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The cationic amino acid transporter 1 (CAT1/ SLC7A1 ) plays a key role in the cellular uptake or export of  l -arginine and some of its derivatives. This study investigated the effect of 113 chemically diverse and commonly used drugs (at 20 and 200 µM) on the CAT1-mediated cellular uptake of  l -arginine,  l -homoarginine, and asymmetric dimethylarginine (ADMA). Twenty-three (20%) of the tested substances showed weak inhibitory or stimulatory effects, but only verapamil showed consistent inhibitory effects on CAT1-mediated transport of all tested substrates.

Screening of commonly prescribed drugs for effects on the CAT1-mediated transport of l-arginine and arginine derivatives