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).

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

RUBINO, TIZIANA;
1991

Abstract

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).
Rusconi, L; de Castiglione, R; Gozzini, L; Ciomei, M; Molinari, I; Basilico, L; Rubino, Tiziana; Vinayek, R; Gardner, Jd
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11383/1806517
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