Interaction of neurotensin with the substance P receptor mediating histamine release from rat mast cells and the flare in human skin.
1 Substance P induced histamine release from rat peritoneal mast cells in a dose-dependent manner over the concentration range 1 to 10 microM. 2 At concentrations in the range 2.5 to 1 0 microM, neurotensin produced only about 5% release of histamine, which was substantially less than the maximum effect obtained with substance P. 3 Neurotensin, 2.5 to 10 microM produced graded inhibition of histamine release induced by substance P. The inhibitory effect of neurotensin was not seen when histamine release was induced by an antigen-antibody effect of neurotensin was not seen when histamine release was induced by an antigen-antibody reaction or by the ionophore, A 23187. Some evidence was obtained to suggest that compound 48/80 may interact with the same receptor as substance P and neurotensin. 4 [D-Arg8]neurotensin, [D-Arg9]neurotensin, xenopsin and the C-terminal octapeptide of substance P (SP4-11) all inhibited histamine release by substance P, but physalaemin did not. 5 Neurotensin inhibited the wheal and flare reactions induced by substance P in human skin. 6 [D-Trp7,9]substance P released histamine from rat mast cells and was about 12 times more potent than substance P itself. [D-Trp7,9]SP1-11 also produced wheal and flare responses in human skin, being 1.8 times more potent than substance P in the production of flare.
D000328:Adult; D000818:Animals; D002199:Capillary Permeability / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D005260:Female; D006636:Histamine Release / Q000187:drug effects*; D006801:Humans; D008297:Male; D008407:Mast Cells / Q000378:metabolism*; D009496:Neurotensin / Q000494:pharmacology*; D010455:Peptides / Q000494:pharmacology; D051381:Rats; D011956:Receptors, Cell Surface / Q000187:drug effects*; D018040:Receptors, Neurokinin-1; D012867:Skin / Q000098:blood supply / Q000187:drug effects*; D013373:Substance P / Q000494:pharmacology
D010455:Peptides; D011956:Receptors, Cell Surface; D018040:Receptors, Neurokinin-1; D013373:Substance P; D009496:Neurotensin