In:
FEBS Letters, Wiley, Vol. 311, No. 1 ( 1992-10-12), p. 12-16
Abstract:
In 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.
Type of Medium:
Online Resource
ISSN:
0014-5793
,
1873-3468
DOI:
10.1016/0014-5793(92)81355-P
Language:
English
Publisher:
Wiley
Publication Date:
1992
detail.hit.zdb_id:
1460391-3
SSG:
12
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