Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter.

Article Details

Citation

Wu X, Huang W, Prasad PD, Seth P, Rajan DP, Leibach FH, Chen J, Conway SJ, Ganapathy V

Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter.

J Pharmacol Exp Ther. 1999 Sep;290(3):1482-92.

PubMed ID
10454528 [ View in PubMed
]
Abstract

We have demonstrated in the present study that novel organic cation transporter (OCTN) 2 is a transporter for organic cations as well as carnitine. OCTN2 transports organic cations without involving Na(+), but it transports carnitine only in the presence of Na(+). The ability to transport organic cations and carnitine is demonstrable with human, rat, and mouse OCTN2s. Na(+) does not influence the affinity of OCTN2 for organic cations, but it increases the affinity severalfold for carnitine. The short-chain acyl esters of carnitine are also transported by OCTN2. Two mutations, M352R and P478L, in human OCTN2 are associated with loss of transport function, but the protein expression of these mutants is comparable to that of the wild-type human OCTN2. In situ hybridization in the rat shows that OCTN2 is expressed in the proximal and distal tubules and in the glomeruli in the kidney, in the myocardium, valves, and arterioles in the heart, in the labyrinthine layer of the placenta, and in the cortex, hippocampus, and cerebellum in the brain. This is the first report that OCTN2 is a Na(+)-independent organic cation transporter as well as a Na(+)-dependent carnitine transporter and that OCTN2 is expressed not only in the heart, kidney, and placenta but also in the brain.

DrugBank Data that Cites this Article

Drug Transporters
DrugTransporterKindOrganismPharmacological ActionActions
AmphetamineSolute carrier family 22 member 5ProteinHumans
Unknown
Substrate
Details
CholineSolute carrier family 22 member 5ProteinHumans
Unknown
Inhibitor
Details
Choline salicylateSolute carrier family 22 member 5ProteinHumans
Unknown
Inhibitor
Details
CimetidineSolute carrier family 22 member 5ProteinHumans
Unknown
Inhibitor
Details
ClonidineSolute carrier family 22 member 5ProteinHumans
Unknown
Inhibitor
Details
DesipramineSolute carrier family 22 member 5ProteinHumans
Unknown
Inhibitor
Details
DopamineSolute carrier family 22 member 5ProteinHumans
Unknown
Inhibitor
Details
GuanidineSolute carrier family 22 member 5ProteinHumans
Unknown
Inhibitor
Details
LevocarnitineSolute carrier family 22 member 5ProteinHumans
Unknown
Substrate
Details
MetamfetamineSolute carrier family 22 member 5ProteinHumans
Unknown
Inhibitor
Details
NicotineSolute carrier family 22 member 5ProteinHumans
Unknown
Inhibitor
Details
NorepinephrineSolute carrier family 22 member 5ProteinHumans
Unknown
Inhibitor
Details
ProcainamideSolute carrier family 22 member 5ProteinHumans
Unknown
Inhibitor
Details
ThiamineSolute carrier family 22 member 5ProteinHumans
Unknown
Inhibitor
Details
Polypeptides
NameUniProt ID
Solute carrier family 22 member 5O76082Details