Search results for " antagonist"
showing 10 items of 1421 documents
Atrial fibrillation and chronic kidney disease: focus on rivaroxaban
2015
Renal insufficiency increases the risk of stroke and bleeding in atrial fibrillation patients. Although vitamin K antagonists reduce the risk of stroke in patients with moderate renal dysfunction, this observation is less clear in patients with renal impairment. Moreover, the risk of bleeding with vitamin K antagonists increases as renal function worsens. Maintaining international normalized ratio values within therapeutic targets is more difficult in patients with renal dysfunction, and those agents may cause warfarin-related nephropathy and vascular calcification. Rivaroxaban is the only nonvitamin K oral anticoagulant with a dose specifically tested in patients with moderate renal insuff…
Chemosensory signalling pathways involved in sensing of amino acids by the ghrelin cell
2015
AbstractTaste receptors on enteroendocrine cells sense nutrients and transmit signals that control gut hormone release. This study aimed to investigate the amino acid (AA) sensing mechanisms of the ghrelin cell in a gastric ghrelinoma cell line, tissue segments and mice. Peptone and specific classes of amino acids stimulate ghrelin secretion in the ghrelinoma cell line. Sensing of L-Phe occurs via the CaSR, monosodium glutamate via the TAS1R1-TAS1R3 while L-Ala and peptone act via 2 different amino acid taste receptors: CaSR & TAS1R1-TAS1R3 and CaSR & GPRC6A, respectively. The stimulatory effect of peptone on ghrelin release was mimicked ex vivo in gastric but not in jejunal tissue …
Ovicidal Activity of Maternally Applied Ecdysteroids in the Large Milkweed Bug (Heteroptera: Lygaeidae)
1982
Exogenous ecdysteroids (ecdysone, 20-hydroxyecdysone and makisterone A) administered to reproducing females of Oncopelus fasciatus (Dallas) reduced egg hatch drastically. The ovicidal activity apparently stemmed from ecdysteroids—unchanged hormone or metabolites—transferred from mother into oocyte. Different stages of embryogenesis were affected. Makisterone A, the predominant ecdysteroid in normal embryos, is by far the most effective ecdysteroid.
Disease control and treatment pathways of asthma patients after initiating ICS/LABA
2019
Introduction: GINA guidelines recommend medium dose (MED) and high dose (HD) ICS/LABA as the preferred controller for step 4 asthma patients and clinicians should consider step up/down based on their patients’ asthma control. Limited data is available on how step 4 patients respond to ICS/LABA and how they step up/down in clinical practice. Methods: We conducted a retrospective cohort study using UK Clinical Practice Research Datalink to assess control status of asthma patients in one year after initiating a MED or HD ICS/LABA between 2007 and 2015, and examined their treatment pathways within one year after the treatment initiation. Results: 29,229 and 16, 575 patients initiated MED and HD…
Darstellung und Reaktionen von 2-Methylen-canrenon
1995
Ausgehend vom Mannich-Salz 1 des Aldosteronantagonisten Canrenon oder von 2-Methylen-canrenon (2) wurden die am A-Ring anellierten Hetero- und Carbocyclen 5, 6, 8–13 dargestellt. Mit den Verbindungen 2, 3, 4b, 5, 6b, 8 und 12 wurden Bindungsstudien am Estradiol-, Progesteron-, Androgen-, Glucocorticoid- und Mineralocorticoid-Rezeptor sowie an den Serumproteinen Sexualhormonbindendes Globulin (SHBG) und Corticosteroidbindendes Globulin (CBG) durchgefuhrt. Die relativen Bindungsaffinitaten lagen bei CBG unter 1%, in allen anderen Fallen niedriger als 0.01%. Synthesis and Reactions of 2-Methylene-canrenone Starting from the Mannich salt 1 of the aldosterone antagonist canrenone or from 2-methy…
The future: critical knowledge about anti-itch therapy.
2005
: Itch is an extremely frequent and enervating symptom of many diseases. Current anti-itch therapy, which is based almost exclusively on an “immunocentric” viewpoint, is often unsatisfactory. Recent studies show that this symptom is in fact the result of a complex interplay among skin, nervous system, endocrine system, and immune system. This explains the frequent failure of therapeutic strategies focused only on a single factor and suggests the usefulness of a polypharmacologic symptomatic treatment, designed on a case-by-case basis as a result of a multidisciplinary approach. We discuss the perspectives of anti-itch therapy in light of the new pathogenetic and pharmacologic acquisitions.
Cardiorespiratory fitness is not associated with risk of venous thromboembolism: a cohort study
2019
Objectives. The inverse and independent association between cardiorespiratory fitness (CRF) and arterial thrombotic disease is well established. However, the potential association between CRF and venous thromboembolism (VTE) is not well known. We aimed to assess the prospective association of CRF with the risk of VTE. Design. Cardiorespiratory fitness, as measured by maximal oxygen uptake (VO2max), was assessed using a respiratory gas exchange analyser in 2,249 men aged 42-61 years without a history of VTE at baseline in the Kuopio Ischemic Heart Disease prospective cohort. Cox-regression models were used to calculate hazard ratios (HR) with 95% confidence interval (CI) for VTE. We correcte…
Resistin: An Inflammatory Cytokine. Role in Cardiovascular Diseases, Diabetes and the Metabolic Syndrome
2014
Resistin is an adipocyte- and monocyte-derived cytokine which has been implicated in the modulation of insulin action, energy, glucose and lipid homeostasis. Resistin has been associated with insulin resistance and many of its known complications. As a molecular link between metabolic signals, inflammation, and vascular dysfunction, resistin can be proposed as playing a significant role in the heightened inflammatory state induced by metabolic stress linked to excessive caloric intake, thus contributing to the risk for metabolic syndrome (MetS), type 2 diabetes (T2DM), and cardiovascular diseases (CVD). In this review, we highlighted the role of resistin, as an inflammatory cytokine, in the…
Control of Gastric Acid Secretion in Somatostatin Receptor 2 Deficient Mice: Shift from Endocrine/Paracrine to Neurocrine Pathways
2007
The gastrin-enterochromaffin-like (ECL) cell-parietal cell axis is known to play an important role in the regulation of gastric acid secretion. Somatostatin, acting on somatostatin receptor type 2 (SSTR2), interferes with this axis by suppressing the activity of the gastrin cells, ECL cells, and parietal cells. Surprisingly, however, freely fed SSTR2 knockout mice seem to display normal circulating gastrin concentration and unchanged acid output. In the present study, we compared the control of acid secretion in these mutant mice with that in wild-type mice. In SSTR2 knockout mice, the number of gastrin cells was unchanged; whereas the numbers of somatostatin cells were reduced in the antru…
Increased Connexin 43 Expression as a Potential Mediator of the Neuroprotective Activity of the Corticotropin-Releasing Hormone
2009
CRH is a major central stress mediator, but also a potent neuroprotective effector. The mechanisms by which CRH mediates its neuroprotective actions are largely unknown. Here, we describe that the gap junction molecule connexin43 (Cx43) mediates neuroprotective effects of CRH toward experimentally induced oxidative stress. An enhanced gap junction communication has been reported to contribute to neuroprotection after neurotoxic insults. We show that CRH treatment up-regulates Cx43 expression and gap junctional communication in a CRH receptor-dependent manner in IMR32 neuroblastoma cells, primary astrocytes, and organotypic hippocampal slice cultures. MAPKs and protein kinase A-cAMP response…