高达敏, 陈国梁, 杨福秋, 程炜钰, 陈解春, 闵旸, 商宏锚, 张顺安. 多巴胺肽类衍生物的合成及其对心功能的影响J. 药学学报, 1989, 24(6): 422-430.
引用本文: 高达敏, 陈国梁, 杨福秋, 程炜钰, 陈解春, 闵旸, 商宏锚, 张顺安. 多巴胺肽类衍生物的合成及其对心功能的影响J. 药学学报, 1989, 24(6): 422-430.
DM Gao, FQ Yang, CL Chen, WY Cheng, JC Chen, Y Min, HM Shang , SA Zhang, . SYNTHESIS AND CARDIOVASCULAR ACTIVITIES OF PEPTIDYL DOPAMINE DERIVATIVESJ. Acta Pharmaceutica Sinica, 1989, 24(6): 422-430.
Citation: DM Gao, FQ Yang, CL Chen, WY Cheng, JC Chen, Y Min, HM Shang , SA Zhang, . SYNTHESIS AND CARDIOVASCULAR ACTIVITIES OF PEPTIDYL DOPAMINE DERIVATIVESJ. Acta Pharmaceutica Sinica, 1989, 24(6): 422-430.

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

  • 摘要: 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。

     

    Abstract: 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.

     

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