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Inhibition of biological actions of big endothelin-1 by phosphoramidon.

Abstract：

:Endothelin (ET)-1 and big ET-1 both caused contraction of isolated porcine coronary arteries, but the potency of big ET-1 was 1/100-1/200 that of ET-1. These responses were independent of the vascular endothelium. Phosphoramidon blocked the vasoconstriction caused by 30 nM big ET-1, but was ineffective on the action of 0.3 nM ET-1. Also in vivo, phosphoramidon had no effect on the ET-1-induced pressor actions, but blocked the pressor and airway-contractile responses to big ET-1 in rats and/or guinea pigs. Thus, it is likely that the vascular responses to exogenous big ET-1 are at least in part due to its conversion to ET-1 by a phosphoramidon-sensitive ET converting enzyme(s) in the vascular smooth muscle in vitro and in vivo.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Fukuroda T,Noguchi K,Tsuchida S,Nishikibe M,Ikemoto F,Okada K,Yano M

doi

10.1016/0006-291x(90)90685-g

subject

Has Abstract

pub_date

1990-10-30 00:00:00

pages

390-5

issue

2

eissn

0006-291X

issn

1090-2104

pii

0006-291X(90)90685-G

journal_volume

172

pub_type

杂志文章

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