TABLE 2

Comparison of IC₅₀ values for the inhibition of OCT2-mediated NBD transport (column A) or of OCT2-mediated transport of MPP (column B)

Inhibitor	A^{^a}NBD IC₅₀	B^{^b}MPP IC₅₀	IC₅₀^MPP/IC₅₀^NBD
	μM
Ethylacridinium	0.08 ± 0.01 (4)
Ipratropium	0.17 ± 0.05 (3)	15	88
Imipramine	1.4 ± 0.3 (5)	6	4.2
Doxepin	1.5 ± 0.5 (4)	13	8.5
Amitriptyline	2.5 ± 0.5 (4)	14	5.7
Chlorpromazine	2.6 ± 0.4 (4)	14	5.4
MPP	3.0 ± 0.4 (5)
Propafenone	3.6 ± 0.5 (3)	25	7.0
Clonidine	4.5 ± 0.9 (5)	16	3.7
Diphenhydramine	5.8 ± 0.6 (3)
Carvedilol	13.1 ± 0.7 (3)	63	4.8
Verapamil	21.0 ± 1.7 (3)	85	4.1
Quinidine	29.6 ± 5.6 (4)	87	2.9
Disopyramide	39.0 ± 2 (6)	324	8.3
Propranolol	67.2 ± 7.0 (5)	229	3.4
Cimetidine	70.4 ± 8 (5)	120	1.7
TEA	110 ± 14.0 (4)
Trimethoprim	113 ± 14.0 (4)	1318	12
Chloroquine	117 ± 9.0 (3)	1096	9.3
TEMA	125 ± 14.0 (3)
Flecainide	234 ± 3.0 (2)	191	0.82
Metformin	1180 ± 138 (4)	397	0.34

TEMA, triethylmethylammonium.
↵^a Numbers represent the mean (± S.E.) of the number of separate experiments, performed OCT2-expressing CHO cells, indicated in parentheses.
↵b Values were obtained from Table 1 in Zolk et al. (2009).