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. Author manuscript; available in PMC: 2015 Apr 1.
Published in final edited form as: Curr Opin Pharmacol. 2013 Nov 26;15:7–15. doi: 10.1016/j.coph.2013.11.002

Table 1. Chemical diversity of Kir channel modulators.

Compound/PubChem CID Structure Action Selectivity (IC50/EC50)* Channel/Residues References
Chloroquine/2719 graphic file with name nihms540902t1.jpg Pore blocker IKACh (0.4) > IKATP (0.5) > IK1 (0.7) Kir2.1/E224, D259, E299, F254 [18,22]
Pentamidine/4735 Pore blocker Kir2.1 (0.2) > 2.2 > Kir2.3 Kir2.1/E224, D259, E299 [25]
ML133/781301 Pore blocker Kir2.1 (0.3†, 1.9) > 2.6 (2.8) > 2.2 (2.9) > 2.3 (4.0) > 6.2 (7.7) > 7.1 (32.9) > 4.1 (76) > 1.1 (>300) Kir2.1/D172, I176 [28]
Flecainide/3356 graphic file with name nihms540902t2.jpg Potentiator Kir2.1 (0.4†† − 0.8‡) > 2.2 ~ 2.3 ~ 2.1/2.2 ~ 2.1/2.3 Kir2.1/E224, D259, E299, C311 [33]
Fluoxetine/62857 Pore blocker Kir4.1 (15) > 2.1 ~ 1.1 Kir4.1/T128, L151, E158 [46,48]
Nortriptyline/4543 Pore blocker Kir4.1 (28) > 2.1 (245) Kir4.1/T128, L151, E158 [47,48]
VU590/4536383 graphic file with name nihms540902t3.jpg Pore blocker Kir1.1 (0.3) > 7.1 (8) > 2.1 ~ 4.1 Unknown [39]
VU573/44199324 Unknown Kir3.1/3.2 (2) > 2.3 (5) > 7.1 (5) Unknown [52]

See text for details.

*

μM,

†

at pH 8.5;

††

at 50 mV,

‡

at −120 mV