• Medientyp: E-Artikel
  • Titel: Characterization of the inhibitory prostanoid receptors on human neutrophils
  • Beteiligte: Wheeldon, Alan; Vardey, Christopher J.
  • Erschienen: Wiley, 1993
  • Erschienen in: British Journal of Pharmacology
  • Sprache: Englisch
  • DOI: 10.1111/j.1476-5381.1993.tb13504.x
  • ISSN: 0007-1188; 1476-5381
  • Schlagwörter: Pharmacology
  • Entstehung:
  • Anmerkungen:
  • Beschreibung: <jats:p><jats:list list-type="explicit-label"> <jats:list-item><jats:p>We have evaluated the effects of various prostanoid agonists on the release of leukotriene B<jats:sub>4</jats:sub> (LTB<jats:sub>4</jats:sub>) and superoxide anions (O<jats:sub>2</jats:sub><jats:sup>−</jats:sup>) from human neutrophils stimulated with opsonized zymosan (OZ) and formyl‐methionyl‐leucyl‐phenylalanine (FMLP), respectively.</jats:p></jats:list-item> <jats:list-item><jats:p>Prostaglandin E<jats:sub>2</jats:sub> (PGE<jats:sub>2</jats:sub>) and PGD<jats:sub>2</jats:sub> inhibited both OZ‐induced LTB<jats:sub>4</jats:sub> release (EC<jats:sub>50</jats:sub> 0.72 μ<jats:sc>m</jats:sc> and 0.91 μ<jats:sc>m</jats:sc> respectively), and FMLP‐induced O<jats:sub>2</jats:sub><jats:sup>−</jats:sup> release (EC<jats:sub>50</jats:sub> 0.42 μ<jats:sc>m</jats:sc> and 0.50 μ<jats:sc>m</jats:sc> respectively). PGF<jats:sub>2α</jats:sub>, the TP‐receptor agonist, U46619, and the IP‐receptor agonist, iloprost, were also active, but were all at least an order of magnitude less potent than PGE<jats:sub>2</jats:sub> and PGD<jats:sub>2</jats:sub>.</jats:p></jats:list-item> <jats:list-item><jats:p>The EP<jats:sub>2</jats:sub>/EP<jats:sub>3</jats:sub>‐receptor agonist, misoprostol, and the selective EP<jats:sub>2</jats:sub>‐agonist, AH13205, were both effective inhibitors of LTB<jats:sub>4</jats:sub> release, being approximately equipotent with and 16‐times less potent than PGE<jats:sub>2</jats:sub>, respectively. In contrast, the EP<jats:sub>1</jats:sub>/EP<jats:sub>3</jats:sub>‐receptor agonist, sulprostone, had no inhibitory activity at concentrations of up to 10 μ<jats:sc>m</jats:sc>.</jats:p></jats:list-item> <jats:list-item><jats:p>The selective DP‐receptor agonist, BW245C, inhibited LTB<jats:sub>4</jats:sub> release, (EC<jats:sub>50</jats:sub> 0.006 μ<jats:sc>m</jats:sc>) being approximately 50 times more potent than PGD<jats:sub>2</jats:sub>. BW245C also inhibited O<jats:sub>2</jats:sub><jats:sup>−</jats:sup> release, and this inhibition was antagonized competitively by the DP‐receptor blocking drug, AH6809 (pA<jats:sub>2</jats:sub> 6.6).</jats:p></jats:list-item> <jats:list-item><jats:p>These data indicate the presence of both inhibitory EP‐ and DP‐receptors on the human neutrophil. The rank order of potency of EP‐receptor agonists suggest that the EP‐receptors are of the EP<jats:sub>2</jats:sub>‐subtype.;</jats:p></jats:list-item> </jats:list></jats:p>
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