P物质的构象受限环状类似物：对受体结合过程的深入了解。

Conformationally restricted cyclic analogues of substance P: insight into the receptor binding process.

作者信息

Darman P S, Landis G C, Smits J R, Hirning L D, Gulya K, Yamamura H I, Burks T F, Hruby V J

出版信息

Biochem Biophys Res Commun. 1985 Mar 15;127(2):656-62. doi: 10.1016/s0006-291x(85)80211-4.

Abstract

Three new cyclic substance P analogues were prepared to examine the possible role of a pseudocyclic turn structure for receptor recognition. In the guinea pig isolated ileum [Cys5, Cys11]-SP5-11-NH2 and [Cys6, Cys11]-SP5-11-NH2 were inactive at concentrations up to 100 microM, while [Cys5, Cys6, Nle11]-SP was a weak agonist. The order of relative affinities on the rat brain radioreceptor assay was as follows: [Cys5, Cys6, Nle11]-SP greater than [Cys5, Cys11]-SP5-11-NH2 greater than [Cys6, Cys11]-SP5-11-NH2. We interpret these results to indicate that a pseudocyclic structure of the 5-11 sequence may not be an important factor involved in the receptor recognition of substance P.

摘要

制备了三种新的环P物质类似物，以研究假环转折结构在受体识别中可能发挥的作用。在豚鼠离体回肠中，[Cys5，Cys11]-SP5-11-NH2和[Cys6，Cys11]-SP5-11-NH2在浓度高达100 microM时无活性，而[Cys5，Cys6，Nle11]-SP是一种弱激动剂。大鼠脑放射受体测定中相对亲和力的顺序如下：[Cys5，Cys6，Nle11]-SP大于[Cys5，Cys11]-SP5-11-NH2大于[Cys6，Cys11]-SP5-11-NH2。我们将这些结果解释为表明5-11序列的假环结构可能不是参与P物质受体识别的重要因素。