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Glucocorticoid receptor antagonism by cyproterone acetate and RU486.
Cyproterone may inhibit transactivation of the GR by a molecular mechanism recently described as passive antagonism, and new therapeutic profiles may result from compounds designed to selectively stabilize the inactive and active conformations of certain nuclear receptors.
Antihypertensive and natriuretic effects of CGS 30440, a dual inhibitor of angiotensin-converting enzyme and neutral endopeptidase 24.11.
- R. Chatelain, R. Ghai, C. Fink
- Medicine, BiologyThe Journal of pharmacology and experimental…
- 1 March 1998
It is demonstrated that CGS 30440 is an orally active agent which produces tissue ACE and NEP inhibition in rats and plasma ACE inhibition in primates and suggest that the compound may be useful in the treatment of hypertension and congestive heart failure.
Elevated arterial cyclic AMP levels during the onset of renal hypertension in rats.
- R. Chatelain
- Biology, MedicineClinical science
- 1 March 1983
A marked increase in arterial cyclic AMP precedes the initiation of DNA replication and collagen accumulation in vascular territories subjected to high blood pressure, suggesting the participation of this nucleotide in the vascular growth induced by hypertension.
Impaired arterial collagen and elastin metabolism in experimental malignant hypertension.
Elevated arterial cyclic AMP levels during the development of spontaneous hypertension in rats.
Effects of continuous infusions of 4-hydroxyoestradiol and oestradiol on plasma LH-levels in the ovariectomized ewe.
- G. Emons, C. Brack, R. Chatelain, H. Abel, S. Isedor, P. Ball
- Biology, MedicineActa endocrinologica
- 1 November 1984
4-OHE2 had to be infused at 4-5 times higher rates than E2 to obtain comparable plasma concentrations of either oestrogen and under this condition the effects of E2 were similar indicating that 4- OHE2 has the same potency as E2 at central target sites.
Antihypertensive effects of CGS 19281A, an inhibitor of phenylethanolamine-N-methyltransferase.
- R. Chatelain, M. J. Manniello, B. Dardik, M. Rizzo, K. Brosnihan
- Biology, MedicineThe Journal of pharmacology and experimental…
In experimental hypertension, phenylethanolamine-N-methyltransferase (PNMT) activity and adrenaline levels are elevated in brainstem centers involved in cardiovascular regulation and CGS 19281A may be useful for the study of the function of PNMT and adrenaline in the central nervous system.
Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides.
This report describes the discovery and optimization of DGAT1 inhibitors whose plasma exposure is minimized by the action of transporters, including the P-glycoprotein transporter, which has a unique absorption profile on efficacy in rat and dog efficacy models.
Perhydroquinolylbenzamides as novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
- G. Coppola, P. Kukkola, R. Chatelain
- Chemistry, BiologyJournal of medicinal chemistry
- 16 September 2005
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. A…