Evaluation of substrate and inhibitor properties of a novel MDR modulator H17 towards transmembrane efflux pumps.

摘要

Substrate and inhibitor properties of H17 as novel modulator of transmembrane efflux pump activities have been characterized in an in situ absorption model. Poor substrate properties towards P-glycoprotein (P-gp) and multidrug resistance-associated protein (MRP) have been demonstrated. In competition with a MRP substrate H17 proved to have strong MRP-inhibiting properties. The profile of a strong inhibitor with poor substrate properties makes H17 a perspective hopeful candidate for effective therapies of transmembrane efflux pump activities.