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Results for "

AMPA-R

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Amino Acid Derivatives (2) Autophagy (1) Dopamine Receptor (1) Endogenous Metabolite (2) Glucocorticoid Receptor (2) iGluR (27) Lipoxygenase (1) NADPH Oxidase (1) PKC (1) Reference Standards (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (1) Endocrinology (2) Inflammation/Immunology (4) Neurological Disease (30)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B1618

Corticosterone 60+ Cited Publications 17-Deoxycortisol; 11β,21-Dihydroxyprogesterone; Kendall's compound B	Glucocorticoid Receptor Endogenous Metabolite iGluR	Neurological Disease Inflammation/Immunology Endocrinology
Corticosterone (17-Deoxycortisol) is an orally active and adrenal cortex-produced glucocorticoid, which plays an important role in regulating neuronal functions of the limbic system (including hippocampus, prefrontal cortex, and amygdala). Corticosterone increases the Rab-mediated *AMPAR* membrane traffic via SGK-induced phosphorylation of GDI. Corticosterone also interferes with the maturation of dendritic cells and shows a good immunosuppressive effect .

HY-115864

Osavampator TAK-653; NBI-1065845	iGluR Lipoxygenase	Neurological Disease
Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca2+ influx in hGluA1i CHO cells (EC₅₀ = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders .

HY-111751

JNJ-61432059 1 Publications Verification	iGluR	Neurological Disease
JNJ-61432059 is a blood-brain barrier-permeable, orally active TARP γ-8-associated AMPAR modulator with anticonvulsant activity. JNJ-61432059 negatively regulates GluA1 and positively modulates GluA2-containing *AMPAR*s. JNJ-61432059 exerts potent protective effects in rodent epilepsy models. JNJ-61432059 is applicable for epilepsy-related research .

HY-12505

CX546 5 Publications Verification	iGluR Autophagy	Neurological Disease
CX546 is a first-generation and selective benzamide-type positive *AMPAR* modulator. CX546 is a prototypical ampakine agent and has antipsychotic effects .

HY-B1618R

Corticosterone (Standard) 60+ Cited Publications 17-Deoxycortisol(Standard); 11β,21-Dihydroxyprogesterone(Standard); Kendall's compound B (Standard)	Reference Standards Glucocorticoid Receptor Endogenous Metabolite iGluR	Neurological Disease Inflammation/Immunology Endocrinology
Corticosterone (Standard) is the analytical standard of Corticosterone. This product is intended for research and analytical applications. Corticosterone (17-Deoxycortisol) is an orally active and adrenal cortex-produced glucocorticoid, which plays an important role in regulating neuronal functions of the limbic system (including hippocampus, prefrontal cortex, and amygdala). Corticosterone increases the Rab-mediated *AMPAR* membrane traffic via SGK-induced phosphorylation of GDI. Corticosterone also interferes with the maturation of dendritic cells and shows a good immunosuppressive effect .

HY-171844

CX1739	iGluR	Neurological Disease Inflammation/Immunology
CX1739 is an orally active, blood-brain barrier permeable, low-efficacy AMPA-glutamate receptor (AMPAR) potentiator. CX1739 enhances excitatory neurotransmission by potentiating glutamate-induced excitatory currents and promoting in vivo long-term potentiation. CX1739 eliminates amphetamine-induced locomotor activity, reverses opioid-, pentobarbital- and ethanol-induced respiratory depression, and exerts pro-cognitive effects in animals. CX1739 impairs motor function recovery and increases the risk of post-injury complications. CX1739 can be used in research related to attention-deficit/hyperactivity disorder, dementia, respiratory depression and spinal cord injury .

HY-122742

HBT1	iGluR	Neurological Disease
HBT1 is an effective AMPA receptor *AMPA-R* potentiator. HBT1 specifically binds to the ligand-binding domain (LBD) of AMPAR and enhances receptor activity only when AMPA is present., HBT1 has almost no agonistic effect (i.e., reaching the optimal concentration, and then the efficacy decreases as the concentration continues to increase) compared with traditional AMPA-R potentiator, avoiding the bell-shaped reaction of brain-derived neurotrophic factor (BDNF) production in primary neurons. HBT1 can be applicable to a wider range of neurological and psychiatric diseases (such as depression, Alzheimer's disease, etc.) .

HY-104020A

Philanthotoxin 74 dihydrochloride PhTx 74 dihydrochloride	iGluR	Neurological Disease
Philanthotoxin 74 dihydrochloride (PhTx 74) is an *AMPAR* antagonist; inhibits GluR3 and GluR1 with IC₅₀s of 263 and 296 nM, respectively .

HY-P2259

TAT-GluA2 3Y 2 Publications Verification	iGluR	Neurological Disease
TAT-GluA2 3Y, an interference peptide, blocks long-term depression (LTD) at glutamatergic synapses by disrupting the endocytosis of *AMPAR*. TAT-GluA2 3Y can alleviate Pentobarbital-induced spatial memory deficits and synaptic depression .

HY-12503

CFM-2 1 Publications Verification	iGluR	Neurological Disease Cancer
CFM-2 is a potent and selective non-competitive *AMPAR* antagonist . CFM-2 possesses anticonvulsant activity in various models of seizures .

HY-177873

AMPA receptor modulator-10	iGluR	Neurological Disease
AMPA receptor modulator-10 (Compound 9a) is an orally active AMPA receptor (AMPAR) positive allosteric modulator. AMPA receptor modulator-10 exhibits potent activity (pEC₅₀ = 5.0) on the GluA2 subtype of AMPAR, significantly enhancing glutamate-induced calcium influx and current responses. AMPA receptor modulator-10 can reverse the memory impairment induced by Scopolamine (HY-N0296) and enhance cognitive function. AMPA receptor modulator-10 can be used for the research of neurological disease, such as schizophrenia .

HY-16713A

(S)-(-)-5-Fluorowillardiine hydrochloride (5S)-Fluorowillardiine hydrochloride; (S)-5-Fluorowillardiine hydrochloride	iGluR	Neurological Disease
(S)-(-)-5-Fluorowillardiine hydrochloride is a potent and specific AMPAR agonist.

HY-100547

IEM-1754	iGluR	Neurological Disease
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 .

HY-P1386

D15 Dynamin II (828–842)	iGluR	Neurological Disease
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 .

HY-117176

KRP-199	iGluR	Neurological Disease
KRP-199 (compound 14h) is an α-amino-3-hydroxy-5-methylisoxazolepropionic acid receptor (AMPA-R) antagonist (K_i=16 nM) with high potency and selectivity for *AMPA-R* in vitro and good neuroprotective effects in vivo. KRP-199 can be used in the study of neurodegenerative diseases .

HY-114576

Nooglutil Nooglutyl; ONK-10	iGluR Dopamine Receptor	Neurological Disease
Nooglutil (Nooglutyl; ONK-10) is a positive modulator of AMPA-type glutamate receptors (AMPARs). Nooglutil also regulates dopamine D2 receptor function to exert anxiolytic effects. Nooglutil is promising for research of neurodegenerative disorders (e.g., Alzheimer’s disease) .

HY-16713

(S)-(-)-5-Fluorowillardiine (5S)-Fluorowillardiine; (S)-5-Fluorowillardiine	iGluR	Neurological Disease
(S)-(-)-5-Fluorowillardiine is a potent and specific AMPAR agonist.

HY-183101

AMPAR modulator-12	iGluR NADPH Oxidase	Neurological Disease
AMPAR modulator-12 is a blood-brain barrier-permeable *AMPAR* positive allosteric modulator. AMPAR modulator-12 reduces NOX-1 expression, enhances *AMPAR*-mediated currents, promotes excitatory postsynaptic transmission and restores *AMPAR* function. AMPAR modulator-12 enhances excitatory and inhibitory synaptic transmission, reduces burst firing in the lateral habenula after withdrawal, and produces rapid and sustained antidepressant-like effects. AMPAR modulator-12 is applicable for the research of depression .

HY-104020B

Philanthotoxin 74 diTFA PhTx 74 diTFA	iGluR	Neurological Disease
Philanthotoxin 74 (PhTx 74) diTFA is an *AMPAR* antagonist; inhibits GluR3 and GluR1 with IC₅₀s of 263 and 296 nM, respectively .

HY-P1054

pep2-EVKI YNVYGIEEVKI	PKC	Neurological Disease
pep2-EVKI (YNVYGIEEVKI) is an inhibitor peptide that selectively blocks PICK1 interactions, caused the opposite effects on synaptic AMPAR function to PICK1 expression .

HY-107519

(R)-3,4-DCPG	iGluR	Neurological Disease
(R)-3,4-DCPG is an *AMPA* and NMDA antagonist with a K_d of 77 μM for AMPA. (R)-3,4-DCPG complete antagonizes the NMDA-induced depolarization at a concentration of 500 μM. (R)-3,4-DCPG exhibits a weak antagonistic effect on kainate-induced depolarizations .

HY-178153

BPAM363	iGluR	Neurological Disease
BPAM363 is an orally active, selective positive allosteric modulator (PAM) of *AMPARs* with blood-brain barrier penetration. BPAM363 selectively potentiates *AMPAR* activity in human and rat models, with an EC_2x value of 0.96 μM in rat embryonic cortex primary neurons. BPAM363 upregulates BDNF protein expression in rat primary cortical neuronal cultures. BPAM363 enhances AMPA-mediated excitatory postsynaptic responses in rat and mice. BPAM363 can be used for the study of cognitive disorders .

HY-12503R

CFM-2 (Standard)	iGluR	Neurological Disease Cancer
CFM-2 (Standard) is the analytical standard of CFM-2. This product is intended for research and analytical applications. CFM-2 is a potent and selective non-competitive AMPAR antagonist . CFM-2 possesses anticonvulsant activity in various models of seizures .

HY-112699

AMPA receptor modulator-1	iGluR	Neurological Disease
AMPA receptor modulator-1 is a potent, orally active and selective AMPAR regulatory protein TARP γ-8 negative modulator with a pIC₅₀ of 9.7, more selective over GluA1/γ-2 (pIC₅₀=5) .

HY-P4106A

Tat-GluR23Y, scrambled TFA 1 Publications Verification	Amino Acid Derivatives	Neurological Disease
Tat-GluR23Y, scrambled TFA is the scrambled peptide of Tat-GluR23Y (HY-P2259). Tat-GluR23Y is a synthetic peptide containing tyrosine residues that inhibit AMPAR endocytosis and is effective in the research of long-term depression (LTD) .

HY-P4106

Tat-GluR23Y, scrambled	Amino Acid Derivatives	Neurological Disease
Tat-GluR23Y, scrambled is the scrambled peptide of Tat-GluR23Y (HY-P2259). Tat-GluR23Y is a synthetic peptide containing tyrosine residues that inhibit AMPAR endocytosis and is effective in the research of long-term depression (LTD) .

HY-149975

AMPA receptor modulator-4	iGluR	Neurological Disease
AMPA receptor modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), is an orally active positive allosteric modulator of the AMPA receptors (AMPAR PAMs). AMPA receptor modulator-4 can cross the blood-brain barrier. AMPA receptor modulator-4 increases the cognition performance and improves working memory performance in mice .

HY-186183

Normethyl-ZCAN262	iGluR	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Normethyl-ZCAN262 (Normethyl-262) is a blood-brain barrier-permeable selective *GluR2/AMPAR* receptor modulator. Normethyl-ZCAN262 inhibits *AMPA*-mediated neurotoxicity, the formation of the GAPDH-GluR2 complex, and *GluR2/AMPAR* neurotoxicity. Normethyl-ZCAN262 enables in vivo imaging of brain *AMPA* receptors and is used in research related to multiple sclerosis, amyotrophic lateral sclerosis, neuroinflammation, stroke, epilepsy, Parkinson's disease, Alzheimer's disease, dementia, and Huntington's disease .

HY-182631

CX1763	iGluR	Neurological Disease
CX1763 is an *AMPAR* allosteric modulator. CX1763 allosterically potentiates glutamate-evoked currents, accelerates channel opening, and increases the surface levels of *AMPAR* containing Glur2 (R). CX1763 enhances synaptic transmission in the rat hippocampus. CX1763 improves attention in rats and attenuates amphetamine-induced hyperactivity in mice. CX1763 can be used in studies related to attention deficit hyperactivity disorder and opioid-induced respiratory depression .

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 .

Cat. No.	Product Name

HY-L013

Neuronal Signaling Compound Library	3,747 compounds
Neuronal Signaling is involved in the regulation of the mechanisms of the central nervous system (CNS) such as its structure, function, genetics and physiology as well as how this can be applied to understand diseases of the nervous system. Every information processing system in the CNS is composed of neurons and glia, neurons have evolved unique capabilities for intracellular signaling (communication within the cell) and intercellular signaling (communication between cells). G protein-coupled receptors (GPCRs), including 5-HT receptor, histamine receptor, opioid receptor, etc. are the largest class of sensory proteins and are important therapeutic targets in Neuronal Signaling. Besides, Notch signaling, such as β- and γ-secretase, also plays multiple roles in the development of the CNS including regulating neural stem cell (NSC) proliferation, survival, self-renewal and differentiation. GPCR dysfunction caused by receptor mutations and environmental challenges contributes to many neurological diseases. Notch signaling in neurons, glia, and NSCs is also involved in pathological changes that occur in disorders such as stroke, Alzheimer's disease and CNS tumors. Thus, targeting Neuronal Signaling, such as notch signaling and GPCRs, can be used as therapeutic interventions for several different CNS disorders. MCE designs a unique collection of 3,747 Neuronal Signaling-related compounds that act as a useful tool for the research of neuronal regulation and neuronal diseases.

Neuronal Signaling Compound Library

3,747 compounds

Neuronal Signaling is involved in the regulation of the mechanisms of the central nervous system (CNS) such as its structure, function, genetics and physiology as well as how this can be applied to understand diseases of the nervous system. Every information processing system in the CNS is composed of neurons and glia, neurons have evolved unique capabilities for intracellular signaling (communication within the cell) and intercellular signaling (communication between cells). G protein-coupled receptors (GPCRs), including 5-HT receptor, histamine receptor, opioid receptor, etc. are the largest class of sensory proteins and are important therapeutic targets in Neuronal Signaling. Besides, Notch signaling, such as β- and γ-secretase, also plays multiple roles in the development of the CNS including regulating neural stem cell (NSC) proliferation, survival, self-renewal and differentiation. GPCR dysfunction caused by receptor mutations and environmental challenges contributes to many neurological diseases. Notch signaling in neurons, glia, and NSCs is also involved in pathological changes that occur in disorders such as stroke, Alzheimer's disease and CNS tumors. Thus, targeting Neuronal Signaling, such as notch signaling and GPCRs, can be used as therapeutic interventions for several different CNS disorders.

MCE designs a unique collection of 3,747 Neuronal Signaling-related compounds that act as a useful tool for the research of neuronal regulation and neuronal diseases.

Cat. No.	Product Name	Target	Research Area