Watson S P, Sandberg B E, Hanley M R, Iversen L L
Eur J Pharmacol. 1983 Jan 28;87(1):77-84. doi: 10.1016/0014-2999(83)90052-3.
Previous studies from this laboratory suggested that two subtypes of substance P receptor may exist, based on the observations that substance P and related peptides did not exhibit complete cross-desensitisation on guinea-pig ileum, and that two distinct rank orders of potency of tachykinins were observed in various test systems. The present study has added support to this hypothesis by extending the screening of tachykinins to further bioassays and by testing novel analogues. In particular, C-terminal alkyl esters of substance P were found to exhibit a high degree of selectivity to one putative receptor subtype. The synthesis of the alkyl esters by esterification of substance P free acid is described.
该实验室之前的研究表明，基于P物质和相关肽对豚鼠回肠未表现出完全交叉脱敏，以及在各种测试系统中观察到速激肽的两种不同效价顺序，可能存在两种P物质受体亚型。本研究通过将速激肽的筛选扩展到更多生物测定以及测试新型类似物，为该假说提供了进一步支持。特别是，发现P物质的C末端烷基酯对一种假定的受体亚型表现出高度选择性。本文描述了通过P物质游离酸的酯化反应合成烷基酯的方法。
