Search Results - "Bruseo, C W"

Characterization of a potent and selective endothelin-B receptor antagonist, IRL 2500 by Balwierczak, J L, Bruseo, C W, DelGrande, D, Jeng, A Y, Savage, P, Shetty, S S

“…IRL 2500 [N-(3,5-dimethylbenzoyl)-N-methyl-(D)-(4-phenylphenyl)-alany l-L- tryptophan] inhibited the binding of [125I]-endothelin-1 (ET-1) to human ETB (IC50…”
Get more information

Design and Synthesis of a Potent and Selective Endothelin-Converting Enzyme Inhibitor, CGS 35066 by Jeng, Arco Y, De Lombaert, Stéphane, Beil, Michael E, Bruseo, Charles W, Savage, Paula, Chou, Mary, Trapani, Angelo J

“…CGS 26303 has previously been shown to inhibit human endothelin converting enzyme-1 (ECE-1) with an IC50 of 410 nM and to be efficacious in several animal…”
Get full text

Cgs 34043: A non-peptidic, potent and long-acting dual inhibitor of endothelin converting enzyme-1 and neutral endopeptidase 24.11 by Trapani, Angelo J., De Lombaert, Stéphane, Beil, Michael E., Bruseo, Charles W., Savage, Paula, Chou, Mary, Jeng, Arco Y.

“…Endothelin-1 (ET-1) is a potent vasoconstrictor. Its biosynthesis is catalyzed by endothelin converting enzyme (ECE). In contrast, atrial natriuretic peptide…”
Get full text

Synthesis and biological activity of novel potent endothelin-converting enzyme-1 inhibitors by FIROOZNIA, Fariborz, GUDE, Candido, TRAPANI, Angelo J, JENG, Arco Y, CHAN, Kenneth, FINK, Cynthia A, YING QIAO, SATOH, Yoshitaka, MARCOPOULOS, Nicholas, SAVAGE, Paula, BEIL, Michael E, BRUSEO, Charles W

“…Through directed screening of metalloprotease inhibitors, CGS 30084 (1) has been identified as a potent endothelin-converting enzyme-1 (ECE-1) inhibitor in…”
Get full text

Pharmacological Properties of CGS 35066, a Potent and Selective Endothelin-Converting Enzyme Inhibitor, in Conscious Rats by Trapani, Angelo J, Beil, Michael E, Bruseo, Charles W, De Lombaert, Stéphane, Jeng, Arco Y

“…The purpose of this study was to examine the pharmacologic properties of CGS 35066, a novel aminophosphonate inhibitor of endothelin-converting enzyme-1…”
Get full text

CGS 35601 and its Orally Active Prodrug CGS 37808 as Triple Inhibitors of Endothelin-converting Enzyme-1, Neutral Endopeptidase 24.11, and Angiotensin-converting Enzyme by Trapani, Angelo J, Beil, Michael E, Bruseo, Charles W, Savage, Paula, Firooznia, Fariborz, Jeng, Arco Y

“…CGS 35601 is a potent triple inhibitor of endothelinconverting enzyme-1, neutral endopeptidase 24.11, and angiotensinconverting enzyme. It inhibited the…”
Get full text

CGS 34226, a thiol-based dual inhibitor of endothelin converting enzyme-1 and neutral endopeptidase 24.11 by Jeng, Arco Y, Savage, Paula, Beil, Michael E, Bruseo, Charles W, Hoyer, Denton, Fink, Cynthia A, Trapani, Angelo J

“…Endothelins (ETs) are potent vasoconstrictors and have been implicated in the pathogenesis of various cardiovascular and renal diseases. In contrast, atrial…”
Get more information

Synthesis and biological activity of potent heterocyclic thiol-based inhibitors of endothelin-converting enzyme-1 by Firooznia, Fariborz, Gude, Candido, Chan, Kenneth, Tan, Jenny, Fink, Cynthia A., Savage, Paula, Beil, Michael E., Bruseo, Charles W., Trapani, Angelo J., Jeng, Arco Y.

“…Directed screening of metalloprotease inhibitors identified CGS 30084 ( 1) as a potent inhibitor of endothelin-converting enzyme-1 (ECE-1) in vitro (IC 50=77…”
Get full text

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 by Trapani, Angelo J, Beil, Michael E, Bruseo, Charles W, Fink, Cynthia A, Hoyer, Denton, Savage, Paula, Jeng, Arco Y

“…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…”
Get more information

Pharmacological Properties of CGS 35066, a Potent and Selective Endothelin-Converting Enzyme Inhibitor, in Conscious Rats by Trapani, Angelo J, Beil, Michael E, Bruseo, Charles W, De Lombaert, Stéphane, Jeng, Arco Y

“…The purpose of this study was to examine the pharmacologic properties of CGS 35066, a novel aminophosphonate inhibitor of endothelin-converting enzyme-1…”
Get full text

Dipeptide sulfonamides as endothelin ETA/ETB receptor antagonists by Ksander, Gary M, Shetty, Suraj S, DelGrande, Dominick, Balwierczak, Joseph L, Bruseo, Charles W, Savage, Paula, deJesus, Reynalda, Yuan, Andrew, Webb, Randy L, Jeng, Arco Y

“…Endothelin-1 (ET-1) is a potent mitogen and modulator of vascular tone. It is synthesized and released from endothelial cells and acts upon two receptor…”
Get more information