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在第17、18或19位被取代的人β-内啡肽类似物的合成与镇痛活性

Synthesis and analgesic activity of human beta-endorphin analogs substituted at positions 17, 18, or 19.

作者信息

Blake J, Tseng L F, Li C H

出版信息

Int J Pept Protein Res. 1980 Feb;15(2):167-70. doi: 10.1111/j.1399-3011.1980.tb02564.x.

Abstract

Three peptide analogs of beta-endorphin which are substituted in positions 17, 18 or 19 have been synthesized and their analgesic potencies have been measured by the tail-flick method in mice. The results showed that the replacement of Phe-18 or Lys-19 by alanine reduced the potency to 15% whereas the replacement of Leu-17 by alanine reduced the analgesic potency to 68%.

摘要

已经合成了β-内啡肽在第17、18或19位被取代的三种肽类似物,并通过小鼠甩尾法测量了它们的镇痛效力。结果表明,用丙氨酸取代苯丙氨酸-18或赖氨酸-19会使效力降低至15%,而用丙氨酸取代亮氨酸-17会使镇痛效力降低至68%。

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