gluk5

UBP 302 is an effective and selective GLUK5-subunit-containing kainate receptor antagonist (apparent Kd=402 nM) and displays very little affinity on GluK2 kainate receptors.

UBP310 (UBP 310) is a GLUK5 kainate receptor antagonist

NS 3763 is a kainate receptor antagonist.

LBG20304 (compound 2s) serves as a ligand for the homologous GluK5 receptor, demonstrating an IC50 of 432 nM and exhibiting over 40-fold selectivity against the GluK1-3 isoforms. At concentrations below 10 μM, LBG20304 shows neither agonistic nor antagonistic effects on heterologous GluK2/5 receptors. However, at concentrations above 10 μM, it displays minimal agonist activity in neuronal slices (rat).

5-Iodowillardiine is a selective agonist for specific kainate receptor subunits that robustly activates GluK1 (GluR5) and GluK5 (KA2)-containing receptors while displaying minimal activity at AMPA receptors and no measurable agonism toward GluK2 (GluR6) subunits. Despite its excitotoxic neurotoxic activity in vivo, 5-Iodowillardiine remains a powerful experimental tool for dissecting kainate receptor subtype distribution, synaptic function, and excitatory neurotransmission in the brain and spinal cord.

LY-466195 is a competitive antagonist of GLUK5 receptor.