Encequidar (HM30181A) is a potent and selective P-glycoprotein inhibitor.

HM30181 to inhibit Pgp at the murine BBB.?HM30181 was shown to be approximately equipotent with the reference Pgp inhibitor tariquidar in inhibiting rhodamine 123 efflux from CCRF-CEM T cells (IC(50), tariquidar: 8.2 2.0 nM, HM30181: 13.1 2.3 nM).?PET scans with the Pgp substrate (R)-[(11)C]verapamil in FVB wild-type mice pretreated i.v. with HM30181 (10 or 21 mg/kg) failed to show significant increases in (R)-[(11)C]verapamil brain uptake compared with vehicle treated animals.?PET scans with [(11)C]HM30181 showed low and not significantly different brain uptake of [(11)C]HM30181 in wild-type, Mdr1a/b((-/-)) and Bcrp1((-/-)) mice and significantly, i.e. 4.7-fold (P<0.01), higher brain uptake, relative to wild-type animals, in Mdr1a/b((-/-))Bcrp1((-/-)) mice[1].