3.1/3.2 (GIRK1/2) channel activator (IC50
values are 160, 887 and 914 nM for GIRK1/2, GIRK1/4 and GIRK1/3 respectively). Exhibits no effect on GIRK2, GIRK2/3, Kir
2.1 and Kv
7.4 channels, and has minimal effect on a panel of other ion channels, receptors and transporters. Prevents PTZ
-induced epileptic seizures in mice. Brain penetrant.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice.
Kaufmann et al.
ACS Chem.Neurosci., 2013;4:1278
Discovery of 'molecular switches' within a GIRK activator scaffold that afford selective GIRK inhibitors.
Wen et al.