Altered drug disposition of the platelet activating factor antagonist apafant in mdr1a knockout mice

The aim of the present study was to determine a potential impact of P-glycoprotein (P-gp) on the tissue distribution and disposition of apafant (WEB 2086, CAS 105219-56-5), a selective platelet-activating factor antagonist, and on digoxin in mdr1a(−/−) and wildtype mice. Transport experiments in Cac...

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Veröffentlicht in:	European journal of pharmaceutical sciences 2002-08, Vol.16 (3), p.119-128
Hauptverfasser:	Leusch, Andreas, Volz, Astrid, Müller, Gabriele, Wagner, Andrea, Sauer, Achim, Greischel, Andreas, Roth, Willy
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Apafant Area Under Curve ATP Binding Cassette Transporter, Sub-Family B - deficiency ATP Binding Cassette Transporter, Sub-Family B - genetics ATP-Binding Cassette Transporters - genetics Azepines - blood Azepines - chemistry Azepines - pharmacokinetics Bile Ducts - secretion Caco-2 Cells - metabolism Carbon Radioisotopes - pharmacokinetics Digoxin Disposition Humans Intestinal Mucosa - secretion Knock-out mice Male mdr1a Mice Mice, Knockout Platelet Activating Factor - antagonists & inhibitors Platelet Activating Factor - metabolism Tissue Distribution - physiology Triazoles - blood Triazoles - chemistry Triazoles - pharmacokinetics
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Zusammenfassung:	The aim of the present study was to determine a potential impact of P-glycoprotein (P-gp) on the tissue distribution and disposition of apafant (WEB 2086, CAS 105219-56-5), a selective platelet-activating factor antagonist, and on digoxin in mdr1a(−/−) and wildtype mice. Transport experiments in Caco-2 monolayers at low concentrations (
ISSN:	0928-0987 1879-0720
DOI:	10.1016/S0928-0987(02)00088-X