Talinolol

Talinolol (Cordanum) is a long-acting, cardioselective β1-adrenergic receptor blocker. Talinolol exhibits cardioprotective and antihypertensive activities. Talinolol is also a well-known and frequently used probe substrate for P-glycoprotein (P-gp) activity^[1][2]. In Vitro: Human OATP1A2-, rat Oatp1a5-, and rat Mdr1a-mediated Talinolol transport can be inhibited by naringin, with IC₅₀s of 343, 12.7, and 604 μM, respectively, in LLC-PK1 cell and Xenopus laevis oocyte systems^[3]. In Vivo: Talinolol (20 mg/kg; i.p.) plasma and liver AUC_{0-5 h are increased by Zosuquidar administration^[2].
Bioavailability of Talinolol can be enhanced by coadministration with grapefruit juice (GFJ) in rats^[3].}