Stimulation of histamine release by the peptide kinetensin.
The peptide kinetensin isolated from pepsin-treated human plasma induced a dose-dependent release of histamine when exposed to rat peritoneal mast cells. The threshold concentration was around 10(-6) M, the ED50 was 10(-5) M, and the optimal concentration of between 10(-4) to 10(-3) M released 80% of the total histamine. Kinetensin was 10 to 100 times less potent than neurotensin and equipotent with the opioid peptide dynorphin. The histamine release was clearly temperature-dependent, with no release occurring at 0 degrees or 45 degrees C and with an optimum around 37 degrees C. The histamine release was significantly reduced in the absence of extracellular calcium. Kinetensin also induced a dose-dependent increase in vascular permeability when injected intradermally into rats. The findings indicate that kinetensin is a potent histamine releaser in the rat and may serve as an inflammatory mediator.
Sydbom
A
A
Department of Pharmacology, Karolinska Institute, Stockholm, Sweden.
Ware
J
J
Mogard
M H
MH
D000818:Animals; D002199:Capillary Permeability / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006636:Histamine Release / Q000187:drug effects*; D066298:In Vitro Techniques; D008407:Mast Cells / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D009496:Neurotensin / Q000494:pharmacology; D009842:Oligopeptides / Q000008:administration & dosage / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains
D009842:Oligopeptides; C048812:kinetensin; D009496:Neurotensin