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Effects of some neurokinin A analogues on tachykinin-induced contraction of guinea pig trachea.

Authors
  • Abu Shanab, A A1
  • Allen, J M
  • Guthrie, D J
  • Irvine, G B
  • Murphy, R F
  • Walker, B
  • 1 Division of Biochemistry, School of Biology and Biochemistry, Queen's University of Belfast, N. Ireland, UK. , (Ireland)
Type
Published Article
Journal
Peptides
Publisher
Elsevier
Publication Date
Jan 01, 1991
Volume
12
Issue
5
Pages
1069–1075
Identifiers
PMID: 1666182
Source
Medline
License
Unknown

Abstract

A series of analogues of neurokinin A (NKA) has been synthesized and characterized by testing for their abilities, in vitro, to contract guinea pig tracheal smooth muscle or to antagonize NKA-, NKB- and SP-induced contraction of this tissue. Substitution of NKA residues Gly8 or Leu9 by conformationally restricting amino acids produced peptides that were antagonists of NKA action, but the type and specificity of the antagonism depended on the size of the peptide. Thus, while [Ala5, Aib8, Leu10]NKA(2-10) showed no agonism and was a specific, competitive antagonist of NKA, [Ala5, Aib8, Leu10]NKA(4-10) was a noncompetitive antagonist of NKA and substance P (SP) and was itself a weak agonist at concentrations above 10(-7) M.

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