Leban J, Rackur G, Yamaguchi I, Folkers K, Björkroth U, Rosell S, Yanaihara N, Yanaihara C
Acta Chem Scand B. 1979;33(9):664-8. doi: 10.3891/acta.chem.scand.33b-0664.
Fourteen analogs of substances P (SP), six previously synthesized by a solution method and eight newly synthesized by a solid-phase technique, have been tested for agonistic and antagonistic activities utilizing the isolated guinea pig ileum. The primary objective is to achieve effective inhibitors of SP. These analogs had agonistic activities ranging from negligible to that equivalent to SP. Six of the fourteen analogs had some degree of antagonistic activity [D-Leu8, D-Phe9]-SP is an analog which constitutes a lead to new substitutions, because it had antagonistic activity, but only negligible agonistic activity. One concept for effective antagonistic activity requires negligible or no agonistic activity.
已经利用离体豚鼠回肠对14种P物质（SP）类似物进行了激动和拮抗活性测试，其中6种是先前通过溶液法合成的，8种是新通过固相技术合成的。主要目标是获得有效的SP抑制剂。这些类似物的激动活性范围从可忽略不计到与SP相当。14种类似物中有6种具有一定程度的拮抗活性，[D-亮氨酸8，D-苯丙氨酸9]-SP是一种类似物，它是新取代物的先导，因为它具有拮抗活性，但激动活性可忽略不计。有效拮抗活性的一个概念要求激动活性可忽略不计或没有激动活性。
