Synthesis and biological activities of substance P antagonists.

Abstract:

:Several substance P analogues containing various D-amino acid modifications have been synthesized by the solid-phase procedure, detached from the solid support by ammonolysis, and purified by gel filtration combined with reversed-phase chromatography. Three compounds were fair to very potent competitive antagonists of substance P on three bioassays, i.e., guinea pig ileum, rabbit mesenteric vein, and guinea pig trachea. [Arg6,D-Trp10]SP(6-11) is a reasonable antagonist in all three bioassays and [D-Pro4,D-Trp7,9]SP(4-11) is a very potent competitive antagonist with pA2 values ranging around 6.0.

journal_name

J Med Chem

authors

Caranikas S,Mizrahi J,Escher E,Regoli D

doi

10.1021/jm00353a008

subject

Has Abstract

pub_date

1982-11-01 00:00:00

pages

1313-6

issue

11

eissn

0022-2623

issn

1520-4804

journal_volume

25

pub_type

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