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MATE transport can be inhibited by a number of chemicals. Structural examples are shown in Fig. 3.2. The antiparasitic drug, pyrimethamine, is considered one of the most potent and specific inhibitors. Inhibition of mMate1/hMATE1 is achieved at nanomolar concentrations of pyrimethamine, whereas micromolar concentrations are required to block mOct1/hOCT2 and mOct2/hOCT2 [52]. Cis‐inhibition of TEA transport by hMATE1 is observed with cimetidine, quinidine, procainamide, and verapamil and to a lesser degree nicotine, serotonin, and choline [5, 6]. Likewise, a number of hormones can inhibit TEA transport in hMATE1‐ and mMate1‐expressing cells including corticosterone, testosterone, progesterone, and androstenedione [15]. Notably, no effects on hMATE1 or hMATE2‐K activity by organic anions such as p‐aminohippurate, uric acid, and beta‐lactam antibiotics were observed [5, 6].