Title : The Nonmetabolized β-Blocker Nadolol Is a Substrate of OCT1, OCT2, MATE1, MATE2-K, and P-Glycoprotein, but Not of OATP1B1 and OATP1B3.

Pub. Date : 2016 Feb 1

PMID : 26702643






4 Functional Relationships(s)
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Compound Name
Protein Name
Organism
1 The Nonmetabolized beta-Blocker Nadolol Is a Substrate of OCT1, OCT2, MATE1, MATE2-K, and P-Glycoprotein, but Not of OATP1B1 and OATP1B3. Nadolol POU class 2 homeobox 2 Homo sapiens
2 In contrast, a significantly higher nadolol accumulation (at 1 and 10 muM) was found in OCT1, OCT2, MATE1, and MATE2-K cells compared to control cells (P < 0.01). Nadolol POU class 2 homeobox 2 Homo sapiens
3 Km values for OCT2-, MATE1-, and MATE2-K-mediated nadolol uptake were 122, 531, and 372 muM, respectively. Nadolol POU class 2 homeobox 2 Homo sapiens
4 In summary, nadolol is a substrate of the cation transporters OCT1, OCT2, MATE1, MATE2-K, and of P-gp. Nadolol POU class 2 homeobox 2 Homo sapiens