AMPA Receptor Antagonist

CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC₅₀s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist. CNQX blocks the expression of fear-potentiated startle in rats.

NBQX (FG9202) is a highly selective and competitive AMPA receptor antagonist. NBQX has neuroprotective and anticonvulsant activity.

EGIS-9637 is a non-competitive AMPA antagonist and acylated dihydro-2,3-benzodiazepine class member.

Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.

NBQX disodium (FG9202 disodium) is a highly selective and competitive AMPA receptor antagonist. NBQX disodium has neuroprotective and anticonvulsant activity.

DNQX (FG 9041), a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC₅₀s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively).

CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC₅₀s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist. CNQX disodium blocks the expression of fear-potentiated startle in rats.

GYKI 53655 (LY300168) hydrochloride is an α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) antagonist.

Talampanel (LY300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity. Talampanel (IVAX) has neuroprotective effects in rodent stroke models. Talampanel attenuates caspase-3 dependent apoptosis in mouse brain.

GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC₅₀ values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research.

Fanapanel (ZK200775) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.

LY3130481 is an orally available AMPA receptor antagonist, selectively inhibiting the IC₅₀ value of AMPA/TARP γ-8 at 65 nM. LY3130481 has anticonvulsant, antiepileptic, and pain-relieving effects.

Caroverine hydrochloride is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine hydrochloride is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine hydrochloride can be used for the research of inner ear tinnitus.

Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC₅₀s of 263 and 296 nM, respectively.

YM90K is a potent and selective AMPA receptor antagonist with a K_i of 84 nM. YM90K is less potent in inhibiting kainate (K_i of 2.2 μM) and NMDA (K_i of 37 μM) receptors. YM90K has neuroprotective actions.

Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.

Selurampanel (BGG 492) is an orally active and competitive AMPA receptor antagonist with an IC₅₀ of 190 nM. Selurampanel has reasonable blood-brain barrier penetration. Selurampanel can be used for epilepsy research.

SYM2206 is a potent and non-competitive AMPA receptor antagonist, with an IC₅₀ of 1.6 μM. SYM2206 blocks Na_v1.6-mediated persistent currents.

Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.

Fanapanel hydrate (ZK200775 hydrate) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.