Bombesin receptor antagonists. 2. Analogues based on substance P antagonists

Autor: Rusconi, L., Castiglione, R., Gozzini, L., Ciomei, M., Molinari, I., Basilico, L., Tiziana RUBINO, Vinayek, R., Gardner, J. D.
Rok vydání: 1991
Předmět:
Zdroj: Scopus-Elsevier
ISSN: 0014-827X
Popis: 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).
Databáze: OpenAIRE