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
Solubility overview
Soluble in NaOH(aq) (10mM)
Storage instructions
Room temperature
Storage of solutions
Prepare and use solutions on the same day if possible. Store solutions at -20°C for up to one month if storage is required. Equilibrate to RT and ensure the solution is precipitate free before use.
Shipping Conditions
Stable for ambient temperature shipping. Follow storage instructions on receipt.
Important
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.