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P-glycoprotein (P-gp) inhibitors block a drug efflux pump that contributes to multidrug resistance in cells. P-gp, also called multidrug resistance protein 1 (MDR1) or ATP-binding cassette subfamily B member 1 (ABCB1), uses energy from adenosine triphosphate (ATP) hydrolysis. It was first described in 1976 as a surface glycoprotein of drug-resistant Chinese hamster ovary cells. A crystal structure later showed a large drug-binding pocket that accounts for its broad substrate range. Verapamil and its metabolite norverapamil hydrochloride are early inhibitors, and verapamil is also listed under Calcium Channels. Later inhibitors include valspodar, tariquidar, LY335979 and elacridar, which also blocks breast cancer resistance protein (BCRP).
Synonyms: (±)-Norverapamil hydrochloride; D591 hydrochloride
Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
Synonyms: CP-16533-1; ±-Verapamil
Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.
Synonyms: (±)-Norverapamil; D591
Norverapamil, an N-demethylated metabolite of Verapamil, acts as an L-type calcium channel blocker and inhibits P-glycoprotein (P-gp) function. This compound is primarily utilized in research to study calcium ion dynamics and assess the role of P-gp in drug transport and resistance mechanisms. Its ability to modulate calcium influx makes it valuable for applications in cardiovascular and neuropharmacological investigations.
Synonyms: (+)-Neostenine
Neostenine is a stenine-type Stemona alkaloid that acts as a substrate for P-glycoprotein. It exhibits notable antitussive activity and demonstrates high absorptive permeability in Caco-2 monolayer models. Additionally, Neostenine shows oral bioactivity, making it relevant for research applications involving intestinal absorption and therapeutic potential in cough-related conditions.
