iGluR Inhibitor

Evans Blue (Direct Blue 53) is a potent inhibitor of L-glutamate uptake via the membrane bound excitatory amino acid transporter (EAAT). Evans Blue is a L-glutamate and kainate receptor-mediated currents inhibitor. Evans Blue has a strong affinity towards serum albumin, making it a high molecular weight protein tracer. Evans Blue is also used to study BBB (blood-brain barrier) permeability.

GluN1 (356-385) is a polypeptide targeting NMDAR GluN1. GluN1 (356-385) induces the production of autoantibodies, which reduce the density of cell surface NMDAR clusters, impair long-term potentiation, and decrease NMDAR-mediated Ca²⁺ influx. As an immunogen, GluN1 (356-385) induces symptoms similar to anti-NMDAR encephalitis, including memory loss, in mice. GluN1 (356-385) can be used to establish a mouse model that mimics the pathogenesis of anti-NMDAR encephalitis. GluN1 (356-385) is applicable to research related to anti-NMDAR encephalitis.

Bupivacaine liposome is a liposome-encapsulated form of Bupivacaine (HY-B0405). Bupivacaine is an NMDA receptor inhibitor. During the action potential, Bupivacaine blocks sodium channels, thereby inhibiting the generation and conduction of nerve impulses induced by painful stimuli. Bupivacaine liposome reduces the release rate of Bupivacaine, thus achieving a long-lasting pain relief effect.

GluN1 (359-378) is an anti-N-methyl-D-aspartate receptor (NMDAR) peptide. GluN1 (359-378) can cross the blood-brain barrier. GluN1 (359-378) can be used to study anti-NMDAR encephalitis therapy targeting the immune system.

Phenylpiracetam (Carphedon) is a positive allosteric modulator of nicotinic acetylcholine receptors (nAChR) with an IC₅₀ of 5.86 μM. Phenylpiracetam is applicable to studies on scopolamine (Scopolamine) (HY-N0296)-induced amnesia, depression and immune stress.

SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride 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 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders.

LQFM215 is a proline transporter (PROT) inhibitor. LQFM215 inhibits proline transport by competitively binding to the active site of PROT. LQFM215 effectively reduces hyperlocomotion and enhances social interaction.

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

IEM-1460 blocks both AMPA and NMDA glutamate receptor with anticonvulsant effect in vivo.

FSC231 is a PSD‐95/DLG/ZO‐1 (PDZ) domain inhibitor of PICK1. FSC231 has analgesic effects.

Gly-Pro-Glu is a neuroactive peptide with a potent action on acetylcholine release. Gly-Pro-Glu is the N-terminal tripeptide of insulin-like growth factor-I. Gly-Pro-Glu inhibits glutamate binds to N-methyl-D-aspartate (NMDA) receptor with an IC₅₀ value of 14.7 μM. Gly-Pro-Glu can be used for the research of neuroprotection .

Ganglioside GM1 (bovine) ammonium is a type of glycosphingolipid, mainly found on the cell membranes of the central nervous system of vertebrates. Ganglioside GM1 (bovine) ammonium exerts neuroprotective effects by reducing excessive activation of NMDAR, activating TrkA and ERK1/2, and inhibiting oxidative stress and cell apoptosis and autophagy. Ganglioside GM1 (bovine) ammonium can be used in the research of diseases such as traumatic brain injury, Parkinson's disease, Alzheimer's disease, and Huntington's disease.

DQP-997-74 (compound 2i) is a selective negative allosteric modulator of N-methyl-d-aspartate receptor (NMDAR), specifically targeting GluN2C/D (IC₅₀: 0.069 μM and 0.035 μM), with blood-brain barrier penetrability. Where DQP refers to dihydroquinoline-pyrazoline. DQP-997-74 acts synergistically with the agonist glutamate to exhibit time-dependent enhanced potency in inhibiting hypersynchronous activity driven by high-frequency excitatory synaptic transmission. DQP-997-74 reduces the number of epileptogenesis in a murine model of tuberous sclerosis complex (TSC)-induced epilepsy. DQP-997-74 can be used for research on NMDAR-related neurological diseases.

Neboglamine (CR-2249, XY-2401) hydrochloride is an orally active NMDA receptor glycine site positive modulator that can be used in schizophrenia research.

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.

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.

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.