磷酰胺素的鼠李糖部分对于体内抑制内皮素转化酶并非必需。

Rhamnose moiety of phosphoramidon is not required for in vivo inhibition of endothelin converting enzyme.

作者信息

Pollock D M, Shiosaki K, Sullivan G M, Opgenorth T J

机构信息

Abbott Laboratories, Abbott Park, IL 60064.

出版信息

Biochem Biophys Res Commun. 1992 Jul 31;186(2):1146-50. doi: 10.1016/0006-291x(92)90866-j.

DOI:10.1016/0006-291x(92)90866-j

PMID:1497648

Abstract

Experiments were conducted to determine the importance of the carbohydrate moiety of phosphoramidon in the inhibition of the pressor response to big endothelin-1 in anesthetized rats. Big endothelin-1 produced a 42% increase in mean arterial pressure which was nearly abolished by co-infusion of phosphoramidon. Similarly, when an analog of phosphoramidon lacking the rhamnose group (phosphoryl-leu-trp-OH) was co-infused, a significant attenuation of the pressor response was observed. These findings indicate that the rhamnose moiety of phosphoramidon is not responsible for the distinguishing this compound as an inhibitor of the response to big endothelin-1 in the rat.

摘要

进行实验以确定磷酰胺素的碳水化合物部分在抑制麻醉大鼠对大内皮素 -1 的升压反应中的重要性。大内皮素 -1 使平均动脉压升高 42%，而磷酰胺素共同输注几乎可消除该升高。同样，当共同输注缺乏鼠李糖基团的磷酰胺素类似物（磷酰 - 亮 - 色 - 羟基）时，观察到升压反应显著减弱。这些发现表明，磷酰胺素的鼠李糖部分并非该化合物成为大鼠对大内皮素 -1 反应抑制剂的关键因素。