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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
Tyrosine hydroxylase- and nitric oxide synthase-immunoreactive nerve fibers in mitral valve of young adult and aged Fischer 344 rats.
Using confocal fluorescence microscopy we studied, in whole mounts of heart mitral valves of young adult and aged Fischer 344 rats, the distribution of nerves containing the catecholamine markerExpand
Novel and potent BK channel openers: CGS 7181 and its analogs
This article discloses the identification of a novel series of the opener of the large‐conductance Ca2+‐activated K+ (BK) channel, CGS 7181, and its analogs, CGS 7184, CGS 7590, and CGS 7725. TheExpand
New alpha-thiol dipeptide dual inhibitors of angiotensin-I converting enzyme and neutral endopeptidase EC
Dual inhibitors of the two zinc metallopeptidases, neutral endopeptidase (NEP, EC and angiotensin-I converting enzyme, have been the focus of much clinical interest for the treatment ofExpand
Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88.
Small molecule modulators of GPR88 activity (agonists, antagonists, or modulators) are of interest as potential agents for the treatment of a variety of psychiatric disorders including schizophrenia.Expand
The discovery of potent agonists for GPR88, an orphan GPCR, for the potential treatment of CNS disorders.
Modulating GPR88 activity is suggested to have therapeutic utility in the treatment of CNS disorders, such as schizophrenia. This Letter will describe the discovery and SAR development of a class ofExpand
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
Differential effects of the BKCa channel openers NS004 and NS1608 in porcine coronary arterial cells.
The effects of newly claimed BKCa channel openers NS004 (5-trifluoromethyl-(5-chloro-2-hydroxyphenyl)-1,3-dihydro-2H-benzimidazo le-2- one) and NS1608Expand
Pharmacological characterization of AMP 579, a novel adenosine A1/A2 receptor agonist and cardioprotective
AMP 579 1S‐[1α,2β,3β,4α(S*)]‐4‐[7‐[[1‐[(3‐chloro‐2‐thienyl)methyl]propylamino]‐3H‐imidazo[4,5‐b]pyridin‐3‐yl]‐N‐ethyl‐2,3‐dihydroxy cyclopentanecarboxamide) is a novel cardioprotective adenosineExpand
Effects of the ECE/NEP inhibitor CGS 34225 on the big ET-1-induced pressor response and plasma atrial natriuretic peptide concentration in conscious rats.
CGS 34226 is a thiol-containing, potent dual inhibitor of endothelin converting enzyme-1 (ECE-1) and neutral endopeptidase 24.11 (NEP) with IC(50) values of 11 and 5 nM respectively. The purpose ofExpand