Title : Effects of β-blockers and tricyclic antidepressants on the activity of human organic anion transporting polypeptide 1A2 (OATP1A2).

Pub. Date : 2015 Mar

PMID : 25563901






3 Functional Relationships(s)
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1 The primary objective of this study was to investigate OATP1A2 transport activity using rosuvastatin as a probe substrate and evaluate competitive inhibition of its transport by beta-blockers. Rosuvastatin Calcium solute carrier organic anion transporter family member 1A2 Homo sapiens
2 With the exception of carvedilol (IC50 of 3.2 microM), all of the other beta-blockers that were evaluated had a small or insignificant effect on OATP1A2-mediated uptake of rosuvastatin. Rosuvastatin Calcium solute carrier organic anion transporter family member 1A2 Homo sapiens
3 On the other hand, tricyclic compounds with a short aliphatic amine chain inhibited OATP1A2-mediated rosuvastatin transport. Rosuvastatin Calcium solute carrier organic anion transporter family member 1A2 Homo sapiens