TABLE 1.

IC₅₀ values for inhibitors of metformin uptake via cation-selective transporters

The IC₅₀ values reported were experimentally determined except for those entries in which literature values are cited.

Inhibitor	IC50 Values (Mean ± S.D.)
	OCT1	OCT2	OCT3	SERT	CHT	CTLs
	µM
Mitoxantrone	3.0 ± 0.8	135.0 ± 12.0	174.0 ± 19.0	977.2 ± 1.2	N/A	N/A
Cimetidine	20.9 ± 1.4	16.6 ± 1.3	9.8 ± 1.3	N/A	N/A	N/A
Corticosterone	3.2 ± 0.5	1.3 ± 0.1	0.2 ± 0.1	N/A	N/A	N/A
Paroxetine	1.0 ± 0.2	11.9 ± 1.2	6.4 ± 1.3	0.0060 ± 0.00059	N/A	N/A
Desipramine	2.2 ± 0.4	2.4 ± 0.2	3.8 ± 0.3	0.054 ± 0.0042a	N/A	N/A
HC3	112.2 ± 1.5	131.8 ± 1.4	524.8 ± 1.7	70.8 ± 1.2	0.004b	~100c

N/A, not available.

^aBarker et al., 1994.

^bApparsundaram et al., 2000.

^cLockman and Allen, 2002.