talinolol

Talinolol 是一种长效、心脏选择性的 β1-肾上腺素能受体阻滞剂，具有心脏保护和抗高血压作用。它也是众所周知且经常使用的 P-糖蛋白 (P-gp) 活性探针底物。

6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, and 0.22 μM in S9 human intestine cells. It has been studied in the context of drug interactions with grapefruit constituents. It is found in grapefruit juice at concentrations of 0.1-7.4 μM and inhibits the transport of talinolol , a permeability glycoprotein (P-gp/ABCB1) transporter substrate, across Caco-2 cell monolayers (IC50 = 0.7 μM). 6'7'-Epoxybergamottin also has insecticidal properties with a concentration of 5 μg/cm2 leading to 100% mortality of adult olive fruit flies.