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Titolo:
Mechanism of action of the nonlipophilic antiallergic drug eclazolast (REV2871) in the inhibition of mediator release in a mast cell model
Autore:
Fischer, MJE; de Mol, NJ;
Indirizzi:
Univ Utrecht, Fac Pharm, Dept Med Chem, Utrecht Inst Pharmaceut Sci, NL-3508 TB Utrecht, Netherlands Univ Utrecht Utrecht Netherlands NL-3508 TB 3508 TB Utrecht, Netherlands
Titolo Testata:
INFLAMMATION RESEARCH
fascicolo: 11, volume: 48, anno: 1999,
pagine: 569 - 574
SICI:
1023-3830(199911)48:11<569:MOAOTN>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
ACTIVATED SIGNAL-TRANSDUCTION; BASOPHILIC LEUKEMIA-CELLS; IMMUNOGLOBULIN-E RECEPTOR; AFFINITY IGE RECEPTOR; RBL-2H3 CELLS; TYROSINE PHOSPHORYLATION; REV-2871 CHBZ; DERIVATIVES; ASTEMIZOLE; OXATOMIDE;
Keywords:
RBL-2H3; exocytosis; eclazolast; calcium; antiallergic;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Fischer, MJE Univ Utrecht, Fac Pharm, Dept Med Chem, Utrecht Inst Pharmaceut Sci, POB 80082, NL-3508 TB Utrecht, Netherlands Univ Utrecht POB 80082 Utrecht Netherlands NL-3508 TB rlands
Citazione:
M.J.E. Fischer e N.J. de Mol, "Mechanism of action of the nonlipophilic antiallergic drug eclazolast (REV2871) in the inhibition of mediator release in a mast cell model", INFLAMM RES, 48(11), 1999, pp. 569-574

Abstract

Objective and Design. In this study, we compared eclazolast with other lipophilic antiallergic drugs, relating to effects on signal transduction pathways, leading to inhibition of exocytosis in a rat basophilic leukemia cell(RBL-2H3). Materials and Methods: Effects of the drugs on mediator release (beta-hexosaminidase, arachidonic acid metabolites) after Fc epsilon RI activation inRBL-2H3 cell were quantified. Furthermore, effects of the drugs on cellular signalling (Ca2+ influx, intracellular Ca2+ concentration, inositol 1,4,5-trisphosphate (IP3) concentration) were assayed. Effects of the drugs on bilayer and cell membranes have been recorded. Results: It is shown that eclazolast down-regulates IP3 levels. In contrast to lipophilic drugs, eclazolast does not affect artificial bilayers and erythrocyte membranes, and there is no effect on thapsigargin induced Ca2+ influx. The effect of eclazolast was highly dependent on the antigen concentration with which the cells were triggered. Conclusions: The mechanism of action of eclazolast is deviant from lipophilic antiallergic agents. It inhibits exocytosis by intracellularly affecting only direct Fc epsilon RI linked processes and not through inhibition of Ca2+ influx channels, as found for membrane disturbing lipophilic drugs.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/09/18 alle ore 08:46:10