(±)-Talinolol is a β1-selective adrenoceptor antagonist well known for its cardioprotective and antihypertensive activity. By blocking β1-adrenergic receptors, talinolol delays the conduction of stimuli in the AV node, reduces the sino-atrial conduction time, and impedes the sinus node automaticity. Because its metabolism in human liver microsomes is well understood, (±)-talinolol is useful for examining the activity of the drug-transporting MDR1 gene product P-glycoprotein.
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Selective β1-adrenergic blocker structurally related to Practolol. Antihypertensive; antiarrhythmic.
ChEBI: Talinolol is a member of ureas.
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].
Beta-1 adrenergic receptor
[1] abmann i. the actions of talinolol, a β1-selective beta blocker, in cardiac arrhythmia and acute myocardial infarction[j]. current medical research and opinion, 2008, 13(6): 325-342.
[2] trausch b, oertel r, richter k, et al. disposition and bioavailability of the β1‐adrenoceptor antagonist talinolol in man[j]. biopharmaceutics & drug disposition, 1995, 16(5): 403-414.
