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Biological activity of C-terminal partial sequences of substance P.

Abstract：

:Substance P (Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2) and the C-terminal partial sequences down to the tripeptide were synthesized by a solid-phase method. These peptides were assayed for vasodilator, spasmogenic, and venoconstrictor properties using three preparations, viz. the hind limb blood flow of the dog, isolated guinea pig ileum, and the isolated rabbit ear vein. The tripeptide and tetrapeptide possessed weak vasodilator properties only but no activity was detected on the other less sensitive preparations. The pentapeptide produced appreciable spasmogenic and vasoactive effects. Sequences of six or more C-terminal amino acids were able to elicity activity at comparable doses to that of the parent endecapeptide; however, the activity did not increase regularly with the chain length. In each assay preparation the octapeptide was the most potent peptide. It was twice as potent as substance P on a molar basis in the guinea pig ileum but the enhancement of activity beyond that of substance P was less pronounced in the vascular preparations.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Bury RW,Mashford ML

doi

10.1021/jm00228a028

subject

Has Abstract

pub_date

1976-06-01 00:00:00

pages

854-6

issue

6

eissn

0022-2623

issn

1520-4804

journal_volume

19

pub_type

杂志文章

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