| Bioactivity | 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]. |
| Invitro | 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 AUC0-5 h are increased by Zosuquidar administration[2].Bioavailability of Talinolol can be enhanced by coadministration with grapefruit juice (GFJ) in rats[3]. |
| Name | Talinolol |
| CAS | 57460-41-0 |
| Formula | C20H33N3O3 |
| Molar Mass | 363.49 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [1]. Assmann I. The actions of talinolol, a beta 1-selective beta blocker, in cardiac arrhythmia and acute myocardial infarction. Curr Med Res Opin. 1995;13(6):325-42. [2]. Kara ZP, et, al. The effects of P-glycoprotein inhibitor zosuquidar on the sex and time-dependent pharmacokinetics of parenterally administered talinolol in mice. Eur J Pharm Sci. 2021 Jan 1;156:105589. [3]. Shirasaka Y, et, al. Species difference in the effect of grapefruit juice on intestinal absorption of talinolol between human and rat. J Pharmacol Exp Ther. 2010 Jan;332(1):181-9. |