Structure-activity relationship of C-terminal hexa- and heptapeptide substance P antagonists as studied in the guinea-pig ileum

Add time:07/31/2019    Source:sciencedirect.com

The 14 C-terminal heptapeptide analogues and one hexapeptide analogue of substance P (SP) were synthesized on the basis of the SP antagonist [D-Pro2, D-Trp7,9]SP-(1−11). They were tested in the guinea-pit ileum preparation for spasmogenic and antagonistic activities. All analogues except two had antagonistic activity. Spasmogenic activity was observed in three heptapeptide SP antagonists:[Arg5,D-Trp7,D-pCl-Phe9]SP-(5−11), [Arg5, D-Trp7,9,p-Cl-Phe8]SP-(5−11) and [Arg5,D-Trp7,9,Nle11]SP-(5–11). However, this effect became greatly reduced upon successive applications in almost all ileum preparations. For antagonistic potency D-Trp turned out to be greater importance in position 9 than in position 7 of the SP molecule. The presence of a free amino group at the N-terminal of the peptide was also of significant importance for antagonistic potency. Exchange of Met11 for Nle resulted in a considerable increase of antagonistic potency, while other substitutions in this position were ineffective or slightly reduced the antagonistic effect in the ileum preparation.

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