iGluR Inhibitor

Praeruptorin A ((+)-Praeruptorin A) is an orally active isomer of (±)-Praeruptorin A (HY-N0081). Praeruptorin A also acts as a Calcium channel blocker. Praeruptorin A can be isolated from Peucedanum. Praeruptorin A serves as a substrate for CYP3A4. Praeruptorin A downregulates NMDA receptors containing GluN2B and inhibits neuronal Apoptosis. Praeruptorin A mediates vasodilation, inhibits vascular hypertrophy and reduces blood pressure. Praeruptorin A can be used in research related to neurological diseases, myocardial ischemia, heart failure, exertional angina, renovascular hypertension and spontaneous hypertension.

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.

SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders.

Brophenexin free base (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. Brophenexin free base shows neuroprotective activity. Brophenexin free base prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC₅₀ of 2.1 μM. Brophenexin free base protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss.

Naftazone is a naphthoquinone derivative, it can be used for the research of venous insufciency. Naftazone protects blood vessels, increases venous tonicity and capillary resistance, and improves lymphatic and venous circulation.

Trans-4-Carboxy-L-prolineis a selective glutamate transporter inhibitor.

Perzinfotel (EAA-090) is a potent, selective, and competitive NMDA receptor antagonist with neuroprotective effects. Perzinfotel (EAA-090) shows high affinity (IC₅₀=30 nM) for the glutamate site.

GluN1/3A-IN-1 (Compound GM-10) is a GluN1/GluN3A NMDA receptor inhibitor. GluN1/3A-IN-1 exhibits potent inhibitory activity against GluN1/GluN3A (IC₅₀: 0.98 µM). GluN1/3A-IN-1 exerts its inhibitory effect by targeting the pre-M1 region and forming hydrogen bond interactions with key residues. GluN1/3A-IN-1 can be used to study GluN1/GluN3A-related neurological diseases.

Arcaine (sulfate) is a glutamate NMDA receptor inhibitor.

Dimiracetam is an orally active compound, with anti-neuropathic activity. Dimiracetam inhibits hypersensitivity and neurological alterations, and inhibits Sorafenib (HY-10201)-induced neuropathy in cold stimulation rat models.

FP802 dihydrochloride is an orally active potent TwinF interface inhibitor that disrupts and detoxifies the NMDAR/TRPM4 death complex. FP802 dihydrochloride exerts powerful neuroprotective effects in the 5xFAD mouse model of Alzheimer’s disease (AD) by preventing cognitive decline, preserving neuronal structural integrity, reducing amyloid-β plaque formation, and mitigating mitochondrial pathology. FP802 dihydrochloride stops loss of motor neurons, reduces serum neurofilament light chain (NfL) levels, improves motor performance, and extends life in a mouse model of amyotrophic lateral sclerosis (ALS). FP802 dihydrochloride can be used for AD and ALS research.

Felbamate-d₄ (W-554-d4) is the deuterium labeled Felbamate. Felbamate (W-554) is a potent anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA).

BZAD-01 is a potent, selective and orally active inhibitor of NMDA NR2B subunit, with a K_i of 72 nM. BZAD-01 can improve postural asymmetry as well as Apomorphine-induced rotation.

TAT-EE3 is a neuroprotective peptide which can uncouple TRPM2-NMDARs interaction. TAT-EE3 inhibits TRPM2-induced enhancement of NMDAR surface expression and current amplitude.TAT-EE3 protects neurons against ischemic injury in vitro and in vivo. TAT-EE3can be used for the study of ischemic stroke.

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.

YY-23 is a selective inhibitor of NMDAR (containing GluN2C or GluN2D). YY-23 inhibits GABAergic neurotransmission and enhances excitatory transmission by inhibiting NMDARs containing GluN2D on GABAergic interneurons in the prefrontal cortex. YY-23 has antidepressant activity and can be used for the research of neurological diseases.

Bis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine. Bis(7)-tacrine dihydrochloride prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors. Bis(7)-tacrine dihydrochloride is a potent GABA_Areceptor antagonist. Bis(7)-tacrine dihydrochloride has the potential for the research of Alzheimer's disease .

pep2-SVKI is a selective peptide inhibitor. pep2-SVKI inhibits the binding of AMPA-type glutamate receptor (GluA2) (C-terminal PDZ site) to glutamate receptor interacting protein (GRIP), AMPA receptor binding protein (ABP), and C-kinase interacting protein (PICK1). pep2-SVKI increases the amplitude of AMPA receptor-mediated currents and blocks long-term depression (LTD). pep2-SVKI can be used to study neurological diseases.

FP802 is an orally active potent TwinF interface inhibitor that disrupts and detoxifies the NMDAR/TRPM4 death complex. FP802 exerts powerful neuroprotective effects in the 5xFAD mouse model of Alzheimer’s disease (AD) by preventing cognitive decline, preserving neuronal structural integrity, reducing amyloid-β plaque formation, and mitigating mitochondrial pathology. FP802 stops loss of motor neurons, reduces serum neurofilament light chain (NfL) levels, improves motor performance, and extends life in a mouse model of amyotrophic lateral sclerosis (ALS). FP802 can be used for AD and ALS research.

DAAO inhibitor-1 is a potent D-amino acid oxidase (DAAO) inhibitor with an IC₅₀ of 0.12 μM.