ML297
GIRK inhibitor / Selective GIRK ½ (Kir3.1/3.2) channel activator, IC50 = 160, 887 and 914 nM for GIRK1/2, GIRK1/4 and GIRK1/3 respectively. Has no effect on GIRK2, GIRK2/3, Kir2.1 and Kv7.4 channels.1,2 Displays antiseizure activity2 and decreases anxiety-related behavior without sedative or addictive effects3. Reduces glucose- and IBMX-stimulated GLP-1 secretion with no effect on GIP in murine L and K cells.4 Brain penetrant.
Biochemicals & reagents
1443246-62-5
VU0456810
1) Wen et al. (2014), Discovery of potent and selective GIRK1/2 modulators via “molecular switches’ within a series of 1-(3-cyclopropyl-1-phenyl-1H-pyrazol-5-yl)ureas; Bioorg. Med. Chem. Lett., 24 5102 2) Kaufmann et al. (2013), ML-297 (VU0456810), the first potent and selective activator of the GIRK otassium channel, displays antiepileptic properties in mice; ACS Chem. Neurosci., 4 1278 3) Wydeven et al. (2014), Mechanisms underlying the activation of G-protein-gated inwardly rectifying K+ (GIRK) channels by the novel anxiolytic drug, ML297; Proc. Natl. Acad. Sci. USA, 111 10755 4) Psichas et al. (2016), Galanin inhibits GLP-1 and GIP secretion via the GAL1 receptor in enteroendocrine L and K cells; Br. J. Pharmacol., 173 888
-20°C
TARGET: Ion channel -- PATHWAY: Potassium channel; Carbohydrate metabolism -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Mood disorders