Effect of gliquidone on the ABCB1 protein functional activity in vivo

Autor: D S Titov, A A Nikiforov, S. K Pravkin
Rok vydání: 2015
Předmět:
Zdroj: I.P. Pavlov Russian Medical Biological Herald. 23:39-43
ISSN: 2500-2546
0204-3475
DOI: 10.17816/pavlovj2015439-43
Popis: In the in vivo study in rabbits the effect of gliquidone at 10 mg / kg body weight of the functional activity of the protein transporter P-glycoprotein (P-gp, ABCB1 protein) was studied. P-gp activity was evaluated by pharmacokinetics of its marker substrate - fexofenadine after a single intragastric administration. Applying gliquidone for 14 days led to an increase in the maximum concentration of fexofenadine, its halflife, area under the concentration-time curve from zero to the last point of drawing blood, area under the concentration-time curve from zero to infinity, and the retention time of marker substrate and reduce the overall clearance and rate of absorption, indicating that the inhibition of the functional activity of the protein transporter at the level of the whole organism.
Databáze: OpenAIRE