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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.
Tyrosine hydroxylase- and nitric oxide synthase-immunoreactive nerve fibers in mitral valve of young adult and aged Fischer 344 rats.
Novel and potent BK channel openers: CGS 7181 and its analogs
It is concluded that CGS 7181 and its analogs directly open BK channels from either side of the membrane with a combination of potency and efficacy superior to any known BK channel openers, and an internal site of action best accounts for the results of the authors' studies.
Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88.
New alpha-thiol dipeptide dual inhibitors of angiotensin-I converting enzyme and neutral endopeptidase EC 126.96.36.199.
- C. Fink, Y. Qiao, C. Berry, Y. Sakane, R. Ghai, A. Trapani
- Biology, ChemistryJournal of medicinal chemistry
- 22 December 1995
A novel series of alpha-thio dipeptides containing central cyclic non-natural amino acids were prepared and were evaluated for their ability to inhibit these two metallopeptidases in vitro and in vivo and several were found to be excellent dual inhibitors of ACE and NEP in vitro.
Diaminoindanes as microsomal triglyceride transfer protein inhibitors.
- G. Ksander, R. Dejesus, A. Hospattankar
- Chemistry, BiologyJournal of medicinal chemistry
- 21 November 2001
In normolipidemic rats and dogs, oral administration of 8aR dose-dependently reduced both plasma triglycerides and total cholesterol and hepatic lipid accumulation resulted in negligible change in total liver weight and was reversible after withdrawal of the compound.
The discovery of potent agonists for GPR88, an orphan GPCR, for the potential treatment of CNS disorders.
Differential effects of the BKCa channel openers NS004 and NS1608 in porcine coronary arterial cells.
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.