Structure-activity studies of heptapeptide derivatives related to substance P, neurokinin A, B and other tachykinins on smooth muscles |
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Authors: | E Munekata K Kubo H Tanaka F Osakada |
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Institution: | 1. Department of Pharmacy, “G. D''Annunzio” University of Chieti-Pescara, Via dei Vestini 31, 66100 Chieti Scalo (CH), Italy;2. Department of Chemistry, “Sapienza” Università di Roma, P. le A. Moro, 5, 00187 Rome, Italy;3. Laboratoire de Cancérologie et de Toxicologie Expérimentale, Faculté de Pharmacie, Université Libre de Bruxelles, 1050 Brussels, Belgium |
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Abstract: | Diverse C-terminal heptapeptide derivatives related to substance P, kassinin, physalaemin, neurokinin A and B were synthesized and the contracting activities on the guinea pig ileum as well as rat duodenum were compared. In the partial sequence of C-terminal of tachykinin peptides, -I-II-Phe-III-Gly-Leu-Met-NH2, the combination of amino acid residues at positions I and III have significant roles in contraction of smooth muscle. For the activation of rat duodenal muscle (SP-E), Asp(I) and aliphatic amino acid(III), and for guinea pig ileal muscle(SP-P), Gln(I) and aromatic amino acid(III) are essential. Moreover, guinea pig ileum is sensitive to a full sequence of neurokinin peptides. |
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