Effects of some neurokinin A analogues on tachykinin-induced contraction of guinea pig trachea.
Division of Biochemistry, School of Biology and Biochemistry, Queen's University of Belfast, N. Ireland, UK.
- Published Article
- Publication Date
Jan 01, 1991
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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The corresponding record at NLM can be accessed at https://www.ncbi.nlm.nih.gov/pubmed/1666182