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Vol. 30, Issue 2, 212-219, February 2002
Department of Pharmacology, Toxicology, and Therapeutics,
University of Kansas Medical Center, Kansas City, Kansas
Organic cation transporters (OCTs) are responsible for excretion of
cationic substances into urine. Tissue OCT expression may be important
for the disposition and excretion of xenobiotics. Therefore, OCT1,
OCT2, OCT3, OCTN1, and OCTN2 mRNA levels were measured in adult rat
tissues and rat kidney tissue at various stages of development from day
0 to 45. OCT1 mRNA expression was highest in kidney and spleen,
moderate in skin, and low in the gastrointestinal tract, brain, lung,
thymus, muscle, and prostate. OCT2 mRNA levels were highest in kidney,
with low expression in other tissues, and with renal OCT2 levels being
approximately 4 times higher in males than that in females. In
gonadectomized males, OCT2 mRNA levels were attenuated to female
levels, suggesting a role for testosterone in OCT2 expression. OCT3 was
moderately expressed in kidney and was highest in blood vessel, skin,
and thymus. OCTN1 was expressed in most of the tissues examined, with relatively higher expression in kidney and ileum and lower levels in
thymus. Lastly, OCTN2 was expressed abundantly in kidney and ileum,
moderately in large intestine, dorsal prostate, bladder, duodenum, and
cerebellum, and minimally in thymus, spleen, and cerebral cortex. Renal
OCT1, OCTN1, and OCTN2 mRNA levels increased gradually from postnatal
day 0 through day 45 in both genders. Renal OCT2 levels remained the
same in males and females through day 25 and then dramatically
increased only in male kidney after day 30. In summary, OCT mRNA was
detected primarily in kidney, and the high level of renal OCT
expression may explain why the kidney is a target organ for xenobiotics
with cationic properties.
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