Table I.

Membrane proteins that are modified by the TZDs

TZD PPARγ EC50a Off-target and effect EC50b Reference 
 µM  µM  
Troglitazone 0.5 ATP-sensitive potassium channel KATP 0.7 Lee et al., 1996  
  L-type calcium channels 3–4 Nakamura et al., 1998  
  Ca2+-activated potassium channel BKCa 20–30c Knock et al., 1999; Stowers et al., 2000  
  Delayed rectifier potassium channel Kv1.3 Ahn et al., 2007  
  Acute glucose transport 3c Preininger et al., 1999  
  Na+/H+ exchange 10c de Dios et al., 2001  
  Bile transport (bile salt export pump) 4 10c Funk et al., 2001; Snow and Moseley, 2007  
Rosiglitazone 0.06–0.09 Voltage-dependent Ca2+ current 2c Knock et al., 1999  
  Ca2+-activated potassium channels, BKCa 20c Knock et al., 1999; Stowers et al., 2000  
  Delayed rectifier potassium channel Kv1.3 18 Ahn et al., 2007  
  Bile transport 10c Snow and Moseley, 2007  
Pioglitazone 0.6 L-type calcium channels 45 Nakamura et al., 1998  
Ciglitazone 3–23 Ca2+-activated potassium channel BKCa 16 Stowers et al., 2000  
  Store-operated calcium+ channels 30c Kim et al., 2005; Epshtein et al., 2009  
  Bile transport 5c Snow and Moseley, 2007  
TZD PPARγ EC50a Off-target and effect EC50b Reference 
 µM  µM  
Troglitazone 0.5 ATP-sensitive potassium channel KATP 0.7 Lee et al., 1996  
  L-type calcium channels 3–4 Nakamura et al., 1998  
  Ca2+-activated potassium channel BKCa 20–30c Knock et al., 1999; Stowers et al., 2000  
  Delayed rectifier potassium channel Kv1.3 Ahn et al., 2007  
  Acute glucose transport 3c Preininger et al., 1999  
  Na+/H+ exchange 10c de Dios et al., 2001  
  Bile transport (bile salt export pump) 4 10c Funk et al., 2001; Snow and Moseley, 2007  
Rosiglitazone 0.06–0.09 Voltage-dependent Ca2+ current 2c Knock et al., 1999  
  Ca2+-activated potassium channels, BKCa 20c Knock et al., 1999; Stowers et al., 2000  
  Delayed rectifier potassium channel Kv1.3 18 Ahn et al., 2007  
  Bile transport 10c Snow and Moseley, 2007  
Pioglitazone 0.6 L-type calcium channels 45 Nakamura et al., 1998  
Ciglitazone 3–23 Ca2+-activated potassium channel BKCa 16 Stowers et al., 2000  
  Store-operated calcium+ channels 30c Kim et al., 2005; Epshtein et al., 2009  
  Bile transport 5c Snow and Moseley, 2007  
a

Henke et al., 1998.

b

Nominal concentrations, not accounting for drug distribution.

c

Effective concentration.

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