OCT2 Inhibitors

OCT2 inhibitors encompass a diverse set of compounds that act either directly or indirectly to modulate OCT2 activity by targeting specific pathways or cellular processes crucial for its regulation. Cimetidine, a H2 receptor antagonist, directly inhibits OCT2 by competing for substrate binding sites, thereby reducing the transport of cationic substrates by OCT2. Probenecid, a URAT1 inhibitor, indirectly influences OCT2 by reducing renal excretion, elevating systemic levels of substrates recognized by OCT2. Trimethoprim, an antibiotic, directly interferes with OCT2 transport activity, particularly impacting organic cation substrates. Dolutegravir, an integrase inhibitor, indirectly affects OCT2 by influencing the P-glycoprotein (P-gp) efflux pump, altering the disposition of drugs recognized by both P-gp and OCT2. Quinidine, an antiarrhythmic agent, directly inhibits OCT2 by competing for substrate binding sites, reducing the transport of cationic drugs. Verapamil, a calcium channel blocker, indirectly impacts OCT2 by inhibiting P-glycoprotein (P-gp), affecting the disposition of substrates recognized by both P-gp and OCT2. Famotidine, another H2 receptor antagonist, directly inhibits OCT2 by competing for binding sites, reducing the transport of cationic substrates. Pyrimethamine, an antiprotozoal agent, indirectly influences OCT2 by inhibiting P-glycoprotein (P-gp), affecting the disposition of drugs recognized by both P-gp and OCT2. Amiloride, a sodium channel blocker, indirectly affects OCT2 by inhibiting NHE3, a sodium-hydrogen exchanger, potentially altering the cellular environment and impacting OCT2 activity. Rifampin, an antibiotic, indirectly influences OCT2 by inducing the expression of efflux transporters, such as P-glycoprotein (P-gp). Minoxidil, a vasodilator, directly inhibits OCT2 by competing for substrate binding sites. Gemfibrozil, a PPARα agonist, indirectly modulates OCT2 activity by influencing the expression of organic anion transporters (OATs), which can impact the disposition of substrates recognized by both OATs and OCT2. In summary, OCT2 inhibitors present a versatile collection of compounds that offer potential strategies for precise modulation of OCT2 activity through direct and indirect mechanisms.