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https://www.readbyqxmd.com/read/28507312/design-and-evaluation-of-ephrina1-mutants-with-cerebral-protective-effect
#1
Yuanjun Zhu, Yuanqing Gao, Danping Zheng, Mengyang Shui, Kuai Yu, Xiaoyan Liu, Yuan Lin, Li Su, Wenxing Yang, Yinye Wang
The activation of EphA2 receptor by its natural ligand EphrinA1 causes blood brain barrier dysfunction, and inactivation of EphA2 reduces BBB damage in ischemic stroke. Thus, EphA2 targeted antagonists may serve as neuroprotective agents. We engineered four mutants of EphrinA1, EM1, EM2, EM3 and EM4, respectively. The computational analysis showed that these four mutants were capable of interacting with EphA2. Their potential neuroprotective effects were examined in mouse focal ischemia/reperfusion (I/R) model...
May 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28499171/quinazoline-based-%C3%AE-1-adrenoreceptor-antagonists-with-potent-antiproliferative-activity-in-human-prostate-cancer-cell-lines
#2
Valentina Maestri, Andrea Tarozzi, Elena Simoni, Antonio Cilia, Elena Poggesi, Marina Naldi, Benedetta Nicolini, Letizia Pruccoli, Michela Rosini, Anna Minarini
New α1-adrenoreceptor (α1-AR) antagonists related to prazosin and doxazosin were synthesized by replacing piperazine ring with (S)- or (R)-3-aminopiperidine. Binding studies indicated that the S configuration at the 3-C position of the piperidine ring is crucial for an optimal interaction of the compounds at all three α1-AR subtypes. Quinazolines 9 and 10, bearing a quinone ring on the lateral chain, exhibited also potent antiproliferative activity in LNCaP androgen-sensitive prostate cancer cell lines, higher than that of doxazosin...
May 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28459764/the-effect-of-the-bedtime-dosing-doxazosin-on-nocturnal-hypoxia-triggered-blood-pressure-surge-in-a-young-adult-man-with-severe-obstructive-sleep-apnea-syndrome-and-a-history-of-three-recurrent-sleep-onset-strokes
#3
Tetsuro Yoshida, Mitsuo Kuwabara, Satoshi Hoshide, Kazuomi Kario
No abstract text is available yet for this article.
June 2017: Blood Pressure Monitoring
https://www.readbyqxmd.com/read/28440455/%C3%AE-adrenoceptor-mediated-enhanced-inducibility-of-atrial-fibrillation-in-a-canine-system-inflammation-model
#4
Ying-Ying Chen, Ze-Wei Sun, Jian-Ping Jiang, Xiao-Dong Kang, Lin-Lin Wang, Yue-Liang Shen, Xu-Dong Xie, Liang-Rong Zheng
The exact mechanism associated with inflammation and atrial fibrillation (AF) remains unknown. The aim of the present study was to investigate the roles of connexin 43 (Cx43) and a1‑adrenergic receptor (α1‑AR) activation in the pathogenesis of system inflammation‑induced AF. A canine model of chronic low‑grade system inflammation was established by administrating a low dose of lipopolysaccharide (LPS; 0.1 µg/kg) for 2 weeks. Programmed stimulation was applied on the right atrial appendage to determine the effective refractory periods (ERP) and the window of vulnerability (WOV)...
June 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28440105/effect-of-doxazosin-on-stress-reactivity-and-the-ability-to-resist-smoking
#5
Terril L Verplaetse, Andrea H Weinberger, Lindsay M Oberleitner, Kathryn Mz Smith, Brian P Pittman, Julia M Shi, Jeanette M Tetrault, Meaghan E Lavery, Marina R Picciotto, Sherry A McKee
Preclinical findings support a role for α1-adrenergic antagonists in reducing nicotine-motivated behaviors, but these findings have yet to be translated to humans. The current study evaluated whether doxazosin would attenuate stress-precipitated smoking in the human laboratory. Using a well-validated laboratory analogue of smoking-lapse behavior, this pilot study evaluated whether doxazosin (4 and 8 mg/day) versus placebo attenuated the effect of stress (vs neutral imagery) on tobacco craving, the ability to resist smoking and subsequent ad-libitum smoking in nicotine-deprived smokers ( n=35)...
April 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28349274/a-systematic-review-of-add-on-pharmacologic-therapy-in-the-treatment-of-resistant-hypertension
#6
REVIEW
Anita P Tataru, Arden R Barry
INTRODUCTION: The objective of this systematic review was to evaluate the efficacy and safety of add-on pharmacologic therapies in the treatment of resistant hypertension (RH), defined as blood pressure (BP) above target despite three antihypertensive agents. METHODS: A systematic search was performed in MEDLINE, Embase, CENTRAL, CINAHL, ClinicalTrials.gov, and Google Scholar (inception to June 2016) to identify randomized controlled trials (RCTs) that compared any antihypertensive agent with control in patients with RH...
March 27, 2017: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
https://www.readbyqxmd.com/read/28272220/clinical-study-of-duloxetine-hydrochloride-combined-with-doxazosin-for-the-treatment-of-pain-disorder-in-chronic-prostatitis-chronic-pelvic-pain-syndrome-an-observational-study
#7
RANDOMIZED CONTROLLED TRIAL
Mingxin Zhang, Hanzhong Li, Zhigang Ji, Dexin Dong, Su Yan
To explore the safety and efficacy of the selective 5-serotonin and norepinephrine reuptake inhibitor duloxetine hydrochloride and alpha-adrenergic receptor blocker (alpha-blocker) doxazosin mesylate-controlled tablets in the treatment of pain disorder in chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS).In all, 150 patients were enrolled and 126 patients completed the study (41 patients in the doxazosin group, 41 patients in the sertraline group, and 44 patients in the duloxetine group). This was an open randomized 6-month study...
March 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/27992238/antiangiogenic-effects-of-doxazosin-on-experimental-choroidal-neovascularization-in-mice
#8
Jiaxian Guo, Xueting Luo, Jian Liang, Meichun Xiao, Xiaodong Sun
PURPOSE: The present study was designed to evaluate the effects of doxazosin on experimental choroidal neovascularization (CNV) in mice. METHODS: Six- to 8-week-old male C57BL/6 mice were divided into a control group and a doxazosin-treated group (5 mg/kg, i.p., daily). Experimental CNV was induced by laser photocoagulation. Seven and 14 days after laser induction, fluorescein angiography, choroidal flat mounts, and histological studies were performed to evaluate the fluorescence leakage, area, and thickness of CNV lesions, respectively...
January 2017: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27987130/ultrasound-image-features-of-intravesical-prostatic-protrusion-indicated-failure-of-medication-therapy-of-finasteride-and-doxazosin-in-patients-with-benign-prostatic-hyperplasia-luts-bph
#9
Qiang Liu, Yunkai Zhu, Jianping Liu, Jun Qi, Jian Kang
BACKGROUND: Intravesical prostatic protrusion (IPP) is a type of benign prostatic hyperplasia (BPH) adenoma, and it plays a critical role in the pathogenesis of bladder outlet obstruction in patients with lower urinary tract syndromes (LUTS/BPH). AIMS: The goal of this study was to investigate the effect of a combination therapy with finasteride and doxazosin on IPP in BPU/LUTS patients. METHODS: A total of 322 BPH patients with enlarged prostatic volume as well as moderate to severe symptom scores were enrolled and divided into four groups according to the degree of IPP (IPP > 10 mm, 5-10 mm, <5 mm and no IPP) in this study...
December 16, 2016: International Urology and Nephrology
https://www.readbyqxmd.com/read/27981373/-combined-treatment-of-bps-with-tamsulosin-and-finasteride-literature-review-and-prescription-data
#10
K Höfner, S Ulrich, R Berges
Combined therapy of benign prostatic syndrome (BPS) with α1-blockers and 5α-reductase (5AR)-inhibitors is recommended according to two leading studies on doxazosin/finasteride and tamsulosin/dutasteride for all 10 in Germany possible combinations (five α1-blockers and two 5AR inhibitors). Because tamsulosin and finasteride predominate in the treatment of BPS in Germany, the role of the combination tamsulosin/finasteride and its scientific basis from clinical studies has been investigated. A pharmacoepidemiological extrapolation from receipts of pharmacy data centres showed a strong increase of the combination tamsulosin/finasteride since 2003...
May 2017: Der Urologe. Ausg. A
https://www.readbyqxmd.com/read/27885499/the-effects-of-alpha-1-adrenoceptor-blockade-and-angiotensin-converting-enzyme-inhibition-on-central-and-brachial-blood-pressure-and-vascular-reactivity-the-doxazosin-ramipril-study
#11
Andreas Jekell, Majid Kalani, Thomas Kahan
We aimed to study whether inhibition of the renin-angiotensin-aldosterone system has effects on vascular structure and function beyond the effects on blood pressure reduction alone. Patients with mild-to-moderate hypertension (n = 61, age 54 ± 12 years, 34% women) received the angiotensin converting enzyme inhibitor ramipril 10 mg or the alpha 1-adrenoceptor blocker doxazosin 8 mg double-blind for 12 weeks. Aortic blood pressure, pulse wave velocity, and augmentation index were assessed by applanation tonometry...
November 24, 2016: Heart and Vessels
https://www.readbyqxmd.com/read/27856806/comparative-effectiveness-of-fourth-line-anti-hypertensive-agents-in-resistant-hypertension-a-systematic-review-and-meta-analysis
#12
Sarah-Jo Sinnott, Laurie A Tomlinson, Adrian A Root, Rohini Mathur, Kathryn E Mansfield, Liam Smeeth, Ian J Douglas
Aim We assessed the effectiveness of fourth-line mineralocorticoid receptor antagonists in comparison with other fourth-line anti-hypertensive agents in resistant hypertension. Methods and results We systematically searched Medline, EMBASE and the Cochrane library from database inception until January 2016. We included randomised and non-randomised studies that compared mineralocorticoid receptor antagonists with other fourth-line anti-hypertensive agents in patients with resistant hypertension. The outcome was change in systolic blood pressure, measured in the office, at home or by ambulatory blood pressure monitoring...
February 2017: European Journal of Preventive Cardiology
https://www.readbyqxmd.com/read/27794178/the-effect-of-doxazosin-and-sildenafil-citrate-combination-on-bladder-tissue-contractility-alpha-adrenergic-receptor-and-inos-subtype-expression-in-a-male-rat-model-of-partially-bladder-outlet-obstruction
#13
Abdulkadir Gumrah, Yiloren Tanidir, Ilker Tinay, Mustafa Ozyurek, Tufan Tarcan
AIMS: Our aim was to investigate the effects of doxazosin, sildenafil, and their combination on bladder tissue contractility and adrenergic receptor (AR) and inducible nitric oxide synthase (iNOS) expression utilizing a male rat model of partial urethral obstruction (PUO). METHODS: Thirty male Sprague Dawley rats were divided into five groups. Except the SHAM group, all animals in remaining four groups underwent surgery for PUO. No further treatment was given to the first group (NT group)...
October 29, 2016: Neurourology and Urodynamics
https://www.readbyqxmd.com/read/27782749/lower-physical-fitness-in-patients-with-primary-aldosteronism-is-linked-to-the-severity-of-hypertension-and-kalaemia
#14
V Tuka, M Matoulek, T Zelinka, J Rosa, O Petrák, O Mikeš, Z Krátká, B Štrauch, R Holaj, J Widimský
Hypokalaemia as a typical feature of primary aldosteronism (PA) is associated with muscle weakness and could contribute to lower cardiopulmonary fitness. The aim of this study was to describe cardiopulmonary fitness and exercise blood pressure and their determinants during a symptom-limited exercise stress test in patients with PA. We performed a cross-sectional study of patients with confirmed PA who were included before adrenal vein sampling on whom a symptom-limited exercise stress test with expired gas analysis was performed...
October 26, 2016: Physiological Research
https://www.readbyqxmd.com/read/27761703/intraoperative-floppy-iris-syndrome-and-its-association-with-various-concurrent-medications-bulbus-length-patient-age-and-gender
#15
Michael Wahl, Saskia M Tipotsch-Maca, Pia V Vecsei-Marlovits
PURPOSE: To evaluate the association between intraoperative floppy iris syndrome (IFIS) and concurrent medications containing selective alpha1A receptor antagonists as well as nonselective alpha1-adrenergic receptor antagonists, bulbus length, patient age and gender. METHODS: We performed a prospective data acquisition of IFIS occurrence and grading, and retrospective evaluation of concurrent medications, bulbus length, patient age and gender of all patients undergoing cataract surgery over a 6-month period...
January 2017: Graefe's Archive for Clinical and Experimental Ophthalmology
https://www.readbyqxmd.com/read/27754015/br-04-1management-of-treatment-resistant-hypertension
#16
David John Webb
Treatment-resistant hypertension (TRH) is defined as the failure to achieve an office BP target of <140/90 mmHg (<130/80 mmHg in patients with chronic kidney disease (CKD) or diabetes) in patients with hypertension (HT), despite adherence to at least 3 antihypertensive medications at optimal tolerated doses, ideally including a diuretic (Calhoun et al., Circulation 2008). TRH identifies patients with hard-to-treat HT, who might benefit from specialist investigation and treatment. Although some studies put the prevalence of TRH as >10%, these levels may be inflated by white-coat hypertension and poor adherence...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27753973/os-11-06-the-effect-of-vagus-nerve-stimulation-on-arterial-hypertension-using-active-implantable-device
#17
Sekib Sokolovic, Samir Mehmedagic
OBJECTIVE: The goal of this paper was to present the effects of the vagus nerve stimulation (VNS) on a blood pressure (BP) and heart rate (HR) in arterial hypertension patient. DESIGN AND METHOD: The pilot study (SPM-005) was designed to evaluate the eficiancy and safety profile of the neurostimulation of the cholinergic anti-inflammatory pathways using the active implantable device for the vagus nerve stimulation in rheumatoid arthritis patient. We investigated the VNS on the BP and HR in 68 years old female patient with a long-standing arterial hypertension and the lisinopril and hydrochlorothiazide in a therapy...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27753923/os-04-07-the-comparative-effectiveness-of-4th-line-anti-hypertensive-agents-in-patients-with-resistant-hypertension-a-meta-analysis
#18
Sarah-Jo Sinnott, Adrian Root, Rohini Mathur, Kathryn Mansfield, Laurie Tomlinson, Ian Douglas
OBJECTIVE: Recent evidence points to the effectiveness of spironolactone vs placebo in the treatment of resistant hypertension (RH). However, placebo is rarely a realistic treatment choice in uncontrolled hypertension. Using meta-analysis, we assessed the effectiveness of alternative 4 line anti-hypertensive agents in comparison to 4 line spironolactone/eplenerone in RH. DESIGN AND METHOD: Pubmed, EMBASE and the Cochrane library were systematically searched for randomised and non-randomised studies that compared any 4 line anti-hypertensive agent to spironolactone/eplenerone in RH...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27753873/ish-aha-2-a-case-of-chronic-indolent-pheochromocytoma-which-caused-medically-controlled-hypertension-but-treatment-resistant-diabetes-mellitus
#19
Hae-Young Lee, Chan-Soon Park, Sang-Hoon Na, Kyung-Jin Kim, Chan Joo Lee, Sungha Park
A 47-year-old woman was admitted via emergency department due to dyspnea NYHA Fc II-III aggravated for 2 months after upper respiratory infection. Her height and body weight were 161 cm / 67 kg. Initial vital signs were 110/70 mmHg - 112 BPM - 24/min - 36.5°C. Chest PA showed cardiomegaly and pulmonary congestion (Figure 1). B-natriuretic peptide level was markedly increased (2002 pg/mL, normal range ≤ 100 pg/mL). The echocardiographic examination showed severely dilated LV cavity (61/72 mm) and severe LV systolic dysfunction (EF 28%) with normal left ventricular wall thickness (9/11 mm) (Figure 2)...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27725022/inappropriate-medicine-prescribing-in-older-south-africans-a-cross-sectional-analysis-of-medicine-claims-data
#20
J A Van Heerden, J R Burger, J J Gerber
BACKGROUND: Prescribing for older patients is a well-recognised problem, and inappropriate items are prescribed frequently. Several tools and criteria are available to promote rational prescribing in older patients. OBJECTIVE: To determine the prevalence of potentially inappropriate prescriptions (PIPs) in older South African patients. METHODS: A retrospective drug utilisation review was conducted using medicine claims data over a 1-year period...
September 9, 2016: South African Medical Journal, Suid-Afrikaanse Tydskrif Vir Geneeskunde
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