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Titolo:
5-Hydroxytryptamine release from skin mast cells in vivo induced by peptide but not by nonpeptide ligands for bradykinin receptors
Autore:
Griesbacher, T; Rainer, I;
Indirizzi:
Graz Univ, Dept Expt & Clin Pharmacol, A-8010 Graz, Austria Graz Univ Graz Austria A-8010 xpt & Clin Pharmacol, A-8010 Graz, Austria
Titolo Testata:
IMMUNOPHARMACOLOGY
fascicolo: 2-3, volume: 43, anno: 1999,
pagine: 195 - 201
SICI:
0162-3109(199909)43:2-3<195:5RFSMC>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
RAT PAW EDEMA; B-2 RECEPTOR; HISTAMINE-RELEASE; ANTAGONIST; FR173657; INDUCTION; FR167344; HOE-140; ANALOGS; KININS;
Keywords:
bradykinin antagonists; FR167344; FR173657; icatibant; hoe-140; bradykinin agonists; FR190997; mast cell degranulation; 5-hydroxytryptamine release;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
26
Recensione:
Indirizzi per estratti:
Indirizzo: Griesbacher, T Graz Univ, Dept Expt & Clin Pharmacol, Univ Pl 4, A-8010 Graz, Austria Graz Univ Univ Pl 4 Graz Austria A-8010 8010 Graz, Austria
Citazione:
T. Griesbacher e I. Rainer, "5-Hydroxytryptamine release from skin mast cells in vivo induced by peptide but not by nonpeptide ligands for bradykinin receptors", IMMUNOPHARM, 43(2-3), 1999, pp. 195-201

Abstract

A number of biologically active peptides including bradykinin (BK) are known to elicit an unspecific, non-receptor-mediated release of mediators frommast cells. We have investigated whether novel, nonpeptide BK B-2 receptorligands, i.e., the antagonists N-[N-[3-[(3-bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxymethyl]-2,3-dichlorophenyl]-N-methyla-minocarbonylmethyl]-4-(dimethylaminocarbonyl)cinnamylamide hydrochloride (FR167344) and (E)-3-(6-acetamido-3-pyridyl)-N-[N-(2,4-dichloro- 3-{(2-methyl-8-quinolinyl)oxymethyl}phenyl]-N-methylaminocarbonylmethyl]acrylamide (FR173657), and the agonist 8-[2,6-dichloro-3-[ N-[( E)-4-( N-methylcarbamoyl)cinnamidoacetyl]-N-methylamino]-benzyloxy]2-methyl-4-(2-pyridylmethoxy)quinoline (FR190997), would be devoid of this unspecific action. Paw oedema in anaesthetized rats was observed following subplantar injection of BK, FR190997, the B-2 antagonist D-Arg-[Hyp(3), Thi(5), D-Tic(7), Oic(8)]-BK (icatibant, previously Hoe-140),the B-1 agonist des-Arg(9)-BK (DABK) and the B-1 antagonist des-Arg(9)-[Leu(8)]-BK (DALBK). The effect of BK was inhibited by systemic pretreatments with icatibant and methysergide in an additive manner, whereas the local effect of icatibant was only sensitive to methysergide. Oedema induced by DABK and DALBK was also attenuated by methysergide. Mepyramine pretreatment was ineffective for all oedema-producing agents. Effects of FR190997 were abolished by pretreatment with icatibant. FR167343 and FR173657 did not induceoedema formation. Depletion of mast cells by compound 48/80 mimicked the effects of methysergide on BK and icatibant and had no effect on FR190997. It is concluded that the novel nonpeptide receptor ligands are devoid of theunspecific mast cell-degranulating action observed with the peptide ligands. (C) 1999 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 11/07/20 alle ore 19:39:45