Rusconi L, de Castiglione R, Gozzini L, Ciomei M, Molinari I, Basilico L, Rubino T, Vinayek R, Gardner J D
Ricerca & Sviluppo Farmitalia Carlo Erba S.r.l.-Erbamont Group, Milano, Italia.
Farmaco. 1991 Jun;46(6):725-42.
Although bombesin (BN) and substance P share only the C-terminal dipeptide amide, some substance P receptor antagonists are also weak bombesin receptor antagonists. In order to increase the selectivity of the antagonism for the BN receptor, a series of hybrid peptides were synthesized by the solid-phase methodology, and screened on 3T3 fibroblasts for binding and mitogenic activity. The analogues inhibiting BN-induced thymidine incorporation were further tested for peripheral (amylase release and urinary bladder contraction) and central activity (grooming behaviour).
尽管蛙皮素（BN）和P物质仅在C末端二肽酰胺部分相同，但一些P物质受体拮抗剂也是较弱的蛙皮素受体拮抗剂。为了提高对BN受体拮抗作用的选择性，采用固相方法合成了一系列杂合肽，并在3T3成纤维细胞上进行结合和促有丝分裂活性筛选。对抑制BN诱导的胸苷掺入的类似物进一步进行外周活性（淀粉酶释放和膀胱收缩）和中枢活性（梳理行为）测试。
