• Publications
  • Influence
Glucocorticoid receptor antagonism by cyproterone acetate and RU486.
TLDR
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.
Novel and potent BK channel openers: CGS 7181 and its analogs
TLDR
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 3.4.24.11.
TLDR
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.
TLDR
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.
Antihypertensive and natriuretic effects of CGS 30440, a dual inhibitor of angiotensin-converting enzyme and neutral endopeptidase 24.11.
TLDR
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.
...
...