ML-297

G protein-regulated inwardly rectifying potassium (GIRK1-4) channels are a family of K_ir3.1-K_ir3.4 ion channels that modulate cell excitability. The four different GIRK subunits are composed in different homo- and heterotetrameric combinations, which are expressed with regional specificity throughout the central nervous system and in the periphery.¹ ML-297 is a selective GIRK1/2 activator (EC₅₀s = 0.16 and 1.8 μM for GIRK1/2 and GIRK1/4, respectively, and is completely inactive at GIRK2/3).^1,2 In two different mouse models of epilepsy, ML-297 at 60 mg/kg was shown to delay seizure onset and to prevent convulsions.¹

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1. Kaufmann, K., Romaine, I.M., Days, E., et al. ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice. ACS Chem. Neurosci. 4(9), 1278-1286 (2013).

2. Wen, W., Wu, W., Romaine, I.M., et al. Discovery of 'molecular switches' within a GIRK activator scaffold that afford selective GIRK inhibitors. Bioorg. Med. Chem. Lett. 23(16), 4562-4566 (2013).