Conformationally restricted cyclic analogues of substance P: Insight into the receptor binding process
作者： Paul S. Darman , Geoffrey C. Landis , John R. Smits , Lane D. Hirning , Karoly Gulya
DOI: 10.1016/S0006-291X(85)80211-4
关键词:
摘要: Three new cyclic substance P analogues were prepared to examine the possible role of a pseudocyclic turn structure for receptor recognition. In guinea pig isolated ileum [Cys5, Cys11]-SP5-11-NH2 and [Cys6, inactive at concentrations up 100 microM, while Cys6, Nle11]-SP was weak agonist. The order relative affinities on rat brain radioreceptor assay as follows: greater than Cys11]-SP5-11-NH2. We interpret these results indicate that 5-11 sequence may not be an important factor involved in recognition P.
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