AMPA Receptor Inhibitor

Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy.

Naspm (1-Naphthyl acetyl spermine), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.

Naspm trihydrochloride (1-Naphthylacetyl spermine trihydrochloride), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.

Decanoic acid-d₁₉9 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects.

JNJ-55511118 is a selective TARP γ-8 binding AMPA receptor modulator with oral bioavailability and blood-brain barrier permeability, with a K_i of 26 nM. JNJ-55511118 reduces voluntary intake of sweetened alcohol in male mice. In rodent models, JNJ-55511118 inhibits hippocampal neurotransmission, reduces specific electroencephalogram frequency bands, induces transient hyperlocomotion, impairs learning and memory abilities, and exerts anticonvulsant effects. JNJ-55511118 is applicable to research related to alcohol use disorder and seizures.

gamma-DGG is a competitive AMPA receptor blocker.

Decanoic acid-d₅ is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects.

TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction.

Decanoic acid-d₃ is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects.

IEM-1754, a dicationic adamantane derivative, is a potent blocker of open channels of native ionotropic glutamate receptors including quisqualate-sensitive receptors in insect muscles, NMDAR in cultured rat cortical neurons, and AMPAR in freshly isolated hippocampal cells. IEM-1754 shows anticonvulsant potency in vivo.

D15, a peptide with 15 aa segment of dynamin, is an AMPAR endocytosis inhibitor. D15 blocks the interaction of dynamin with amphiphysin 1 and 2. D15 significantly increases AMPAR excitatory postsynaptic potential (EPSC) amplitude of medium spiny neurons (MSNs) in Sapap3 KO mice. D15 can be used for neuropsychiatric disorder research.

ZCAN262 (compound 6 ) is an AMPA modulator. ZCAN262 prevents AMPA-mediated excitotoxicity by targeting an allosteric binding site.

BDZ-P7 inhibits AMPA receptor GluA2, GluA1/2, GluA2/3, and GluA1 subunit with IC₅₀s of 3.03 μM, 3.14 μM, 3.19 μM, 3.2 μM. BDZ-P7 has neuroprotective effect and reinstates locomotor abilities in a mouse model of Parkinson’s disease.

Pep2m is a peptide receptor inhibitor. Pep2m inhibits the interaction between the C-terminus of the AMPA-type glutamate receptor (GluA2) subunit and N-ethylmaleimide-sensitive fusion protein (NSF). Pep2m prevents synaptic long-term depression (LTD). Pep2m can reduce postsynaptic currents in neurons, AMPA-mediated currents in cultured hippocampal neurons, and AMPA receptor surface expression^{[1][2][3][4][5]}.

TAN 950A is antifungal amino acid antibiotic. TAN 950A has affinity for three excitatory amino acid (EAA) receptor and can inhibit [3H]AMPA, [3H]kainite and [3H]CPP binding competitively. TAN 950A can be used for the researches of infection and neurological disease.

Decanoic acid-d₂ is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects.