Allen M C, Brundish D E, Wade R, Sandberg B E, Hanley M R, Iversen L L
J Med Chem. 1982 Oct;25(10):1209-13. doi: 10.1021/jm00352a022.
Substance P has been prepared 3H labeled at Phe8 by catalytic deiodination of a protected precursor. Synthesis of the precursor was by solid-phase methodology on polydimethylacrylamide resin and by condensation in solution of fragments covering sequences 1-4, 5-7, and 8-11. Free peptide made by each route analyzed satisfactorily and had the same chromatographic characteristics as unlabeled substance P. It was indistinguishable from the latter by radioimmunoassay when N and C terminally directed antisera were used and in the ability to cause contractions of isolated guinea pig ileum. Specific radioactivity was 23 Ci/mmol.
通过对受保护前体进行催化脱碘反应，制备了苯丙氨酸8位被3H标记的P物质。前体的合成采用聚二甲基丙烯酰胺树脂上的固相方法，以及通过溶液中覆盖序列1 - 4、5 - 7和8 - 11的片段缩合反应。通过每种途径制备的游离肽经分析令人满意，并且具有与未标记P物质相同的色谱特征。当使用N端和C端定向抗血清时，通过放射免疫测定法，它与后者没有区别，并且在引起豚鼠离体回肠收缩的能力方面也没有区别。比放射性为23 Ci/mmol。
