In vitro stability and intestinal absorption characteristics of hexapeptide endothelin receptor antagonists

Life Sciences ◽  
1998 ◽  
Vol 63 (18) ◽  
pp. 1599-1609 ◽  
Author(s):  
Hyo-kyung Han ◽  
Barbra H. Stewart ◽  
Annette M. Doherty ◽  
Wayne L. Cody ◽  
Gordon L. Amidon
Keyword(s):  
Intestinal Absorption ◽  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Receptor Antagonists ◽  
In Vitro Stability ◽  
Absorption Characteristics

Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies

2002 ◽  
Vol 103 (s2002) ◽  
pp. 107S-111S ◽  
Author(s):  
J. Ruth WU-WONG ◽  
Douglas B. DIXON ◽  
William J. CHIOU ◽  
Brian K. SORENSEN ◽  
Gang LIU ◽  
...  
Keyword(s):  
Arachidonic Acid ◽  
Amino Acid ◽  
Small Molecule ◽  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Arachidonic Acid Release ◽  
Functional Responses ◽  
Receptor Antagonists ◽  
Acid Release

Endothelins (ETs), 21-amino-acid peptides involved in the pathogenesis of various diseases, bind to ETA and ETB receptors to initiate their effects. Based on the same core structure, we have developed four small-molecule ET receptor antagonists, ABT-627, ABT-546, A-182086 and A-192621, which exhibit difference in selectivity for ETA and ETB receptors. In this report, we compare the potency and selectivity of these four antagonists in inhibiting 125I-labelled ET-1 binding to cloned human ETA and ETB receptors, and in blocking ET-1-induced functional responses (arachidonic acid release and phosphatidylinositol hydrolysis).

In vitro permeability screening for identification of orally bioavailable endothelin receptor antagonists

1997 ◽  
Vol 23 (1-3) ◽  
pp. 99-109 ◽  
Author(s):  
Harma Ellens ◽  
Evangeline P. Eddy ◽  
Chao-Pin Lee ◽  
Phyllis Dougherty ◽  
Amparo Lago ◽  
...  
Keyword(s):  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Receptor Antagonists ◽  
Orally Bioavailable

Synthesis and in vitro evaluation of ambrisentan analogues as potential endothelin receptor antagonists

2011 ◽  
Vol 21 (13) ◽  
pp. 3894-3897 ◽  
Author(s):  
Jun Xia ◽  
Jianfei Song ◽  
Le Zhen ◽  
Xiuling Zhang ◽  
Xiantao Lei ◽  
...  
Keyword(s):  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Receptor Antagonists ◽  
In Vitro Evaluation

ChemInform Abstract: 2-Aryloxycarbonylthiophene-3-sulfonamides: Highly Potent and ETA Selective Endothelin Receptor Antagonists.

ChemInform ◽  
2010 ◽  
Vol 28 (50) ◽  
pp. no-no
Author(s):  
B. RAJU ◽  
C. WU ◽  
R. CASTILLO ◽  
I. OKUN ◽  
F. STAVROS ◽  
...  
Keyword(s):  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Receptor Antagonists
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