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Results for "

NMDAR inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (2) Amyloid-β (3) Apoptosis (5) ATP Citrate Lyase (1) Autophagy (4) Bacterial (1) Calcium Channel (1) CaMK (1) Cholinesterase (ChE) (4) Dopamine Receptor (1) Drug Derivative (1) ERK (4) Free Fatty Acid Receptor (1) Glutathione S-transferase (1) HDAC (1) iGluR (33) mTOR (5) NO Synthase (2) Opioid Receptor (1) P-glycoprotein (1) p38 MAPK (1) Phytohormone (1) PI3K (2) Reactive Oxygen Species (ROS) (1) Reference Standards (4) Serotonin Transporter (3) Tau Protein (3) Trk Receptor (2) TRP Channel (6)
By Research Areas:	Cancer (5) Cardiovascular Disease (3) Infection (1) Inflammation/Immunology (5) Metabolic Disease (5) Neurological Disease (36)

By Targets:

Akt (2)

Amyloid-β (3)

Apoptosis (5)

ATP Citrate Lyase (1)

Autophagy (4)

Bacterial (1)

Calcium Channel (1)

CaMK (1)

Cholinesterase (ChE) (4)

Dopamine Receptor (1)

Drug Derivative (1)

ERK (4)

Free Fatty Acid Receptor (1)

Glutathione S-transferase (1)

HDAC (1)

iGluR (33)

mTOR (5)

NO Synthase (2)

Opioid Receptor (1)

P-glycoprotein (1)

p38 MAPK (1)

Phytohormone (1)

PI3K (2)

Reactive Oxygen Species (ROS) (1)

Reference Standards (4)

Serotonin Transporter (3)

Tau Protein (3)

Trk Receptor (2)

TRP Channel (6)

By Research Areas:

Cancer (5)

Cardiovascular Disease (3)

Infection (1)

Inflammation/Immunology (5)

Metabolic Disease (5)

Neurological Disease (36)

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B1488

Tacrine hydrochloride Maximum Cited Publications 8 Publications Verification	Cholinesterase (ChE) iGluR	Neurological Disease
Tacrine hydrochloride is a potent brain-penetrant inhibitor of both AChE and BChE, with IC₅₀s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a *NMDAR* inhibitor, with an IC₅₀ of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease .

HY-N10546

Ganglioside GM1	iGluR Trk Receptor ERK Apoptosis Autophagy	Neurological Disease
Ganglioside GM1 is a type of glycosphingolipid, mainly found on the cell membranes of the central nervous system of vertebrates. Ganglioside GM1 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 can be used in the research of diseases such as traumatic brain injury, Parkinson's disease, Alzheimer's disease, and Huntington's disease .

HY-N0837

Veratramine 1 Publications Verification NSC17821; NSC23880	PI3K Akt mTOR Autophagy Apoptosis	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to *NMDAR* and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .

HY-P0117

Tat-NR2B9c 5+ Cited Publications Tat-NR2Bct; NA-1	iGluR NO Synthase	Neurological Disease
Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC₅₀ values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC₅₀ values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy .

HY-139142

Simufilam 1 Publications Verification PTI-125	mTOR iGluR Amyloid-β Tau Protein	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Simufilam (PTI-125) is an orally active FLNA modulator. Simufilam restores *NMDAR* signaling and Arc expression. Simufilam inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ₄₂-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam can be used for research of Alzheimer's disease .

HY-P11117

TAT-EE3	TRP Channel iGluR Calcium Channel	Neurological Disease
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 .

HY-N1916

Coniferyl ferulate 1 Publications Verification	Glutathione S-transferase P-glycoprotein Apoptosis iGluR CaMK p38 MAPK Reactive Oxygen Species (ROS) Bacterial	Infection Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
Coniferyl ferulate is an orally active phenolic acid compound. Coniferyl ferulate is a potent inhibitor of glutathione S-transferase (GST) (IC₅₀ = 0.3 μM), which downregulates P-gp expression, induces apoptosis in B-MD-C1 (ADR+/+) cells, and reverses multidrug resistance. Coniferyl ferulate blocks the *NMDAR/NR2B-CaMKII-MAPKs* signaling pathway, inhibits ROS production and mitochondrial apoptosis, while reshapes the intestinal microbiota and microbial metabolism, ameliorates colonic inflammation and alleviates depressive symptoms in mice. Coniferyl ferulate can alleviate the toxicity of xylene to hematopoietic stem and progenitor cells by targeting Mgst2. Coniferyl ferulate exhibits antibacterial activity against the Gram-positive Bacillus subtilis and Staphylococcus aureus .

HY-111973

Phaseic acid	Phytohormone iGluR	Neurological Disease
Phaseic acid is a Abscisic acid terpenoid catabolite that can able to activate a subset of Abscisic acid repectors. Phaseic acid is a plant hormone associated with photosynthesis arrest and abscission. Phaseic acid is the antagonist for NMDA-type glutamate receptor (NMDAR) that inhibits NMDAR currents with an IC₅₀ of 34.37 μM. Phaseic acid reduces intracellular calcium influx, and exhibits neuroprotective effect .

HY-100457

IC87201 2 Publications Verification	iGluR	Neurological Disease
IC87201, an inhibitor of PSD95-nNOS protein-protein interactions, suppresses *NMDAR*-dependent NO and cGMP formation.

HY-139192

Brophenexin 3 Publications Verification NMDAR/TRPM4-IN-2	iGluR TRP Channel ERK	Neurological Disease
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 .

HY-139142B

Simufilam hydrochloride 1 Publications Verification PTI-125 hydrochloride	mTOR iGluR Amyloid-β Tau Protein	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Simufilam hydrochloride (PTI-125 hydrochloride) is an orally active FLNA modulator. Simufilam hydrochloride restores *NMDAR* signaling and Arc expression. Simufilam hydrochloride inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ₄₂-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam hydrochloride can be used for research of Alzheimer's disease .

HY-P991611

ART5803	iGluR	Inflammation/Immunology
ART5803 is a humanized IgG1 monoclonal antibody inhibitor targeting *NMDAR. ART5803 binds to the N-terminal domain (NTD) of the NMDAR* GluN1 subunit (GluN1-NTD) with a high affinity. ART5803 blocks NMDAR internalization induced by pathogenic autoantibodies and restores cell-surface NMDAR expression and functions. ART5803 reverses behavioral abnormalities and NMDAR expression in marmoset disease models. ABT-147 can be used to study anti-NMDAR encephalitis .

HY-172261

YY-23	iGluR	Neurological Disease
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 .

HY-155811

DQP-997-74	iGluR	Neurological 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 .

HY-P0117A

Tat-NR2B9c TFA 5+ Cited Publications Tat-NR2Bct TFA; NA-1 TFA	iGluR NO Synthase	Neurological Disease
Tat-NR2B9c TFA (Tat-NR2Bct TFA) is a postsynaptic density-95 (PSD-95) inhibitor, with EC₅₀ values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c TFA disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC₅₀ values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c TFA also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy .

HY-139192A

Brophenexin free base 3 Publications Verification NMDAR/TRPM4-IN-2 free base	iGluR TRP Channel ERK	Neurological Disease
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 .

HY-170790

HZS60	TRP Channel	Neurological Disease
HZS60 is a *NMDAR/TRPM4* inhibitor with brain permeability that can improve cerebral ischemia. HZS60 has significant neuroprotective effects on primary neuronal ischemic damage caused by NMDA and oxygen-glucose deprivation/reoxygenation. HZS60 exhibits good pharmacokinetic characteristics and can inhibit cerebral ischemia-reperfusion injury. HZS60 can be used as a potential inhibitor of ischemic stroke .

HY-N0837R

Veratramine (Standard) NSC17821 (Standard); NSC23880 (Standard)	Reference Standards PI3K Akt mTOR Autophagy Apoptosis	Neurological Disease Metabolic Disease Cancer
Veratramine (NSC17821; NSC23880) (Standard) is the analytical standard of Veratramine (HY-N0837). This product is intended for research and analytical applications. Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to *NMDAR* and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .

HY-139142A

Simufilam dihydrochloride PTI-125 dihydrochloride	Tau Protein Amyloid-β mTOR iGluR	Neurological Disease
Simufilam dihydrochloride (PTI-125 dihydrochloride) is an orally active FLNA modulator. Simufilam dihydrochloride restores *NMDAR* signaling and Arc expression. Simufilam dihydrochloride inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ₄₂-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam dihydrochloride can be used for research of Alzheimer's disease .

HY-N10546A

Ganglioside GM1 (bovine) ammonium	iGluR Trk Receptor ERK Apoptosis Autophagy	Neurological Disease
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 .

HY-W611371

FP802	TRP Channel iGluR	Neurological Disease
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 .

HY-172419

Blixeprodil GM-1020	iGluR	Neurological Disease
Blixeprodil (GM-1020) is the orally active antagonist for NMDA receptor with an affinity of K_i=3.25 µM in rat cortical tissue. Blixeprodil inhibits NR1/2A-NMDAR-mediated currents in HEK293 cell with IC₅₀ of 1.192 µM. Blixeprodil exhibits antidepressant in rats models. Blixeprodil can cross blood-brain barrier .

HY-173016

HINT1-IN-1	Opioid Receptor	Neurological Disease
HINT1-IN-1 (Compound 8) is the inhibitor for histidine triad nucleotide-binding protein 1 (HINT1) with a K_i of 1.14 μM. HINT1-IN-1 affects the cross-regulation between μ-opioid receptor (MOR) and NMDA receptor (NMDAR). HINT1-IN-1 enhances the analgesic effect of morphine without causing opioid tolerance and has independent analgesic effects in mouse model .

HY-W611371A

FP802 dihydrochloride	TRP Channel iGluR	Neurological Disease
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 .

HY-157476

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

HY-147873

NMDAR/HDAC-IN-1	iGluR HDAC	Neurological Disease
NMDAR/HDAC-IN-1 (Compound 9d) is a dual *NMDAR* and HDAC inhibitor with a K_i of 0.59 μM for NMDAR and IC₅₀ values of 2.67, 8.00, 2.21, 0.18 and 0.62 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8, respectively. NMDAR/HDAC-IN-1 efficiently penetrates the blood brain barrier .

HY-106397

Delucemine NPS-1506	Serotonin Transporter iGluR	Neurological Disease
Delucemine is a selective serotonin reuptake inhibitor (SSRI) and NMDAR antagonist. Delucemine can be used as an antidepressant .

HY-106397A

Delucemine hydrochloride NPS-1506 hydrochloride	Serotonin Transporter iGluR	Neurological Disease
Delucemine hydrochloride is a selective serotonin reuptake inhibitor (SSRI) and NMDAR antagonist. Delucemine hydrochloride can be used as an antidepressant .

HY-172884

MDAR-IN-1	Cholinesterase (ChE) iGluR	Neurological Disease
MDAR IN-1 (Compound 5m) is a brain-penetrant inhibitor of acetylcholinesterase (AChE) and antagonist of the GluN1/GluN2B subtype of *NMDAR* receptor. MDAR IN-1 effectively inhibits AChE activity, enhances cholinergic neurotransmission, and blocks NMDAR, reducing excitatory neurotoxicity. MDAR IN-1 is promising for research of Alzheimer's disease .

HY-P1123R

MEDICA16 (Standard)	Reference Standards ATP Citrate Lyase Free Fatty Acid Receptor	Metabolic Disease
Tacrine (hydrochloride) (Standard) is the analytical standard of Tacrine (hydrochloride). This product is intended for research and analytical applications. Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease .

HY-B1488R

Tacrine hydrochloride (Standard)	Reference Standards Cholinesterase (ChE) iGluR	Neurological Disease
Tacrine (hydrochloride) (Standard) is the analytical standard of Tacrine (hydrochloride). This product is intended for research and analytical applications. Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease .

HY-170945

Antidepressant agent 9	iGluR Serotonin Transporter	Neurological Disease
Antidepressant agent 9 (Compound 24) is an orally active and BBB-penetrable *NMDAR* and SERT inhibitor with IC₅₀ values of 3.50 μM and 1044 nM, respectively. Antidepressant agent 9 has good metabolic stability and plasma exposure. Antidepressant agent 9 can exert antidepressant-like activity in the mouse forced swim test .

HY-181828

SePP	iGluR Dopamine Receptor	Neurological Disease
SePP is a blood-brain barrier-permeable *NMDAR* antagonist and dopamine/norepinephrine reuptake inhibitor, with a K_i of 28.7 nM for rat *NMDAR*. SePP exerts anticonvulsant effects. SePP can be used in research related to fragile X syndrome .

HY-119781

Kaitocephalin PF1191	iGluR	Neurological Disease
Kaitocephalin (PF1191) is an ionotropic glutamate receptor (NMDAR) antagonist with K_i values of 7.8, 590, and 14000 nM for *NMDAR, AMPAR, and KAR, respectively. Kaitocephalin protects neurons by inhibiting* excitotoxicity, exhibiting neuroprotective effects. Kaitocephalin can be used in research on neurological diseases such as Alzheimer's disease .

HY-185027

Memagal	Cholinesterase (ChE) iGluR	Neurological Disease
Memagal is an AchE inhibitor (IC₅₀ = 1.16 nM) and a *NMDAR* antagonist (K_i = 4.6 μM). Memagal inhibits the neurotoxicity induced by NMDA (HY-17551), with its IC₅₀ value being 0.28 nM. Memagal can be used for research on Alzheimer's disease .

HY-182068

NFI23	iGluR	Cardiovascular Disease Neurological Disease
NFI23 is a blood-brain barrier-penetrant *GluN2B-NMDAR* inhibitor, with an IC₅₀ of 1.31 μM and a K_i of 5.98 nM against GluN2B-NMDAR. NFI23 reduces NMDA-induced Ca ²⁺ influx and ROS production, maintains mitochondrial membrane potential, inhibits neuronal apoptosis, and restores the expression of p-ERK1/2. NFI23 exerts neuroprotective effects against NMDA-induced cytotoxicity and in the rat middle cerebral artery occlusion (MCAO) model. NFI23 can be used for the research of ischemic stroke .

HY-100457R

IC87201 (Standard)	iGluR Reference Standards	Neurological Disease
IC87201 (Standard) is the analytical standard of IC87201 (HY-100457). This product is intended for research and analytical applications. IC87201, an inhibitor of PSD95-nNOS protein-protein interactions, suppresses NMDAR-dependent NO and cGMP formation.

HY-180370

Nitromemantine NitroSynapsin; YQW-036; NMI-6979	iGluR Drug Derivative	Cardiovascular Disease Neurological Disease
Nitromemantine (NitroSynapsin) is a nitrate derivative of Memantine (HY-B0591) and is a dual-functional *NMDAR* antagonist. Nitromemantine exhibits significant efficacy in rodent models of cerebral infarction through a dual mechanism of blocking channels and regulating receptors via NO/redox regulation. Nitromemantine can target ischemic neurons under hypoxic conditions and enhance its activity. Nitromemantine inhibits the current induced by NMDA, with its IC₅₀ being 2.4 μM. Nitromemantine can be used for the study of cerebral ischemic stroke .

Cat. No.	Product Name	Target	Research Area