The substance P receptor on rat mast cells and in human skin.
(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 microM, 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 microM 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.
D000328:Adult; D000818:Animals; D004305:Dose-Response Relationship, Drug; D006636:Histamine Release / Q000187:drug effects; D006801:Humans; D015286:Kassinin; D008297:Male; D008407:Mast Cells / Q000032:analysis*; D008875:Middle Aged; D009842:Oligopeptides / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011956:Receptors, Cell Surface / Q000032:analysis*; D018040:Receptors, Neurokinin-1; D012867:Skin / Q000032:analysis*; D013373:Substance P / Q000037:antagonists & inhibitors
D009842:Oligopeptides; D011956:Receptors, Cell Surface; D018040:Receptors, Neurokinin-1; D013373:Substance P; D015286:Kassinin