iGluR Inhibitor

PSD-95/nNOS PPI-IN-1 is a inhibitor targeting the PSD-95/nNOS interaction with potential blood-brain barrier penetration. PSD-95/nNOS PPI-IN-1 binds to the PSD-95 PDZ2 domain with high affinity (K_i = 19.45 μM). PSD-95/nNOS PPI-IN-1 inhibits glutamate-induced excitotoxicity by reducing intracellular ROS levels and inhibiting apoptosis. PSD-95/nNOS PPI-IN-1 significantly reduces cerebral infarct volume in rat tMCAO models. PSD-95/nNOS PPI-IN-1 can be used for the study of acute ischemic stroke.

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.

TAT-NSF222 Fusion Peptide is a fusion polypeptide with two domains, a TAT domain, which enters cells through macropinocytosis, and an NSF domain that inhibits N-ethylmaleimide-sensitive factor (NSF). TAT-NSF222 Fusion Peptide is an exocytosis inhibitor.

Bupivacaine hydrochloride monohydrate is a NMDA receptor inhibitor. Bupivacaine hydrochloride monohydrate can block sodium, L-calcium, and potassium channels. Bupivacaine hydrochloride monohydrate potently blocks SCN5A channels with the IC₅₀ of 69.5 μM. Bupivacaine hydrochloride monohydrate can be used for the research of chronic pain.

Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC₅₀ of 42.0 μM.

Oleoyl-D-lysine sodium is a selective Glycine Transporter-2 (GlyT2) inhibitor based on lipid. Oleoyl-D-lysine sodium reverses neuropathic pain in mice, shows antidrowsiness effect on chronic neuropathic pain. Oleoyl-D-lysine sodium is safe and effective without respiratory depression.

BTS 72664 is a broad-spectrum, non-sedating, orally effective anticonvulsant. Its anticonvulsant effect mainly arises from enhancing GABA_A receptor (GABA_A receptor)-mediated chloride channel currents, while it exerts weak blocking effects on Na⁺ channels (K_i = 350 μM) and NMDA receptors (NMDA receptor) (IC₅₀ = 43 μM). BTS 72664 prevents the elevation of extracellular glutamate, glycine and serine concentrations in neurons, reduces cerebral infarct size, promotes functional recovery, prevents multiple types of epileptic seizures, and has low sedative potential. BTS 72664 can be used for the research of epilepsy, stroke and migraine.

(S)-3-Hydroxyphenylglycine ((S)-3HPG) is a metabotropic glutamate receptor (mGluR) agonist with an EC₅₀ of 98 μM in rats. (S)-3-Hydroxyphenylglycine stimulates phosphoinositide hydrolysis, inhibits ACPD-induced depolarization, and exerts weak agonistic and inhibitory effects on mGluR1-mediated signal transduction. (S)-3-Hydroxyphenylglycine selectively activates mGluR1/5, downregulates NMDA receptor channels, reduces NMDA whole-cell currents and intracellular Ca²⁺ accumulation, and induces rapid intracellular Ca²⁺ oscillations in cortical neurons.

AMPA-IN-2 is an orally active AMPA inhibitor that can cross the blood-brain barrier. AMPA-IN-2 improves epileptic seizures by inhibiting the intrinsic excitability of neurons and inhibiting the excitability of glutamatergic transmission. AMPA-IN-2 exerts anti-epileptic effects in the pentylenetetrazol (PTZ) model and can be used as a promising candidates with high broad-spectrum anti-epileptic potential.

AChE-IN-53 (Compound I-52) is a potent NMDAR inhibitor, which is a compound with favorable behavioral and neuroprotective effects.

Tat-CBD3 TFA, a 15-amino acid peptide from CRMP2, fused to the TAT cell-penetrating motif of the HIV-1 protein, disrupts CRMP2-NMDAR interaction without change in NMDAR localization.

L644711 is an anion transport inhibitor that reduces cell swelling by inhibiting potassium-activated D-aspartate release in astrocytes. L644711 can be used in the study of brain injury and neuroprotection.

AVLX-125 (UCCB01-125) is a PSD-95 and PDZ domain inhibitor with K_d value of 10 nM. AVLX-125 can be used in the study of inflammatory pain.

LBG20304 (compound 2s) is a ligand for the homologous GluK5 receptor (IC₅₀: 432 nM), more than 40-fold selective over the homologous GluK1-3 isoforms. Low doses of LBG20304 (<10 μM) have no agonist or antagonist functional response at heterologous GluK2/5 receptors, and at high doses (>10 μM), it exhibits low agonist activity in neuronal slices (rat).

Felbamate (Standard) is the analytical standard of Felbamate. This product is intended for research and analytical applications. Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA).

(S)-Norzopiclone ((S)-N-Desmethyl zopiclone; SEP-174559) is a metabolite of Zopiclone with anxiolytic and anticonvulsant effects. (S)-Norzopiclone has benzodiazepine-like actions at γ2-bearing subtypes of the GABA_A receptor and inhibits nACh and NMDA receptors.

BMS-986169 is an inhibitor of the glutamate N-methyl-D-aspartate 2B receptor (GluN2B). BMS-986169 has a high binding affinity for the allosteric regulatory site of the GluN2B subunit, with a K_i value of 4.03-6.3 nM. BMS-986169 can inhibit the function of GluN2B receptors in Xenopus oocytes, with an IC₅₀ value of 24.1 nM. BMS-986169 can also inhibit the activity of the hERG channel, with an IC₅₀ value of 28.4 μM. BMS-986169 can be used in research on treatment-resistant depression.

NMDA-IN-2 (compound 6b), a Procaine derivative, is a NMDA receptor 2B subtype inhibitor.

Caged MK801 (cMK801) is a selective, non-competitive, irreversible NMDA receptor open-channel blocker. NVOC cages are neuro pharmocologically compatible.

Felbamate hydrate (W-554 hydrate) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA) .