UBP 302

Biological Activity

UBP 302 is a potent and selective GluK1 (formally GluR5)-subunit containing kainate receptor antagonist (apparent K_D = 402 nM); active enantiomer of UBP 296 (Cat. No. 2078). Displays ~ 260-fold selectivity over AMPA receptors, ~ 90-fold selectivity over recombinant human GluK2 (formally GluR6) and GluK5 (formally KA2)-containing kainate receptors and has little or no action at NMDA or group I mGlu receptors. Selectively blocks kainate receptor-mediated LTP induction in rat hippocampal mossy fibers. Also protects against soman-induced seizures and neuronal degeneration for up to 30 days when administered one hour after soman exposure.

Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. The Limitations of D.pam as a Treatment for Nerve Agent-Induced Seizures and Neuropathology in Rats: Comparison with UBP302.
   Apland et al.
   J.Pharmacol.Exp.Ther., 2014;351:359
2. Characterisation of UBP296: a novel, potent and selective kainate receptor antagonist.
   More et al.
   Neuropharmacology, 2004;47:46
3. Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.
   Dolman et al.
   J.Med.Chem., 2005;48:7867

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