TABLE 1

Pharmacology of TREK-1 K+ channel inhibition


Drug

IC50

Source
μM
Penfluridol 0.187,0.350 Gomora and Enyeart (1999a), Enyeart et al. (2002a)
Fluspirilene 0.232 Gomora and Enyeart (1999a)
Pimozide 0.354 Gomora and Enyeart (1999a)
Amlodipine 0.43 This study
Mibefradil 0.500 Gomora and Enyeart (1999b)
Niguldipine 0.75 This study
Flupenthixol 2.0 Thümmler et al. (2007)
Flunarizine 2.48 This study
Chlorpromazine 2.70 Meadows et al. (2001)
Sipatrigine 4.0 Meadows et al. (2001)
Fluphenazine 4.7 Thümmler et al. (2007)
Anandamide 5.10 This study
Haloperidol 5.5 Meadows et al. (2001)
Nifedipine 8.18 This study
Fluoxetine 19.0 Kennard et al. (2005)
Loxapine 19.7 Meadows et al. (2001)
Quinidine 24.1 Gomora and Enyeart (1999a)
l-cis-Diltiazem 24.8 Gomora and Enyeart (1999a)
Yb3+ 50 Enyeart et al. (2002b)
La3+ 52 Enyeart et al. (2002b)
Glibenclamide 64 Gomora and Enyeart (1999a)
Bupivacaine 113 Gomora and Enyeart (1999a)
Caffeine 377 Harinath and Sikdar (2005)
Theophylline 486 Harinath and Sikdar (2005)
Zinc 659 Gruss et al. (2004)
Tolbutamide 784 Gomora and Enyeart (1999a)
Ba2+ 1027 Gomora and Enyeart (1999a)
4-AP 2750 Gomora and Enyeart (1999a)
TEA
24,270
Gomora and Enyeart (1999a)