Abstract
(D-Pro4 D-Trp7,9,10)SP4–11 (SPA) has been shown to be a competitive antagonist of the histamine releasing action of substance P in rat peritoneal mast cells. Antagonist activity of SPA is expressed in the concentration range 1 to 10 μM, but at higher concentrations SPA releases histamine.
SPA inhibits the flare response induced by substance P in human skin but is without effect on the wheal response. Up to 12.5 pmol SPA produces neither wheal nor flare response by itself.
The structurally related peptide, kassinin, does not cause histamine release from rat mast cells at concentrations up to 10 μM whereas the methyl ester of substance P was found to 1.6 times more active than substance P in this respect.
The findings are discussed in terms of the classification of substance P receptors and the mechanism of wheal and flare in human skin.
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Piotrowski, W., Devoy, M.A.B., Jordan, C.C. et al. The substance P receptor on rat mast cells and in human skin. Agents and Actions 14, 420–424 (1984). https://doi.org/10.1007/BF01973842
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DOI: https://doi.org/10.1007/BF01973842