Title : Tropane alkaloids as substrates and inhibitors of human organic cation transporters of the SLC22 (OCT) and the SLC47 (MATE) families.

Pub. Date : 2017 Feb 1

PMID : 27676604






3 Functional Relationships(s)
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1 Overexpression of OCTs or MATEs in HEK293 cells resulted in an up to 63-fold increase in the uptake of ipratropium (Km of 0.32 mum to OCT2 and Vmax of 3.34 nmolxmg protein-1xmin-1 to MATE1). Ipratropium solute carrier family 22 member 2 Homo sapiens
2 Genetic polymorphisms in OCT1 and OCT2 affected ipratropium uptake and clinically relevant concentration of ondansetron and pyrithiamine inhibited ipratropium uptake via MATEs by more than 90%. Ipratropium solute carrier family 22 member 2 Homo sapiens
3 This study suggests that OCT1, OCT2 and MATEs may be strongly involved in the renal and extra-renal elimination of ipratropium and other quaternary amine alkaloids. Ipratropium solute carrier family 22 member 2 Homo sapiens