Tetrazolyl glycine is an NMDA receptor agonist. It binds to rat brain membranes with IC50 values of 98 and 36 nM for [3H]CGS19755 and [3H]glutamate, respectively, in radioligand binding assays. It induces depolarization in rat cortical slices, an effect that is blocked by the NMDA receptor antagonist LY233053. It induces degeneration of GABAergic and cholinergic neurons in the striatum of adult rats and the formation of excitotoxic lesions and seizures in neonatal rats (ED50 = 0.071 mg/kg). Intrastriatal injection of tetrazolyl glycine (5 μM) increases COX-2 expression in striatal neurons and the vasculature near the striatal injection site in a mouse model of excitotoxicity-induced neuronal injury.
