An endothelin B receptor‐selective antagonist: IRL 1038, [Cys 11 ‐Cys 15 ]‐endothelin‐1(11–21)
1992; Wiley; Volume: 311; Issue: 1 Linguagem: Inglês
10.1016/0014-5793(92)81355-p
ISSN1873-3468
AutoresYoshihiro Urade, Yasushi Fujitani, Kyoko Oda, Tadashi Watakabe, Ichiro Umemura, Michihiro Takai, Toshikazu Okada, Kiyoshi Sakata, Hideaki Kiraki,
Tópico(s)Renin-Angiotensin System Studies
ResumoIn the inhibition of specific binding or [ 125 ]endothelins (ETs) to membranes from various tissues of rats, guinea pigs, pigs and humans, [Cys 11 ‐Cys 15 ]‐ET‐1(11–21), IRL 1038, has a much higher affinity for ET B receptors ( K i = 6–11 nM) than for ET A receptors ( K i = 0.4–0.7 μM). In contraction assays, with ET‐3 as a stimulant, 3 μM IRL 1038 antagonized the ET B receptor‐mediated contraction of guinea pig ileal and tracheal smooth muscle without any significant agonistic activity, but did not effect the ET A receptor‐mediated contraction of rat aortic smooth muscle. IRL 1038 is, therefore, considered to be the first antagonist selective to the ET B receptor.
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