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Evidence that the multiflorine‐derived substituted quinazolidine 55P0251 augments insulin secretion and lowers blood glucose via antagonism at α 2 ‐adrenoceptors in mice

Autor: Immanuel Adorjan, Leonhardt Bauer, Clemens Fürnsinn, Karin Stadlbauer, B. Brunmair, Thomas Scherer, Miroslav Genov, Zsuzsanna Lehner, Alexandra Kautzky-Willer, Mika Scheinin

Publikováno v: Diabetes, Obesity & Metabolism

Aims To investigate the mechanism of action of 55P0251, a novel multiflorine‐derived substituted quinazolidine that augments insulin release and lowers blood glucose in rodents, but does not act via mechanisms addressed by any antidiabetic agent in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c6b45da0afccda987f504e676565d5c
https://doi.org/10.1111/dom.13895

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Preclinical characterization of 55P0251, a novel compound that amplifies glucose-stimulated insulin secretion and counteracts hyperglycaemia in rodents

Autor: Leonhardt Bauer, Zsuzsanna Lehner, Anton Luger, Clemens Fürnsinn, Karin Stadlbauer, B. Brunmair, Thomas Scherer, Immanuel Adorjan

Publikováno v: Diabetes, Obesity and Metabolism. 19:1088-1096

Aims 55P0251 is a novel compound with blood glucose lowering activity in mice, which has been developed from a molecular backbone structure found in herbal remedies. We here report its basic pharmacological attributes and initial progress in unmaskin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7a6747d72993e7af6e1f84981b003c6d
https://doi.org/10.1111/dom.12914

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Lipophilicity as a determinant of thiazolidinedione action in vitro: findings from BLX-1002, a novel compound without affinity to PPARs

Autor: Karin Stadlbauer, B. Brunmair, Clemens Fürnsinn, Zsuzsanna Lehner, Katrin Staniek, Charles W. Bolten, Debendranath Dey, Anton Luger

Publikováno v: American Journal of Physiology-Cell Physiology. 300:C1386-C1392

The pharmacology of thiazolidinediones (TZDs) seems to be driven not only by activation of peroxisome proliferator-activated receptor-γ (PPARγ), but also by PPARγ-independent effects on mitochondrial function and cellular fuel handling. This study

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::33e9656bdeea37e22d139f3dd3b1958a
https://doi.org/10.1152/ajpcell.00401.2010

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Effects of free fatty acids on carbohydrate metabolism and insulin signalling in perfused rat liver

Autor: Christian Anderwald, Michael Roden, Michael Krebs, Clemens Fürnsinn, Karin Stadlbauer, B. Brunmair

Publikováno v: European Journal of Clinical Investigation. 37:774-782

Background Elevated circulating free fatty acids (FFAs) induce insulin resistance and play a crucial role in the development of type 2 diabetes, in which fasting hepatic glucose production (HGP) is increased. However, direct effects of FFAs on fastin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4feb7dfc657d3d0ab31f4c48ca62fd5
https://doi.org/10.1111/j.1365-2362.2007.01858.x

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Insulin does not regulate glucose transport and metabolism in human endothelium

Autor: Michaela Artwohl, Clemens Fürnsinn, Sabina Baumgartner-Parzer, Georg Rainer, B. Brunmair, Nicole Huttary, Angelika Freudenthaler, E. M. Porod, T. Hölzenbein

Publikováno v: European Journal of Clinical Investigation. 37:643-650

BACKGROUND: Although endothelial cells express insulin receptors, it is controversially discussed whether the endothelium represents an insulin-responsive tissue. Since available data are primarily restricted to animal endothelial cells, this study t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cc34496691c2c0693e65415ef22bcb98
https://doi.org/10.1111/j.1365-2362.2007.01838.x

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55P0110, a Novel Synthetic Compound Developed from a Plant Derived Backbone Structure, Shows Promising Anti-Hyperglycaemic Activity in Mice

Autor: Clemens Fürnsinn, Zsuzsanna Lehner, Klaus Frobel, Anton Luger, Immanuel Adorjan, Leonhardt Bauer, Karin Stadlbauer, B. Brunmair, Thomas Scherer

Publikováno v: PLoS ONE, Vol 10, Iss 5, p e0126847 (2015)
PLoS ONE

Starting off with a structure derived from the natural compound multiflorine, a derivatisation program aimed at the discovery and initial characterisation of novel compounds with antidiabetic potential. Design and discovery of the structures was guid

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e98558685b4482432aa3ca890d9d0dc
http://europepmc.org/articles/PMC4431753?pdf=render

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Peroxisome proliferator-activated receptor-δ, a regulator of oxidative capacity, fuel switching and cholesterol transport

Autor: Clemens Fürnsinn, T. M. Willson, B. Brunmair

Publikováno v: Diabetologia. 50:8-17

Synthetic agonists of peroxisome proliferator-activated receptor (PPAR)-delta have shown a promising pharmacological profile in preclinical models of metabolic and cardiovascular disease. At present, the pharmaceutical development of these drugs expl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::837bc726b2c09ab33120cfedda57257b
https://doi.org/10.1007/s00125-006-0492-0

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Expression of uncoupling protein-3 mRNA in rat skeletal muscle is acutely stimulated by thiazolidinediones: an exercise-like effect?

Autor: Werner Waldhäusl, Ludwig Wagner, F. Gras, Michaela Artwohl, Clemens Fürnsinn, B. Brunmair, B. Zierhut

Publikováno v: Diabetologia. 47:1611-1614

We examined whether thiazolidinediones (TZDs) acutely affect uncoupling protein-3 ( UCP-3) expression in skeletal muscle and plasma NEFA in Sprague-Dawley rats.Expression of UCP-3 mRNA in hindlimb muscles and plasma NEFA were measured after a single

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee01a3fe6f26edc9c80672780760cfa1
https://doi.org/10.1007/s00125-004-1488-2

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Mechanisms of antihyperglycaemic action of efaroxan in mice: time for reappraisal of α2A-adrenergic antagonism in the treatment of type 2 diabetes?

Autor: Clemens Fürnsinn, K. Frobel, Anton Luger, Zsuzsanna Lehner, M. Belz, V. A. M. de Cillia, Karin Stadlbauer, B. Brunmair, I. Adorjan, Anna Fenzl, Ingo Rustenbeck, L. Bauer, D. Gruber

Publikováno v: Diabetologia. 55(11)

Inspired by recent speculation about the potential utility of α(2A)-antagonism in the treatment of type 2 diabetes, the study examined the contribution of α(2)-antagonism vs other mechanisms to the antihyperglycaemic activity of the imidazoline (±

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e16d5c9ede677d22aeb0effa697ef845
https://pubmed.ncbi.nlm.nih.gov/22898767

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Progesterone impairs cell respiration and suppresses a compensatory increase in glucose transport in isolated rat skeletal muscle: a non-genomic mechanism contributing to metabolic adaptation to late pregnancy?

Autor: Werner Waldhäusl, Z. Szöcs, L. Quarré, F. Gras, Clemens Fürnsinn, B. Brunmair

Publikováno v: Diabetologia. 50(12)

The aim of the study was to gain better insight into the mechanisms responsible for impaired glucose metabolism during late pregnancy. We explored the direct effects of progesterone on glucose metabolism of skeletal muscle.Specimens of skeletal muscl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::82a2683f81da9ff8c05ca135d6addaa4
https://pubmed.ncbi.nlm.nih.gov/17932647

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