Peptides and histamine release from rat peritoneal mast cells.
Various vasoactive peptides were compared for their histamine releasing effects on rat mast cells. Neurotensin, substance P (SP), and kallidin were the most active natural peptides, followed by bradykinin; neurokinin A and B, bombesin, angiotensin and tuftsin were practically inactive. Several kinins and tachykinin-related peptides were tested in an attempt to characterize the receptors mediating histamine liberation. The order of potency of the kinins was the following: kallidin greater than [Tyr(Me)8]bradykinin = bradykinin greater than [desArg10]kallidin greater than desArg9-bradykinin, the same as that found in smooth muscle possessing receptors of the B2 type. Tachykinin-related peptides were potent stimulants and followed the order: [D-Tryp7,9,10]SP-(1-11) greater than [D-Pro2,D-Tryp7,9,10]SP-(1-11) greater than SP-(1-11) greater than SP-(1-9) greater than [D-Pro4,D-Tryp7,9,Leu11]SP-(4-11) greater than SP-(1-7) greater than SP-(4-11) greater than neurokinin A = neurokinin B, indicating that: (a) undecapeptide antagonists of SP behave as superagonists; (b) both N- and C-terminal portions of SP-(1-11) are essential for activity; and (c) receptors for the tachykinins mediating histamine release appear to be of the SP-P type.
Devillier
P
P
Renoux
M
M
Giroud
J P
JP
Regoli
D
D
D000818:Animals; D001920:Bradykinin / Q000494:pharmacology; D006636:Histamine Release / Q000187:drug effects*; D066298:In Vitro Techniques; D007609:Kallidin / Q000494:pharmacology; D007705:Kinins / Q000494:pharmacology; D008407:Mast Cells / Q000378:metabolism*; D009419:Nerve Tissue Proteins / Q000494:pharmacology; D010455:Peptides / Q000494:pharmacology*; D010529:Peritoneal Cavity / Q000166:cytology; D051381:Rats; D011919:Rats, Inbred Strains; D013373:Substance P / Q000494:pharmacology; D015320:Tachykinins
D007705:Kinins; D009419:Nerve Tissue Proteins; D010455:Peptides; D015320:Tachykinins; D013373:Substance P; D007609:Kallidin; D001920:Bradykinin