34,641 results match your criteria receptor blockers


Preliminary study of ovariectomy and chronic losartan-induced alterations in brain AT receptors.

Brain Res 2021 May 12:147520. Epub 2021 May 12.

College of Pharmacy, Nova Southeastern University, Fort Lauderdale, FL; Department of Pharmacology and Physiology, School of Medicine, Georgetown University, Washington, DC. Electronic address:

Women who undergo oophorectomy prior to the age of natural menopause have a higher risk of neurological and psychological impairment. Treatment with the angiotensin receptor blocker (ARB) losartan for 10 weeks following ovariectomy of Long-Evans rats at 3 months of age reduced the ovariectomy-induced cognitive decrements. Following completion of the behavioral experiments, (Campos et al. Read More

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Nitrosamine contamination in pharmaceuticals: threat, impact, and control.

J Pharm Sci 2021 May 11. Epub 2021 May 11.

Department of Food and Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand. Electronic address:

Nitrosamine-contaminated medicinal products have raised safety concerns towards the use of various drugs, not only valsartan and all tetrazole-containing angiotensin II receptor blockers, but also ranitidine, metformin, and other medicines, many of which have been recalled and prone to shortage. At any stages, from drug substance synthesis throughout each product's lifetime, these impurities may evolve if an amine reacts with a nitrosating agent coexisting under appropriate conditions. Consequently, drug regulatory authorities worldwide have established stringent guidelines on nitrosamine contamination for all drug products in the market. Read More

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The Aging GABAergic System and Its Nutritional Support.

Authors:
Demetra J Mills

J Nutr Metab 2021 25;2021:6655064. Epub 2021 Apr 25.

Patent Trial and Appeal Board Biotechnology, 5232 Capon Hill Pl, Burke, VA 22015, USA.

Aging is associated with a decline in hormones and an associated decline in GABAergic function and calcium and ion current dysregulation. Neurosteroid hormones act as direct calcium channel blockers, or they can act indirectly on calcium channels through their interaction with GABA receptors. The calcium channel dysfunction associated with hormone loss further leads to an excitatory cell state, which can ultimately lead to cell death. Read More

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Uncovering Modern Clinical Applications of Fuzi and Fuzi-Based Formulas: A Nationwide Descriptive Study With Market Basket Analysis.

Front Pharmacol 2021 27;12:641530. Epub 2021 Apr 27.

Graduate Institute of Natural Products, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan.

As time evolved, traditional Chinese medicine (TCM) became integrated into the global medical system as complementary treatments. Some essential TCM herbs started to play a limited role in clinical practices because of Western medication development. For example, Fuzi (Aconiti Lateralis Radix Praeparata) is a toxic but indispensable TCM herb. Read More

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Structural insights into ligand recognition and activation of angiotensin receptors.

Trends Pharmacol Sci 2021 May 10. Epub 2021 May 10.

Research Center for Molecular Mechanisms of Aging and Age-Related Diseases, Moscow Institute of Physics and Technology, Dolgoprudny, Moscow Region, Russia; Bridge Institute, Departments of Chemistry and Biological Sciences, University of Southern California, Los Angeles, CA, USA. Electronic address:

G protein-coupled angiotensin II receptors, ATR and ATR, are integral components of the renin-angiotensin system (RAS) that regulates blood pressure and fluid balance in humans. While ATR is a well-established target of angiotensin receptor blockers (ARBs) for managing hypertension and a prime system for studying biased signaling, ATR has been recognized as a promising target against neuropathic pain and lung fibrosis. In this review, we discuss how recent structural advances illuminate ligand-binding modes and subtype selectivity, shared and distinct features of the receptors, their transducer-coupling patterns, and downstream signaling responses. Read More

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A Novel Report on the Compassionate Use of Baricitinib in Treating a Pediatric Patient With Severe Symptoms of COVID-19 Infection.

J Med Cases 2021 Mar 19;12(3):94-98. Epub 2021 Jan 19.

Richmond University Medical Center, Staten Island, NY, USA.

Since the outbreak of the pandemic coronavirus disease 2019 (COVID-19), there has been an increasing need for treatment to decrease morbidity and mortality of patients presenting with severe disease symptoms. There has been increasing evidence to suggest that the pathophysiological basis is a severe inflammatory response that resembles the cytokine release syndrome. Current strategies to counteract this involve modifiers of the immune response such as interleukin (IL)-6 receptor blockers and Janus kinase (JAK) inhibitors. Read More

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Associations Between the Use of Renin-Angiotensin System Inhibitors and the Risks of Severe COVID-19 and Mortality in COVID-19 Patients With Hypertension: A Meta-Analysis of Observational Studies.

Front Cardiovasc Med 2021 26;8:609857. Epub 2021 Apr 26.

Peking University People's Hospital, Beijing, China.

Angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) share a target receptor with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The use of ACEIs/ARBs may cause angiotensin-converting enzyme 2 receptor upregulation, facilitating the entry of SARS-CoV-2 into host cells. There is concern that the use of ACEIs/ARBs could increase the risks of severe COVID-19 and mortality. Read More

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Impact of in-hospital discontinuation with angiotensin receptor blockers or converting enzyme inhibitors on mortality of COVID-19 patients: a retrospective cohort study.

BMC Med 2021 05 12;19(1):118. Epub 2021 May 12.

Department of Cardiology, University Hospital Príncipe de Asturias, Alcalá de Henares, Madrid, Spain.

Background: In the first wave of the COVID-19 pandemic, the hypothesis that angiotensin receptor blockers (ARBs) and angiotensin-converting enzyme inhibitors (ACEIs) increased the risk and/or severity of the disease was widely spread. Consequently, in many hospitals, these drugs were discontinued as a "precautionary measure". We aimed to assess whether the in-hospital discontinuation of ARBs or ACEIs, in real-life conditions, was associated with a reduced risk of death as compared to their continuation and also to compare head-to-head the continuation of ARBs with the continuation of ACEIs. Read More

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Effects of a β2-adrenergic receptor blocker on experimental periodontitis in spontaneously hypertensive rats.

Life Sci 2021 May 9;277:119593. Epub 2021 May 9.

Department of Orthodontics, School of Dentistry, Aichi Gakuin University, 2-11 Suemoridori, Chikusa-ku, Nagoya, Aichi 464-8651, Japan.

Aims: Recent studies have reported a relationship between periodontal disease and hypertension, and previous evidence suggests that the sympathetic nervous system plays an important role in the control of bone metabolism. This study sought to evaluate the effect of the beta-2 adrenergic receptor (β2-AR) blocker butoxamine on experimental periodontitis in a rat model.

Materials And Methods: Wistar-Kyoto and spontaneously hypertensive rats (n = 6 per group) were orally administered butoxamine 1 mg/kg/day and experimental periodontitis was induced by applying an orthodontic ligature wire. Read More

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Small-Molecule Inhibitors of the Coronavirus Spike: ACE2 Protein-Protein Interaction as Blockers of Viral Attachment and Entry for SARS-CoV-2.

ACS Infect Dis 2021 May 12. Epub 2021 May 12.

Inhibitors of the protein-protein interaction (PPI) between the SARS-CoV-2 spike protein and human ACE2 (hACE2), which acts as a ligand-receptor pair that initiates the viral attachment and cellular entry of this coronavirus causing the ongoing COVID-19 pandemic, are of considerable interest as potential antiviral agents. While blockade of such PPIs with small molecules is more challenging than that with antibodies, small-molecule inhibitors (SMIs) might offer alternatives that are less strain- and mutation-sensitive, suitable for oral or inhaled administration, and more controllable/less immunogenic. Here, we report the identification of SMIs of this PPI by screening our compound library focused around the chemical space of organic dyes. Read More

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Impact of heart failure drug therapy on rates of gastrointestinal bleeding in LVAD recipients: An INTERMACS analysis.

Int J Artif Organs 2021 May 12:3913988211013366. Epub 2021 May 12.

Division of Cardiology, Department of Medicine, NewYork-Presbyterian Hospital, Columbia University, New York, NY, USA.

Introduction: Gastrointestinal bleeding (GIB) remains a common and vexing complication of left ventricular assist device (LVAD) support. Recent single-center analyses suggest that ACE inhibitors (ACEi)/angiotensin receptor blockers (ARB) and digoxin may prevent GIB in LVAD patients. Here we evaluate the effect of guideline-directed medical therapies (GDMT) for heart failure (HF) on rates of GIB through analysis of the INTERMACS registry database. Read More

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An update on emerging therapeutics to combat COVID-19.

Basic Clin Pharmacol Toxicol 2021 May 11. Epub 2021 May 11.

Division of Veterinary Parasitology, Faculty of Veterinary Sciences and Animal Husbandry, Sher-e-Kashmir University of Agricultural Sciences and Technology of Jammu, R.S Pura-181102, J & K, India.

Background: The COVID-19 pandemic has demanded effective therapeutic protocol from researchers and clinicians across the world. Currently, a large amount of primary data have been generated from several preclinical studies. At least 300 clinical trials are underway for drug repurposing against COVID-19; the clinician needs objective evidence-based medication to treat COVID-19. Read More

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Randomized Prospective Open Label Study Shows No Impact on Clinical Outcome of Adding Losartan to Hospitalized COVID-19 Patients with Mild Hypoxemia.

Infect Dis Ther 2021 May 11. Epub 2021 May 11.

Sharp Memorial Hospital, Sharp Memorial Research Pharmacy, 7901 Frost Street, San Diego, CA, 92123, USA.

Introduction: Despite considerable scientific debate, there have been no prospective clinical studies on the effects of angiotensin II receptor blockers (ARBs) on the course of COVID-19 infection. Losartan is the ARB that was chosen to be tested in this study.

Methods: Patients with COVID-19 and mild hypoxia (receipt of ≤ 3 L/min O by nasal cannula) admitted to three hospitals were randomized in a 1:1 ratio within 72 h of SARS-CoV-2 nucleic acid testing confirmation to prospectively receive standard of care (SOC) alone or SOC plus losartan 12. Read More

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Targeting Treg cells with GITR activation alleviates resistance to immunotherapy in murine glioblastomas.

Nat Commun 2021 May 11;12(1):2582. Epub 2021 May 11.

Edwin L. Steele Laboratories, Department of Radiation Oncology, Massachusetts General Hospital (MGH) and Harvard Medical School (HMS), Boston, MA, USA.

Immune checkpoint blockers (ICBs) have failed in all phase III glioblastoma (GBM) trials. Here, we show that regulatory T (Treg) cells play a key role in GBM resistance to ICBs in experimental gliomas. Targeting glucocorticoid-induced TNFR-related receptor (GITR) in Treg cells using an agonistic antibody (αGITR) promotes CD4 Treg cell differentiation into CD4 effector T cells, alleviates Treg cell-mediated suppression of anti-tumor immune response, and induces potent anti-tumor effector cells in GBM. Read More

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Shocking HIV-1 with immunomodulatory latency reversing agents.

Semin Immunol 2021 May 7:101478. Epub 2021 May 7.

Service of Molecular Virology, Department of Molecular Virology (DBM), Université Libre de Bruxelles (ULB), Gosselies, Belgium. Electronic address:

The "shock-and-kill" strategy is one of the most explored HIV-1 cure approaches to eliminate latent virus. This strategy is based on HIV-1 reactivation using latency reversing agents (LRAs) to reactivate latent proviruses (the "shock" phase) and to induce subsequent elimination of the reactivated cells by immune responses or virus-induced cytopathic effects (the "kill" phase). Studies using immunomodulatory LRAs such as blockers of immune checkpoint molecules, toll-like receptor agonists, cytokines and CD8 T cell depleting antibodies showed promising potential as LRAs inducing directly or indirectly cellular pathways known to control HIV transcription. Read More

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Prognostic association of medication trajectories with 3-year mortality in heart failure and preserved ejection fraction: findings from the EPICAL2 cohort study.

Eur J Clin Pharmacol 2021 May 10. Epub 2021 May 10.

APEMAC, Université de Lorraine, 54000, Nancy, France.

Purpose: The aims of this study were to describe combinations of beta-blockers (BB), renin-angiotensin system (RAS) blockers, and mineralocorticoid receptor antagonist (MRA) prescriptions and their trajectories in heart failure with preserved ejection fraction (HFpEF) patients, and to assess their effect on the three-year all-cause and cardiovascular (CV)-mortality.

Methods: We used data from the EPICAL2 cohort of 689 hospitalized HFpEF patients. Medication prescriptions were collected at hospital discharge and at 6, 12, and 24 months after discharge. Read More

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Angiotensin II Receptor Blockers but Not Angiotensin-Converting Enzyme Inhibitors Are Associated With a Reduced Risk of Acute Kidney Injury After Major Surgery.

Front Pharmacol 2021 23;12:662301. Epub 2021 Apr 23.

Department of Internal Medicine, National Taiwan University Hospital and College of Medicine, Taipei, Taiwan.

We investigated the respective effects of preoperative angiotensin-converting-enzyme inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) on the incidence of postoperative acute kidney injury (AKI) and mortality. In this nested case-control study, we enrolled 20,276 patients who received major surgery. We collected their baseline demographic data, comorbidities and prescribed medication, the outcomes of postoperative AKI and mortality. Read More

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Predictors of adherence to composite therapy after acute coronary syndromes.

J Cardiovasc Med (Hagerstown) 2021 May 6. Epub 2021 May 6.

Division of Cardiology, Department of Advanced Biomedical Sciences, University of Napoli 'Federico II', Napoli, Italy.

Aims: Adherence to medical therapy following acute coronary syndrome (ACS) affects a patient's prognosis. In this cohort study, we sought to assess the factors that could affect a patient's adherence to therapy after ACS.

Methods: We prospectively collected information from patients (N = 964) hospitalized at the coronary care unit of the Federico II University Hospital, from 1 January 2015 to 30 June 2017, for ACS. Read More

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β1-blocker in sepsis.

J Intensive Care 2021 May 8;9(1):39. Epub 2021 May 8.

Department of Anesthesiology and Critical Care Medicine, Fujita Health University School of Medicine, 1-98 Dengakugakubo, Kutsukake-cho, Toyoake, Aichi, 470-1192, Japan.

Background: The use of ultrashort-acting β1-blockers recently has attracted attention in septic patients with non-compensatory tachycardia. We summarized the metabolic and hemodynamic effects and the clinical evidence of ultrashort-acting β1-blockers.

Main Body: A recent meta-analysis showed that ultrashort-acting β1-blockers reduced the mortality in septic patients with persistent tachycardia. Read More

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Quality of care and risk of incident atrial fibrillation in patients with newly-diagnosed heart failure: A nationwide cohort study.

Eur Heart J Qual Care Clin Outcomes 2021 May 7. Epub 2021 May 7.

Danish Center for Clinical Health Services Research, Aalborg University, Aalborg, Denmark.

Aims: Incident atrial fibrillation (AF) is an adverse prognostic indicator in heart failure (HF); identifying modifiable targets may be relevant to reduce the incidence and morbidity of AF. Therefore, we examined the association between quality of HF care and risk of AF.

Methods And Results: Using the Danish Heart Failure Registry, we conducted a nationwide registry-based cohort study of all incident HF patients diagnosed between 2008 and 2018 and without history of AF. Read More

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Knockout of immunotherapy prognostic marker genes eliminates the effect of the anti-PD-1 treatment.

NPJ Precis Oncol 2021 May 7;5(1):37. Epub 2021 May 7.

Department of Basic Medical Science, School of Medicine, Tsinghua University, Beijing, China.

The efficacy of immunotherapy is largely patient-specific due to heterogeneity in tumors. Combining statistic power from a variety of immunotherapies across cancer types, we found four biological pathways significantly correlated with patient survival following immunotherapy. The expression of immunotherapy prognostic marker genes (IPMGs) in these pathways can predict the patient survival with high accuracy not only in the TCGA cohort (89. Read More

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Sphingosine 1-phosphate, a potential target in neovascular retinal disease.

Br J Ophthalmol 2021 May 7. Epub 2021 May 7.

School of Pharmacy, University College Cork, Cork, Ireland

Neovascular ocular diseases (such as age-related macular degeneration, diabetic retinopathy and retinal vein occlusion) are characterised by common pathological processes that contribute to disease progression. These include angiogenesis, oedema, inflammation, cell death and fibrosis. Currently available therapies target the effects of vascular endothelial growth factor (VEGF), the main mediator of pathological angiogenesis. Read More

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Perceived risk profile and treatment optimization in heart failure: an analysis from BIOlogy Study to TAilored Treatment in chronic heart failure.

Clin Cardiol 2021 May 7. Epub 2021 May 7.

Université de Lorraine, INSERM, Centre d'Investigations Cliniques Plurithématique 1433, Inserm U1116, CHRU de Nancy and F-CRIN INI-CRCT, Nancy, France.

Background: Achieving target doses of angiotensin-converting-enzyme inhibitor/angiotensin-receptor blockers (ACEi/ARB) and beta-blockers in heart failure with reduced ejection fraction (HFrEF) is often underperformed. In BIOlogy Study to TAilored Treatment in chronic heart failure (BIOSTAT-CHF) study, many patients were not up-titrated for which no clear reason was reported. Therefore, we hypothesized that perceived-risk profile might influence treatment optimization. Read More

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The Role of Renin-Angiotensin-Aldosterone System in the Heart and Lung: Focus on COVID-19.

Front Pharmacol 2021 20;12:667254. Epub 2021 Apr 20.

Campania Regional Centre for Pharmacovigilance and Pharmacoepidemiology, Naples, Italy.

The renin-angiotensin-aldosterone system (RAAS) firstly considered as a cardiovascular circulating hormonal system, it is now accepted as a local tissue system that works synergistically or independently with the circulating one. Evidence states that tissue RAAS locally generates mediators with regulatory homeostatic functions, thus contributing, at some extent, to organ dysfunction or disease. Specifically, RAAS can be divided into the traditional RAAS pathway (or classic RAAS) mediated by angiotensin II (AII), and the non-classic RAAS pathway mediated by angiotensin 1-7. Read More

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Effect of medical treatment on heart failure incidence in patients with a systemic right ventricle.

Heart 2021 May 6. Epub 2021 May 6.

Adult Congenital Heart Centre, National Centre for Pulmonary Hypertension, Royal Brompton Hospital, London, UK.

Background: To date, clinical trials have been underpowered to demonstrate a benefit from ACE inhibitors (ACEis) or angiotensin II receptor blockers (ARBs) in preventing systemic right ventricle (sRV) failure and disease progression in patients with transposition of the great arteries (TGA). This observational study aimed to estimate the effect of ACEi and ARB on heart failure (HF) incidence and mortality in a large population of patients with an sRV.

Methods: Data on all patients with an sRV under active follow-up at two tertiary centres between January 2007 and September 2018 were studied. Read More

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