Histamine liberation as a result of nonreceptor interaction

The highly lipophilic drug exaprolol liberates histamine from isolated mast cells and decreases the uptake of extracellular histamine in a dose-dependent manner. Intracellular histamine depletion was confirmed by electron microscopy and was accompanied by calcium displacement from intracellular stor...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Agents and Actions 1990-04, Vol.30 (1-2), p.74-76
Hauptverfasser: Nosál, R, Drábiková, K, Pecivová, J, Jakubovský, J
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The highly lipophilic drug exaprolol liberates histamine from isolated mast cells and decreases the uptake of extracellular histamine in a dose-dependent manner. Intracellular histamine depletion was confirmed by electron microscopy and was accompanied by calcium displacement from intracellular storage sites. The significant decrease in membrane fluidity due to exaprolol was temperature-dependent and was most probably a result of its high membrane affinity and intracellular penetration. Membrane perturbation by exaprolol may account for this nonreceptor interaction. This could contribute to the understanding of adverse reactions to beta-adrenoceptor blocking drugs.
ISSN:0065-4299
1420-908X
DOI:10.1007/BF01969002