Biochem/physiol Actions

ML297 (VU0456810) is the first potent and selective activator of the GIRK potassium channel. The G protein-coupled inwardly-rectifying potassium channels (GIRKs 1-4) are widely distributed broadly in the central nervous system (GIRKs 1-3) and also found in the heart (GIRK-4). ML297 activates GIRK channels containing a GIRK1 subunit, and does not activate channels without a GIRK1 subunit or the closely related potassium channel Kir2.1 or voltage-gated potassium channels. ML297 has been shown to activate GIRK1/2 with a potency of ~160 nM and also to activate GIRK channels comprising of GIRK1/3 and GIRK1/4 subunit combinations. ML297 was active in two in vivo models of epilepsy, and showed equal or greater efficacy than the anti-seizure medication, sodium valproate.

Features and Benefits

This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Packaging

5, 25 mg in glass bottle