多巴胺肽类衍生物的合成及其对心功能的影响

SYNTHESIS AND CARDIOVASCULAR ACTIVITIES OF PEPTIDYL DOPAMINE DERIVATIVES

将氨基酸或小肽引入多巴胺分子中,共合成了十八个具有不同立体构型和亲脂性的氨基酸多巴胺肽。在麻醉狗上药理初筛表明,多巴胺分子中引入L型氨基酸非常显著地增加心肌收缩力和动脉压,而引入D型氨基酸或N-甲基氨基酸后,则生理活性显著减弱。当多巴胺分子中引入亲脂性的氨基酸后,能明显增加心肌收缩力和血压,同时能明显延长作用时间。

Amino acids and small peptides with different steric configurat ions and lipophilicities were aprended to dopamine. Eighteen compounds have been synthesized. The attachment of D-amino acids or N-methyl amino acids onto the dopamine molecule caused a marked decrease in cardiovascular activity by intravenous injection, while the introduction of lipophilic amino acids caused a marked increase in myocardial contractility and blood pressure in anesthetized dogs. The durations of action were also prolonged.