<unk>  is a selective non-competitive antagonist of AMPA receptors, the major subtype of ionotropic glutamate receptors. It was the first drug of this class approved for epilepsy. Whole-cell voltage clamp studies have demonstrated that<unk>  is a negative allosteric AMPA receptor antagonist.<unk>  caused a slow (τ∼1 s at 3 μM), concentration-dependent inhibition of AMPA receptor currents. The rates of block and unblock of AMPA receptor currents were 1.5 × 105 M−1 s−1 and 0.58 s−1, respectively.<unk>  did not affect NMDA receptor currents. The extent of block (IC50, 0.56 μM) was similar at all agonist concentrations, demonstrating a noncompetitive blocking action.<unk>  did affect AMPA receptor desensitization, or the ratio of peak to late response to rapid application of AMPA.<unk>  is a selective negative allosteric AMPA receptor antagonist of high-affinity and slow blocking kinetics, and is not use-dependent.<unk>  has a prolonged terminal half-life in humans of approximately 105 hours. The drug is 95% bound to plasma protein. Its primary route of metabolism is by CYP3A4. It does not induce P450 enzymes. About 70% of the dose is excreted in the feces and 30% in the urine; less than 2% of the dose is excreted unchanged into the urine.
Perampanel
Glybuzole
Glysobuzole
Methocarbamol
Tirapazamine
Milnacipran
Carbidopa
Tezacaftor