BIG ENDOTHELIN-3-INDUCED HYPERTENSION AND ITS INHIBITION BY PHOSPHORAMIDON IN ANESTHETIZED RATS

被引:11
作者
MATSUMURA, Y [1 ]
FUJITA, K [1 ]
TAKAOKA, M [1 ]
MORIMOTO, S [1 ]
机构
[1] OSAKA UNIV PHARMACEUT SCI,DEPT PHARMACOL,2-10-65 KAWAI,MATSUBARA,OSAKA 580,JAPAN
关键词
ENDOTHELIN-3; BIG ENDOTHELIN-3; HYPERTENSIVE EFFECT; PHOSPHORAMIDON; METALLOPROTEINASE; (CONVERSION);
D O I
10.1016/0014-2999(93)90414-D
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Intravenous injection of big endothelin-3 (big ET-3, 1-41 amide) at 3 nmol/kg to ganglion-blocked anaesthetized rats produced a long-lasting hypertensive action, but the action was less potent than that seen with the same dose of ET-3-(1-21). The pressor effect induced by big ET-3 was markedly attenuated by pretreatment with phosphoramidon, 5 mg/kg i.v., a dose which had no effect on the hypertensive action induced by ET-3. These results strongly suggest that big ET-3 is converted to mature ET-3 by a phosphoramidon-sensitive metalloproteinase in vivo, in a manner similar to the conversion of big ET-1 to ET-1.
引用
收藏
页码:89 / 93
页数:5
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