| Autor: |
WESSALE, Jerry L., ADLER, Andrew L., NOVOSAD, Eugene I., CALZADILLA, Samuel V., DAYTON, Brian D., MARSH, Kennan C., WINN, Martin, JAE, Hwan-Soo, GELDERN, Thomas W.von, OPGENORTH, Terry J., WU-WONG, J. Ruth |
| Zdroj: |
Clinical Science; September 2002, Vol. 103 Issue: Supplement 2002 p112S-117S, 6p |
| Abstrakt: |
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 (atrasentan), ABT-546, A-182086 and A-192621, which exhibit differences in selectivity for ETA and ETB receptors. In this report, we compare the efficacy, potency and pharmacokinetic properties of these four antagonists, including potency in inhibiting ET-1- or Sarafotoxin 6c-induced vessel constriction in isolated arteries and efficacy in antagonizing ET-1-, big ET-1- or Sarafotoxin 6c-induced pressor responses in rats. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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