Potent and selective GluK1 (GluR5) kainate receptor antagonist (Kb = 1.4 nM). Ineffective at GluK2, GluK3 and mGluR 6 and 7 receptors. Blocks NMDA receptor -independent long term potentiation induction.
Solubility & Handling
Soluble in NaOH(aq) (10mM)
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
Dolman NP et al (2007) J Med Chem 50(7) : 1558-70.