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receptor ligands, enzyme inhibitors, signaling tools, ion channel modulators

Potent and competitive AMPA and kainate receptor antagonist. Water soluble, disodium salt. Also antagonizes NMDA receptors at the glycine site. Increases GABA_A receptor spontaneous postsynaptic currents (sPSCs). Shows neuroprotective actions. CNQX also available.

Potent, selective and competitive AMPA receptor antagonist. Also kainate receptor antagonist. Water soluble, disodium salt. Shows neuroprotective, antinociceptive and anticonvulsive actions. NBQX also available.

Novel, potent and selective G-protein coupled receptor kinase 2 and 3 (GRK2/GRK3) inhibitor (IC₅₀ values are 35 and 32 nM at GRK2 and GRK3 respectively).

Has no activity at GRK5 at concentrations up to 125 µM and shows little activity at a broad range of other kinases.

Membrane permeable.

Can be used to study roles of GRK2/3 in GPCR desensitization and other functions.

Shown to potentiate phosphatidylinositol 4,5-bisphosphate (PIP2) depletion and slow agonist-induced desensitization of protease-activated receptor 2 (PAR2).