northern Italy, with 24 h albuminuria of more than 300 mg despite 100 mg per day losartan therapy, blood pressure of less than 140/90 mm Hg, serum creatinine concentration of less than 2 mg/dL, stable renal function on stable renin-angiotensin system inhibitor therapy with a fixed dose of losartan, parathyroid hormone concentration of 20 pg/mL to <110 pg/mL, serum calcium concentration of less than 9·5 mg/dL, and serum phosphate concentration of less than 5 mg/dL, who had been more than 80% compliant with placebo treatment during a 1 month placebo run-in...
November 2, 2017: Lancet Diabetes & Endocrinology
https://www.readbyqxmd.com/read/29092097/brand-vs-generic-adverse-event-reporting-patterns-an-authorized-generic-controlled-evaluation-of-cardiovascular-medications
#13
Y Alatawi, Md M Rahman, N Cheng, J Qian, P L Peissig, R L Berg, C D Page, R A Hansen
WHAT IS KNOWN AND OBJECTIVE: Some public scepticism exists about generics in terms of whether brand and generic drugs produce identical outcomes. This study explores whether adverse event (AE) reporting patterns are similar between brand and generic drugs, using authorized generics (AGs) as a control for possible generic drug perception biases. METHODS: Events reported to the FDA Adverse Event Reporting System from the years 2004-2015 were analysed. Drugs were classified as brand, AG or generic based on drug and manufacturer names...
November 1, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/29083936/losartan-hydrochlorothiazide-combination-is-safe-and-effective-for-morning-hypertension-in-very-elderly-patients
#14
Hiroki Uchiwa, Hisashi Kai, Yoshiko Iwamoto, Takahiro Anegawa, Hidemi Kajimoto, Kenji Fukuda, Tsutomu Imaizumi, Yoshihiro Fukumoto
Morning hypertension is an independent risk for cerebrovascular and cardiovascular events. Although the prevalence of morning hypertension increases with age, treatment of morning hypertension has not been established, particularly in Very-Elderly patients. We compared the safety and efficacy of a losartan/hydrochlorothiazide (HCTZ) combination in controlling morning hypertension between Very-Elderly (≥75 years) and Young/Elderly patients (<75 years). This study was a subanalysis of the Morning Hypertension and Angiotensin Receptor Blocker/Hydrochlorothiazide Combination Therapy study, in which patients with morning hypertension (≥135/85 mmHg) received a 50-mg losartan/12...
October 30, 2017: Clinical and Experimental Hypertension: CHE
https://www.readbyqxmd.com/read/29082266/allopurinol-induced-granulomatous-hepatitis-a-case-report-and-review-of-literature
#15
Umair Iqbal, Hafiz Umair Siddiqui, Hafsa Anwar, Ahmad Chaudhary, Abdulhadi Affan Quadri
Liver enzyme elevation is a common reason for referral to a gastroenterologist. Drugs are one of the most common reasons for asymptomatic elevation of liver enzymes. We present here a case of granulomatous hepatitis (GH) secondary to long-term use of allopurinol. An 83-year-old male with a history of chronic gout and hypertension was evaluated for elevation of liver enzymes. He denies any complaints of abdominal pain, nausea, fever, chills, weight loss, night sweats, or yellowness of skin. He denies any use of herbal medications...
July 2017: Journal of Investigative Medicine High Impact Case Reports
https://www.readbyqxmd.com/read/29081617/efficacy-and-tolerability-of-olmesartan-telmisartan-and-losartan-in-patients-of-stage-i-hypertension-a-randomized-open-label-study
#16
Mrunalini Kalikar, Kundan S Nivangune, Ganesh N Dakhale, Chaitali S Bajait, Smita D Sontakke, Vijay M Motghare, Ritu Budania
OBJECTIVES: To compare the efficacy and tolerability of losartan, telmisartan, and olmesartan as antihypertensive agents and evaluate and compare their effects on lipid profile and blood glucose. MATERIALS AND METHODS: This was a randomized, open-label, parallel-group, comparative study conducted in sixty patients of Stage I hypertension. The eligible patients were randomly allocated into three treatment groups: (1) Tablet olmesartan (20 mg), (2) Tablet telmisartan (40 mg), and (3) Tablet losartan (50 mg)...
July 2017: Journal of Pharmacology & Pharmacotherapeutics
https://www.readbyqxmd.com/read/29078982/topical-reformulation-of-valsartan-for-treatment-of-chronic-diabetic-wounds
#17
Peter Abadir, Sayed Hosseini, Mahya Faghih, Amir Ansari, Frank Lay, Barbara Smith, Aleksandra Beselman, Diep Vuong, Alan Berger, Jing Tian, David Rini, Kevin Keenahan, Joshua Budman, Tadashi Inagami, Neal Fedarko, Guy Marti, John Harmon, Jeremy Walston
Chronic wounds are among the most devastating and difficult to treat consequences of diabetes. Dysregulation of the skin renin-angiotensin system (RAS) is implicated in abnormal wound healing in diabetic and older adults. Given this, we sought to determine the effects of topical reformulations of the angiotensin type 1 receptor blockers (ARB) losartan and valsartan and the angiotensin-converting enzyme (ACE) inhibitor captopril on wound healing in diabetic and aged mice with further validation in older diabetic pigs...
October 24, 2017: Journal of Investigative Dermatology
https://www.readbyqxmd.com/read/29072489/effects-of-losartan-on-vasomotor-function-and-canonical-transient-receptor-potential-channels-in-the-aortas-of-sinoaortic-denervation-rats
#18
Minlie Liang, Wenliang Zhong, Fei Miao, Hongchao Wu, Yingfeng Liu
Increased short-term blood pressure variability (BPV) is strongly correlated with target organ damage. However, the molecular mechanisms underlying abnormal BPV-induced organ damage and effective therapeutic targets are poorly understood. The purpose of this study was to investigate the effects of losartan on vasomotor function and canonical transient receptor potential (TRPC) channels in the aortas of rats with arterial pressure lability induced by sinoaortic denervation (SAD). SAD was performed in male Sprague-Dawley rats at the age of 10 weeks...
October 26, 2017: Clinical and Experimental Hypertension: CHE
https://www.readbyqxmd.com/read/29071895/-effect-of-mild-moxibustion-with-different-terms-at-different-acupoints-on-renal-functions-and-renal-pathological-changes-in-focal-segmental-glomerulosclerosis-rats
#19
Lin Li, Yu-Xia Sun, Jia-Yi Ma, Chun-Ling Zhang, Yi Li
OBJECTIVE: To observe changes of urinary microprotein, and serum creatinine, urea nitrogen and uric acid levels in focal segmental glomerulosclerosis (FSGS) rats treated by mild moxibustion, so as to explore the mechanism of moxibustion underlying improvement of FSGS. METHODS: SD rats were randomized into normal control (normal), sham operation (sham), model, medication (Losartan), moxibustion-Shenshu (BL 23) and moxibustion-Geshu (BL 17) groups. The latter two moxibustion groups were further divided into 10 min, 20 min and 30 min subgroups (n=6 in each group/subgroups)...
December 25, 2016: Zhen Ci Yan Jiu, Acupuncture Research
https://www.readbyqxmd.com/read/29056916/inhibition-of-pro-renin-receptor-contributes-to-renoprotective-effects-of-angiotensin-ii-type-1-receptor-blockade-in-diabetic-nephropathy
#20
Lin Zhang, Xiao-Fei An, Xin Ruan, Dong-Dong Huang, Li Zhou, Hong Xue, Li-Min Lu, Ming He
Aims: Renal renin-angiotensin system (RAS) plays a pivotal role in the development of diabetic nephropathy (DN). Angiotensin II (Ang II) type 1 receptor (AT1R) blockade elevates (pro)renin, which may bind to (pro)renin receptor (PRR) and exert receptor-mediated, angiotensin-independent profibrotic effects. We therefore investigated whether PRR activation leads to the limited anti-fibrotic effects of AT1R blockade on DN, and whether PRR inhibition might ameliorate progression of DN. Methods: To address the issue, the expression of RAS components was tested in different stages of streptozotocin (STZ)-induced diabetic rats (6, 12, and 24 weeks) and 6-week AT1R blockade (losartan) treated diabetic rats...
2017: Frontiers in Physiology
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