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telmisartan

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https://www.readbyqxmd.com/read/28447738/telmisartan-suppresses-cardiac-hypertrophy-by-inhibiting-cardiomyocyte-apoptosis-via-the-nfat-anp-bnp-signaling-pathway
#1
Xiurong Li, Yuhuai Lan, Yan Wang, Minghao Nie, Yanhong Lu, Eryang Zhao
Telmisartan, a type of angiotensin II (Ang II) receptor inhibitor, is a common agent used to treat hypertension in the clinic. Hypertension increases cardiac afterload and promotes cardiac hypertrophy. However, the ventricular Ang II receptor may be activated in the absence of hypertension. Therefore, telmisartan may reduce cardiac hypertrophy by indirectly ameliorating hypertensive symptoms and directly inhibiting the cardiac Ang II receptor. Nuclear factor of activated T‑cells (NFAT) contributes to cardiac hypertrophy via nuclear translocation, which induces a cascade of atrial natriuretic peptide (ANP) and brain/B‑type natriuretic peptide (BNP) expression and cardiomyocyte apoptosis...
March 14, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28445965/molecular-docking-3d-qsar-and-structural-optimization-on-imidazo-pyridine-derivatives-dually-targeting-at1-and-pparg
#2
Jun Zhang, Qing-Qing Hao, Xin Liu, Zhi Jing, Wen-Qing Jia, Shu-Qing Wang, Wei-Ren Xu, Xian-Chao Cheng, Run-Ling Wang
Telmisartan, a bifunctional agent of blood pressure lowering and glycemia reduction, was previously reported to antagonize angiotensin II type 1 (AT1) receptor and partially activate peroxisome proliferator-activated receptor γ (PPARγ) simultaneously. Through the modification to telmisartan, researchers designed and obtained imidazo-\pyridine derivatives with the IC50s of 0.49~94.1 nM against AT1 and EC50s of 20~3640 nM towards PPARγ partial activation. For minutely inquiring the interaction modes with the relevant receptor and analyzing the structure-activity relationships, molecular docking and 3D-QSAR (Quantitative structure-activity relationships) analysis of these imidazo-\pyridines on dual targets were conducted in this work...
April 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28434702/inhibition-or-deletion-of-angiotensin-ii-type-1-receptor-suppresses-elastase-induced-experimental-abdominal-aortic-aneurysms
#3
Haojun Xuan, Baohui Xu, Wei Wang, Hiroki Tanaka, Naoki Fujimura, Masaaki Miyata, Sara A Michie, Ronald L Dalman
OBJECTIVE: Angiotensin (Ang) II type 1 receptor (AT1) activation is essential for the development of exogenous Ang II-induced abdominal aortic aneurysms (AAAs) in hyperlipidemic animals. Experimental data derived from this modeling system, however, provide limited insight into the role of endogenous Ang II in aneurysm pathogenesis. Consequently, the potential translational value of AT1 inhibition in clinical AAA disease management remains incompletely understood on the basis of the existing literature...
April 20, 2017: Journal of Vascular Surgery
https://www.readbyqxmd.com/read/28421141/excess-of-aminopeptidase-a-in-the-brain-elevates-blood-pressure-via-the-angiotensin-ii-type-1-and-bradykinin-b2-receptors-without-dipsogenic-effect
#4
Takuto Nakamura, Masanobu Yamazato, Akio Ishida, Yusuke Ohya
Aminopeptidase A (APA) cleaves angiotensin (Ang) II, kallidin, and other related peptides. In the brain, it activates the renin angiotensin system and causes hypertension. Limited data are available on the dipsogenic effect of APA and pressor effect of degraded peptides of APA such as bradykinin. Wistar-Kyoto rats received intracerebroventricular (icv) APA in a conscious, unrestrained state after pretreatment with (i) vehicle, (ii) 80 μg of telmisartan, an Ang II type-1 (AT1) receptor blocker, (iii) 800 nmol of amastatin, an aminopeptidase inhibitor, and (iv) 1 nmol of HOE-140, a bradykinin B2 receptor blocker...
2017: International Journal of Hypertension
https://www.readbyqxmd.com/read/28415046/cost-benefit-effectiveness-of-angiotensin-ii-receptor-blockers-in-patients-with-uncomplicated-hypertension-a-comparative-analysis
#5
Alberto Mazza, Antonella Paola Sacco, Danyelle M Townsend, Gianni Bregola, Edgardo Contatto, Isabella Cappello, Laura Schiavon, Emilio Ramazzina, Domenico Rubello
OBJECTIVE: The treatment of hypertensive patients (HTs) requires a long-term commitment of compliance for the patient and resources by the healthcare system. This poses an economic dilemma in countries where universal healthcare is standard. The aim of this study was to evaluate the costs/health benefit and effectiveness of treatment with angiotensin-II receptor blockers (ARBs) in uncomplicated essential hypertension. DESIGN AND METHODS: The daily and annual economic commitment for treating patients with ARBs was estimated using pharmacy dispensing records and the BP-lowering effects of candesartan, irbesartan, losartan, olmesartan, telmisartan and valsartan was evaluated retrospectively...
April 14, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28393446/copper-mediated-late-stage-functionalization-of-heterocycle-containing-molecules
#6
Ming Shang, Ming-Ming Wang, Tyler G Saint-Denis, Ming-Hong Li, Hui-Xiong Dai, Jin-Quan Yu
One long-standing issue in directed C-H functionalization is that either nitrogen or sulfur atoms present in heterocyclic substrates may bind preferentially to a transition-metal catalyst rather than to the desired directing group. This competitive binding has largely hindered the application of C-H functionalization in late-stage heterocycle drug discovery. Reported here is the use of an oxazoline-based directing group capable of overriding the poisoning effect of a wide range of heterocycle substrates. The potential use of this directing group in pharmaceutical drug discovery is illustrated by diversification of Telmisartan (an antagonist for the angiotensin II receptor) through copper-mediated C-H amination, hydroxylation, thiolation, arylation, and trifluoromethylation...
May 2, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28390695/achieved-blood-pressure-and-cardiovascular-outcomes-in-high-risk-patients-results-from-ontarget-and-transcend-trials
#7
Michael Böhm, Helmut Schumacher, Koon K Teo, Eva M Lonn, Felix Mahfoud, Johannes F E Mann, Giuseppe Mancia, Josep Redon, Roland E Schmieder, Karen Sliwa, Michael A Weber, Bryan Williams, Salim Yusuf
BACKGROUND: Studies have challenged the appropriateness of accepted blood pressure targets. We hypothesised that different levels of low blood pressure are associated with benefit for some, but harm for other outcomes. METHODS: In this analysis, we assessed the previously reported outcome data from high-risk patients aged 55 years or older with a history of cardiovascular disease, 70% of whom had hypertension, from the ONTARGET and TRANSCEND trials investigating ramipril, telmisartan, and their combination, with a median follow-up of 56 months...
April 5, 2017: Lancet
https://www.readbyqxmd.com/read/28388365/protective-effects-of-telmisartan-and-tempol-on-lipopolysaccharide-induced-cognitive-impairment-neuro-inflammation-and-amyloidogenesis-possible-role-of-brain-derived-neurotrophic-factor
#8
Waleed Abd-Elsalam Khallaf, Basim Messiha, Amira Abo-Youssef, Nesrine Salah El Dine El Sayed
Angiotensin II has pro-inflammatory and pro-oxidant potentials. We investigated the possible protective effects of the angiotensin receptor blocker telmisartan, compared with the superoxide scavenger tempol, on lipopolysaccharide (LPS)-induced cognitive decline and amyloidogenesis. Briefly, mice were allocated into a normal control group, an LPS control group, a tempol treatment group, and two telmisartan treatment groups. A behavioral study was conducted followed by a biochemical study via assessment of brain levels of beta amyloid (Aβ) and brain-derived neurotropic factor (BDNF) as amyloidogenesis and neuroplasticity markers, tumor necrosis factor-alpha (TNF-α), nitric oxide end products (NOx), neuronal and inducible nitric oxide synthase (nNOS and iNOS) as inflammatory markers, and superoxide dismutase (SOD), malondialdehyde (MDA), glutathione reduced (GSH) and nitrotyrosine (NT) as oxido-nitrosative stress markers...
April 7, 2017: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28385651/intranasal-telmisartan-ameliorates-brain-pathology-in-five-familial-alzheimer-s-disease-mice
#9
Nofar Torika, Keren Asraf, Hagit Cohen, Sigal Fleisher-Berkovich
The renin-angiotensin system (RAS) is a major circulative system engaged in homeostasis modulation. Angiotensin II (Ang II) serves as its main effector hormone upon binding to its primary receptor, Ang II receptor type 1 (AT1R). It is well established that an intrinsic independent brain RAS exists. Abnormal AT1R activation both in the periphery and in the brain probably contributes to the development of Alzheimer's disease (AD) pathology that is characterized, among others, by brain inflammation. Moreover, treatment with drugs that block AT1R (AT1R blockers, ARBs) ameliorates most of the clinical risk factors leading to AD...
April 3, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28374982/angiotensin-ii-receptor-blockers-inhibit-the-generation-of-epoxyeicosatrienoic-acid-from-arachidonic-acid-in-recombinant-cyp2c9-cyp2j2-and-human-liver-microsomes
#10
Asuna Senda, Yuji Mukai, Toru Hayakawa, Yuka Kato, Erik Eliasson, Anders Rane, Takaki Toda, Nobuo Inotsume
Cytochrome P450 (CYP) 2C9, CYP2C8 and CYP2J2 enzymes, which metabolize arachidonic acid to epoxyeicosatrienoic acids (EETs), have cardioprotective effects including anti-inflammation and vasodilation. We have recently shown that some angiotensin II receptor blockers (ARBs) may inhibit AA metabolism via CYP2C8. Using recombinant CYP2C9, CYP2J2, and human liver microsomes (HLMs), the aim was now to compare the ability of six different clinically used ARBs to inhibit AA metabolism in vitro. The rank order of the ARBs for the 50% inhibitory concentration (IC50 ) of AA metabolism was losartan < telmisartan < irbesartan < candesartan < olmesartan < valsartan via CYP2C9, and telmisartan < irbesartan < olmesartan < losartan < candesartan and valsartan via CYP2J2...
April 4, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28336160/unexpected-drug-induced-raynaud-phenomenon-analysis-from-the-french-national-pharmacovigilance-database
#11
Émilie Bouquet, Geoffrey Urbanski, Christian Lavigne, Pascale Lainé-Cessac
OBJECTIVE: To estimate the association between exposure to medicinal products and Raynaud phenomenon. METHODS: The study used the data of all adverse drug reactions notified to the French national pharmacovigilance database. All cases reported between 1st January 1995 and 10th December 2012 were selected. A case/non-case method was used to measure disproportionality of the association between drug exposure and Raynaud phenomenon. The cases concerned all observations involving Raynaud phenomenon...
February 22, 2017: Thérapie
https://www.readbyqxmd.com/read/28330645/design-of-fixed-dose-combination-and-physicochemical-characterization-of-enteric-coated-bilayer-tablet-with-circadian-rhythmic-variations-containing-telmisartan-and-pravastatin-sodium
#12
Daoqi Luo, Joo Hee Kim, Chulhun Park, Euichaul Oh, Jun-Bom Park, Jing-Hao Cui, Qing-Ri Cao, Beom-Jin Lee
The aim of this study was to investigate a fixed dose combination (FDC) of telmisartan (TEL) and pravastatin sodium (PRA) in enteric-coated bilayer tablets, which was designed for once-daily bedtime dose in order to match circadian rhythmic variations of hypertension and cholesterol synthesis and optimize the patient friendly dosing treatment. Due to the poor aqueous solubility of TEL, ternary solid dispersions (SD) consisting of TEL, polyethylene glycol 6000 (PEG 6000) and magnesium oxide (MgO) were designed to enhance its dissolution rate in intestinal fluid...
March 19, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28289180/beneficial-effects-of-apelin-on-vascular-function-in-patients-with-central-obesity
#13
Francesca Schinzari, Augusto Veneziani, Nadia Mores, Angela Barini, Nicola Di Daniele, Carmine Cardillo, Manfredi Tesauro
Patients with central obesity have impaired insulin-stimulated vasodilation and increased ET-1 (endothelin 1) vasoconstriction, which may contribute to insulin resistance and vascular damage. Apelin enhances insulin sensitivity and glucose disposal but also acts as a nitric oxide (NO)-dependent vasodilator and a counter-regulator of AT1 (angiotensin [Ang] II type 1) receptor-induced vasoconstriction. We, therefore, examined the effects of exogenous (Pyr(1))apelin on NO-mediated vasodilation and Ang II- or ET-1-dependent vasoconstrictor tone in obese patients...
March 13, 2017: Hypertension
https://www.readbyqxmd.com/read/28285137/functional-analysis-of-carboxylesterase-in-human-induced-pluripotent-stem-cell-derived-enterocytes
#14
Tomoki Kabeya, Wakana Matsumura, Takahiro Iwao, Masakiyo Hosokawa, Tamihide Matsunaga
Human carboxylesterase (CES) is a key esterase involved in the metabolism and biotransformation of drugs. Hydrolysis activity in the human small intestine is predominantly mediated by CES2A1 rather than CES1A. In drug development studies, Caco-2 cells are commonly used as a model to predict drug absorption in the human small intestine. However, the expression patterns of CES2A1 and CES1A in Caco-2 cells differ from those in the human small intestine. There are also species-specific differences in CES expression patterns between human and experimental animals...
April 22, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28274907/mobile-device-based-electronic-data-capture-system-used-in-a-clinical-randomized-controlled-trial-advantages-and-challenges
#15
Jing Zhang, Lei Sun, Yu Liu, Hongyi Wang, Ningling Sun, Puhong Zhang
BACKGROUND: Electronic data capture (EDC) systems have been widely used in clinical research, but mobile device-based electronic data capture (mEDC) system has not been well evaluated. OBJECTIVE: The aim of our study was to evaluate the feasibility, advantages, and challenges of mEDC in data collection, project management, and telemonitoring in a randomized controlled trial (RCT). METHODS: We developed an mEDC to support an RCT called "Telmisartan and Hydrochlorothiazide Antihypertensive Treatment (THAT)" study, which was a multicenter, double-blinded, RCT, with the purpose of comparing the efficacy of telmisartan and hydrochlorothiazide (HCTZ) monotherapy in high-sodium-intake patients with mild to moderate hypertension during a 60 days follow-up...
March 8, 2017: Journal of Medical Internet Research
https://www.readbyqxmd.com/read/28244897/comparing-the-clinical-efficacy-of-resting-and-antihypertensive-medication-in-patients-of-hypertensive-urgency-a-randomized-control-trial
#16
Sung Keun Park, Won Joong Kim, Dong-Young Lee, Sang Yoon Lee, Hyun Sun Park, Hae Won Kim, Beom Kim, Kyoung Hyoub Moon
OBJECTIVE: Hypertensive urgency is defined as a severe elevation of blood pressure (BP) without target organ damage. In emergency room, hypertensive urgency has been conventionally managed by antihypertensive medication. However, there has been increasing concern for the safety of antihypertensive medication in hypertensive urgency. Thus, this study was to compare the clinical efficacy of resting and antihypertensive medication in managing hypertensive urgency. METHODS: For 138 hypertensive urgency patients admitting in emergency room of Veterans Health Center hospital, a single-center, randomized controlled trial was conducted...
February 27, 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/28244896/adjunctive-therapy-with-statins-reduces-residual-albuminuria-proteinuria-and-provides-further-renoprotection-by-downregulating-the-angiotensin-ii-at1-pathway-in-hypertensive-nephropathy
#17
Zhi Zhang, Ziqiang Li, Kaijin Cao, Dailong Fang, Fazhan Wang, Gang Bi, Jian Yang, Yingju He, Jinhui Wu, Yuquan Wei, Xiangrong Song
OBJECTIVES: Blockade of the renin-angiotensin II (Ang II) system by AT1 blockers (ARBs) and angiotensin-converting enzyme inhibitors retards the progression of chronic kidney disease (CKD) by reducing albuminuria/proteinuria. However, many patients with CKD suffer from residual albuminuria/proteinuria, which is an independent risk factor for CKD progression. The aim of the current study is to investigate the effect of pitavastatin, one of the adjunctive agents to ARBs, on the reduction of albuminuria/proteinuria and further renoprotection mediated by telmisartan in spontaneously hypertensive rats...
February 27, 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/28237650/inhibition-and-inactivation-of-human-cyp2j2-implications-in-cardiac-pathophysiology-and-opportunities-in-cancer-therapy
#18
REVIEW
Aneesh Karkhanis, Yanjun Hong, Eric Chun Yong Chan
Extrahepatic cytochrome P450 enzymes (CYP450) are pivotal in the metabolism of endogenous substrates and xenobiotics. CYP2J2 is a major cardiac CYP450 and primarily metabolizes polyunsaturated fatty acids such as arachidonic acid to cardioactive epoxyeicosatrienoic acids. Due to its role in endobiotic metabolism, CYP2J2 has been actively studied in recent years with the focus on its biological functions in cardiac pathophysiology. Additionally, CYP2J2 metabolizes a number of xenobiotics such as astemizole and terfenadine and is potently inhibited by danazol and telmisartan...
February 23, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28230062/triple-combination-therapy-in-the-treatment-of-hypertension-a-review-of-the-evidence
#19
REVIEW
R Düsing, B Waeber, M Destro, C Santos Maia, P Brunel
Hypertension is a serious public health concern with inadequate control of blood pressure (BP) worldwide. Contributing factors include low efficacy of drugs, underuse of combination therapies, irrational combinations, physicians' therapeutic inertia and poor adherence to treatment. Current guidelines recommend the use of initial (dual) combination therapy in high-risk patients for immediate BP response, better short- and long-term BP control, and continued/improved patient adherence. This article aims to review the existing evidence of triple-combination therapies with respect to efficacy, safety and adherence to treatment...
February 23, 2017: Journal of Human Hypertension
https://www.readbyqxmd.com/read/28228970/comparison-of-endothelial-function-improvement-estimated-with-reactive-hyperemia-index-between-ramipril-and-telmisartan-in-hypertensive-patients
#20
You-Jeong Ki, Jae-Bin Seo, Hack-Lyoung Kim, Woo-Hyun Lim, Hye Yeon Seo, Jin Yong Lee, Woo-Young Chung
BACKGROUND: Endothelium has a function to regulate vascular tone by releasing mediators either vasodilating or vasoconstricting blood vessels. Endothelial dysfunction can be measured conveniently by Reactive Hyperemia Index (RHI) with a peripheral arterial tonometry. Angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin II (AT II) receptor blockers (ARBs) are considered to have beneficial effects on endothelium through inhibition of AT II. This study was performed to compare the effect of ACEIs or ARBs on endothelial function estimated by RHI in hypertensive patients...
2017: Clinical Hypertension
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