Transport Mechanism of Nicotine in Primary Cultured Alveolar Epithelial Cells

Journal of Pharmaceutical Sciences
M TakanoRyoko Yumoto

Abstract

Nicotine is absorbed from the lungs into the systemic circulation during cigarette smoking. However, there is little information concerning the transport mechanism of nicotine in alveolar epithelial cells. In this study, we characterized the uptake of nicotine in rat primary cultured type II (TII) and transdifferentiated type I-like (TIL) epithelial cells. In both TIL and TII cells, [(3)H]nicotine uptake was time and temperature-dependent, and showed saturation kinetics. [(3)H]Nicotine uptake in these cells was not affected by Na(+), but was sensitive to extracellular and intracellular pH, suggesting the involvement of a nicotine/proton antiport system. The uptake of [(3)H]nicotine in these cells was potently inhibited by organic cations such as clonidine, diphenhydramine, and pyrilamine, but was not affected by substrates and/or inhibitors of known organic cation transporters such as carnitine, 1-methyl-4-phenylpyridinium, and tetraethylammonium. In addition, the uptake of [(3)H]nicotine in TIL cells was stimulated by preloading the cells with unlabeled nicotine, pyrilamine, and diphenhydramine, but not with tetraethylammonium. These results suggest that a novel proton-coupled antiporter is involved in the uptake of nicotine i...Continue Reading

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Citations

Nov 14, 2016·Human Cell·Shigeki OritaniTakaki Ishikawa
Apr 8, 2020·Journal of Analytical Methods in Chemistry·Vinit V GholapMatthew S Halquist
Aug 28, 2020·Expert Opinion on Drug Delivery·Vinit V GholapMatthew S Halquist
Sep 4, 2017·Life Sciences·Mikihisa TakanoRyoko Yumoto

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