Title : P-glycoprotein and an unstirred water layer barring digoxin absorption in the vascularly perfused rat small intestine preparation: induction studies with pregnenolone-16alpha-carbonitrile.

Pub. Date : 2006 Sep

PMID : 16751264






3 Functional Relationships(s)
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1 Digoxin, a substrate of P-glycoprotein (Pgp) and cytochrome P450 3a (Cyp3a), was used to illustrate the inductive effects of pregnenolone-16alpha-carbonitrile (PCN), a ligand of the pregnane X receptor, on the absorption and disposition of [3H]digoxin in the vascularly perfused rat small intestine preparation. Pregnenolone Carbonitrile ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus
2 PCN pretreatment significantly decreased blood perfusate [3H]digoxin concentrations for both systemic and intraluminal administrations of [3H]digoxin due to increased Pgp levels. Pregnenolone Carbonitrile ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus
3 The apical secretion by Pgp increased at 90 min with PCN treatment, from 11.2 +/- 5.1% of dose to 20.1 +/- 8.6% of dose after systemic administration of [3H]digoxin; this increase was, however, statistically insignificant (P = 0.13) because of the high variability among preparations. Pregnenolone Carbonitrile ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus