PMID- 10454528 OWN - NLM STAT- MEDLINE DCOM- 19990921 LR - 20171116 IS - 0022-3565 (Print) IS - 0022-3565 (Linking) VI - 290 IP - 3 DP - 1999 Sep TI - Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter. PG - 1482-92 AB - 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. FAU - Wu, X AU - Wu X AD - Department of Biochemistry and Molecular Biology, Medical College of Georgia, Augusta, Georgia, USA. FAU - Huang, W AU - Huang W FAU - Prasad, P D AU - Prasad PD FAU - Seth, P AU - Seth P FAU - Rajan, D P AU - Rajan DP FAU - Leibach, F H AU - Leibach FH FAU - Chen, J AU - Chen J FAU - Conway, S J AU - Conway SJ FAU - Ganapathy, V AU - Ganapathy V LA - eng SI - GENBANK/AF110416 SI - GENBANK/AF110417 GR - DA 10045/DA/NIDA NIH HHS/United States GR - HD 33347/HD/NICHD NIH HHS/United States GR - HL 60104/HL/NHLBI NIH HHS/United States GR - etc. PT - Journal Article PT - Research Support, U.S. Gov't, P.H.S. PL - United States TA - J Pharmacol Exp Ther JT - The Journal of pharmacology and experimental therapeutics JID - 0376362 RN - 0 (Carrier Proteins) RN - 0 (Membrane Proteins) RN - 0 (Organic Cation Transport Proteins) RN - 0 (RNA, Messenger) RN - 0 (SLC22A5 protein, human) RN - 0 (Slc22a5 protein, mouse) RN - 0 (Slc22a5 protein, rat) RN - 0 (Solute Carrier Family 22 Member 5) RN - 17298-37-2 (propionylcarnitine) RN - 66-40-0 (Tetraethylammonium) RN - 6DH1W9VH8Q (Acetylcarnitine) RN - S7UI8SM58A (Carnitine) SB - IM MH - Acetylcarnitine/pharmacokinetics MH - Animals MH - Biological Transport, Active MH - Carnitine/analogs & derivatives/pharmacokinetics MH - Carrier Proteins/biosynthesis/metabolism/*physiology MH - Humans MH - In Situ Hybridization MH - Kidney/metabolism MH - Membrane Proteins/biosynthesis/metabolism/*physiology MH - Mice MH - Myocardium/metabolism MH - Organ Specificity MH - *Organic Cation Transport Proteins MH - Placenta/metabolism MH - RNA, Messenger/metabolism MH - Rats MH - Solute Carrier Family 22 Member 5 MH - Tetraethylammonium/pharmacokinetics EDAT- 1999/08/24 00:00 MHDA- 1999/08/24 00:01 CRDT- 1999/08/24 00:00 PHST- 1999/08/24 00:00 [pubmed] PHST- 1999/08/24 00:01 [medline] PHST- 1999/08/24 00:00 [entrez] PST - ppublish SO - J Pharmacol Exp Ther. 1999 Sep;290(3):1482-92.