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Glucocorticoid receptor antagonism by cyproterone acetate and RU486.
The steroid compound cyproterone acetate was identified in a high-throughput screen for glucocorticoid receptor (GR) binding compounds. Cyproterone (Schering AG) is clinically used as an antiandrogenExpand
Antihypertensive and natriuretic effects of CGS 30440, a dual inhibitor of angiotensin-converting enzyme and neutral endopeptidase 24.11.
Dual angiotensin-converting enzyme (ACE)/neutral endopeptidase (NEP) inhibitors, by decreasing angiotensin-II production and by preventing the degradation of atrial natriuretic peptide (ANP), may beExpand
Elevated arterial cyclic AMP levels during the onset of renal hypertension in rats.
1. To determine the possible role of arterial cyclic AMP in the pathogenesis of hypertensive vascular hypertrophy and hyperplasia, the changes in the level of this nucleotide were studied during theExpand
Elevated arterial cyclic AMP levels during the development of spontaneous hypertension in rats.
Vascular cyclic AMP alterations were studied during the initiation of vascular hypertrophy and hyperplasia in spontaneously hypertensive rats (SHR). The onset of hypertension at 6 weeks of ageExpand
Effects of continuous infusions of 4-hydroxyoestradiol and oestradiol on plasma LH-levels in the ovariectomized ewe.
Ovariectomized ewes were infused over a period of 12 h at constant rates with different doses of the catecholoestrogen 4-hydroxyoestradiol (4-OHE2) or the primary oestrogen oestradiol (E2) via aExpand
Antihypertensive effects of CGS 19281A, an inhibitor of phenylethanolamine-N-methyltransferase.
In experimental hypertension, phenylethanolamine-N-methyltransferase (PNMT) activity and adrenaline levels are elevated in brainstem centers involved in cardiovascular regulation. Known PNMTExpand
Perhydroquinolylbenzamides as novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
High-throughput screening identified 5 as a weak inhibitor of 11beta-HSD1. Optimization of the structure led to a series of perhydroquinolylbenzamides, some with low nanomolar inhibitory potency. AExpand
Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides.
High DGAT1 expression levels in the small intestine highlight the critical role this enzyme plays in nutrient absorption. Identification of inhibitors which predominantly inhibit DGAT1 in the gut isExpand
Development of two-kidney Goldblatt hypertension in rats under dietary sodium restriction.
In Sprague-Dawley rats with unilateral renal artery stenosis and an intact contralateral kidney, administration of a low-sodium diet did not prevent the development of hypertension. Despite anExpand
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