含有Nα-甲基氨基酸的缓激肽类似物。
Bradykinin analogues containing N alpha-methyl amino acids.
作者信息
Mazur R H, James P A, Tyner D A, Hallinan E A, Sanner J H, Schulze R
出版信息
J Med Chem. 1980 Jul;23(7):758-63. doi: 10.1021/jm00181a012.
PMID:7401103
Abstract
Analogues of bradykinin were synthesized containing single substitutions by N alpha-methyl amino acids in the 1, 4, 5, 5, and 9 positions. [MeArg]Bradykinin possessed 60% of the muscle-contracting activity of the parent compound in a guinea pig ileum assay. The other analogues were very weak agonists (less than 2%) and, disappointingly, failed to show blocking activity except at very high doses.
摘要
合成了缓激肽类似物，这些类似物在第1、4、5、5和9位含有由Nα-甲基氨基酸构成的单取代。在豚鼠回肠试验中，[甲基精氨酸]缓激肽具有母体化合物60%的肌肉收缩活性。其他类似物是非常弱的激动剂（小于2%），令人失望的是，除了在非常高的剂量下，它们没有表现出阻断活性。
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