Organic Cation Transporter Family

Human OCTN1 (SLC22A4)

   Human OCTN1 is a proton/organic cation exchanger, and is highly expressed at the apical membrane of proximal renal tubular cells in kidney.
   It is reported that human OCTN1 carries several organic cations, including tetraethylammonium, and endogenous nutrients, such as carnitine and ergothioneine.

<References>
   Tamai I, Yabuuchi H, Nezu J, Sai Y, Oku A, Shimane M, Tsuji A. (1997)  Cloning and characterization of a novel human pH-dependent organic cation transporter, OCTN1. FEBS Lett 419(1): 107-11.

   Yabuuchi H, Tamai I, Nezu J, Sakamoto K, Oku A, Shimane M, Sai Y, Tsuji A. (1999)  Novel membrane transporter OCTN1 mediates multispecific, bidirectional, and pH-dependent transport of organic cations. J Pharmacol Exp Ther 289(2): 768-773.

   Tamai I, Nakanishi T, Kobayashi D, China K, Kosugi Y, Nezu J, Sai Y, Tsuji A. (2004)  Involvement of OCTN1 (SLC22A4) in pH-dependent transport of organic cations.  Mol Pharm 1(1): 57-66.

   Kobayashi D, Aizawa S, Maeda T, Tsuboi I, Yabuuchi H, Nezu J, Tsuji A, Tamai I. (2004) Expression of organic cation transporter OCTN1 in hematopoietic cells during erythroid differentiation. Exp Hematol 32(12): 1156-1162.

   Grundemann D, Harlfinger S, Golz S, Geerts A, Lazar A, Berkels R, Jung N, Rubbert A, Schomig E. (2005) Discovery of the ergothioneine transporter. Proc Natl Acad Sci USA 102(14): 5256-61.

   Urban TJ, Brown C, Castro RA, Shah N, Mercer R, Huang Y, Brett CM, Burchard EG, Giacomini KM. (2007) Effect of genetic variation in the novel organic cation transporter, OCTN1, on the renal clearance of gabapentin. Clin Pharmacol Ther Jul 4.