| Autor: |
Breu, Volker, Clozel, Martine, Burri, Kaspar, Hirth, Georges, Neidhart, Werner, Ramuz, Henri |
| Zdroj: |
FEBS Letters; March 1996, Vol. 383 Issue: 1-2 p37-41, 5p |
| Abstrakt: |
We describe here Ro 46‐8443, the first non‐peptide endothelin ETBreceptor selective antagonist. It displays up to 2000‐fold selectivity for ETBreceptors both in terms of binding inhibitory potency and functional inhibition. The observed parallel rightward shift of concentration‐response curves with different antagonist concentrations is consistent with a competitive binding mode. Since Ro 46‐8443 selectively inhibits ETBreceptor mediated responses, it is a valuable tool for clarifying the role of ETBreceptors in pathology. |
| Databáze: |
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