Potent and selective GluK1 (formerly GluR5) and GluK3 (formerly GluR7) subunit selective kainate receptor antagonist (Kb = 10 nM and IC50 = 23 nM respectively). IC50 values are > 100 µM for GluA2, GluK6, GluK2/3 and GluK6/GluK2 respectively. Active at AMPA receptors and inactive against NMDA and Group I mGlu receptors at concentrations of up to 10 µM.
Solubility & Handling
Storage instructions
+4°C
Solubility overview
Soluble in DMSO
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.