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非洲蛙(Kassina senegalensis)皮肤中速激肽十二肽——physalaemin和kassinin的平行生物测定。

Parallel bioassay of physalaemin and kassinin, a tachykinin dodecapeptide from the skin of the African frog Kassina senegalensis.

作者信息

Erspamer G F, Erspamer V, Piccinelli D

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1980 Feb;311(1):61-5. doi: 10.1007/BF00500303.

Abstract
  1. Kassinin, a tachykinin dodecapeptide isolated from the skin of the African frog Kassina senegalensis was submitted to parallel bioassay with physalaemin, eledoisin and substance P, three major representatives of the tachykinin peptide family. Bioassay was carried out on blood pressure, salivary secretion and isolated or in situ smooth muscle preparations. 2. As expected, kassinin possessed the entire spectrum of biological activity peculiar to the tachykinins. However, among the examined tachykinins kassinin was the poorest stimulant of salivary secretion and the weakest hypotensive agent, while displaying very powerful stimulant effects on different smooth muscle preparations, especially on isolated preparations of urinary bladder. 3. Kassinin differed from the other tachykinins also for its more gradual and sustained action on several in situ and isolated preparations. The peptide most similar to kassinin in its spectrum of activity was eledoisin. 4. Emphasis is laid on the possibility to dissociate the effects of the tachykinins on different target systems through changes in the N-moiety of the tachykinin molecule.
摘要
  1. 蛙皮素是从非洲蛙类塞内加尔蛙的皮肤中分离出的一种速激肽十二肽,它与速激肽肽家族的三个主要代表物——雨蛙肽、蛙皮缩胆囊素和P物质进行了平行生物测定。生物测定针对血压、唾液分泌以及离体或原位平滑肌制剂展开。2. 正如预期的那样,蛙皮素具备速激肽特有的全部生物活性谱。然而,在所检测的速激肽中,蛙皮素是唾液分泌的最不活跃刺激剂和最弱的降压剂,同时对不同的平滑肌制剂,尤其是膀胱离体制剂,显示出非常强大的刺激作用。3. 蛙皮素在对几种原位和离体制剂的作用上也与其他速激肽不同,其作用更为渐进和持久。在活性谱上与蛙皮素最相似的肽是蛙皮缩胆囊素。4. 重点在于通过改变速激肽分子的N端部分来区分速激肽对不同靶系统的作用的可能性。

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