GSK494581A is a both a glycine transporter subtype 1 inhibitor and GPR55 agonist.
Uses
GSK494581A is a specific ligand for human GPR55 (pEC50 of 6.8) and also acts as an inhibitor of glycine transporter subtype 1 (GlyT1). GSK494581A may regulate pain signaling, bone morphogenesis, and vascular endothelial cell formation by binding to GPR55[1].
IC 50
rGlyT1
References
[1] Brown AJ, et al. Pharmacology of GPR55 in yeast and identification of GSK494581A as a mixed-activity glycine transporter subtype 1 inhibitor and GPR55 agonist. J Pharmacol Exp Ther. 2011 Apr;337(1):236-46. DOI:10.1124/jpet.110.172650
