Catalog No.
Product Name
Application
Product Information
Citations
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mGlu1 receptors modulator
Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors. -
mGluR agonist
L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92±0.03, 4.6±0.2, 3.9±0.2, 2.7±0.2, 4.0±0.2, and 3.94±0.08 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively. -
mGlu5 modulator
JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC50 of 260 nM. -
metabotropic receptor agonist
trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons. -
group III mGluR receptors agonist
O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2. -
mGlu5 receptor antagonist
Mavoglurant is a structurally novel, non-competitive mGlu5 receptor antagonist, has an IC50 of 30 nM in a functional assay with human mGluR5. -
mGlu5 negative allosteric modulator
Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM. -
mGluR4 modulator
Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) , with an EC50 of 79 nM. Antiparkinsonian effect. -
mGlu5 receptor antagonist
Mavoglurant (racemate) is the racemate of mavoglurant. Mavoglurant is a novel, non-competitive mGlu5 receptor antagonist. -
mGluR5 positive allosteric modulator
(R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC50 of 168 nM for potentiation . -
mGlu5 receptor antagonist
Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM. -
partial mGluR4 agonist
(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM. -
mGluR5 agonist
CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. -
mGluR II agonist
Xanthurenic acid is a putative endogenous Group II metabotropic glutamate receptor agonist, on sensory transmission in the thalamus. -
mGluR5 allosteric modulator
CDPPB is a selective, orally active allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). It enhances AKT and ERK1/2 signaling and upregulates BDNF mRNA expression. CDPPB also inhibits caspase-3 activation and mitigates mitochondrial dysfunction, demonstrating therapeutic potential in improving cognitive impairment, depression, and Huntington’s disease. -
PKA/ERK/CREB activator
4′-Demethylnobiletin is a bioactive metabolite derived from citrus polymethoxyflavones, known for its neuroprotective and cognition-enhancing properties. It activates the PKA/ERK/CREB signaling pathway and enhances CRE (cAMP response element)-mediated transcription in hippocampal neurons, processes essential for synaptic plasticity and memory formation. Additionally, 4′-Demethylnobiletin reverses memory impairment caused by NMDA receptor antagonism by stimulating ERK signaling, highlighting its therapeutic potential for neurodegenerative diseases and cognitive dysfunction. -
NMDAR/TRPM4 inhibitor
Brophenexin (compound 8) is a potent inhibitor of the interaction interface between NMDA receptors (NMDAR) and TRPM4 channels, exhibiting significant neuroprotective activity. It prevents NMDA-induced excitotoxicity, including cell death and mitochondrial dysfunction in hippocampal neurons, with an IC₅₀ of 2.1 μM. In vivo, Brophenexin protects against brain damage in mice subjected to middle cerebral artery occlusion (MCAO) and preserves retinal ganglion cells from NMDA-induced degeneration. These findings support its potential as a therapeutic agent for neurodegenerative diseases and ischemic brain injury. -
Endogenous Glucocorticoids
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. -
L-glutamate Uptake Inhibitor
Evans Blue is a potent inhibitor of L-glutamate uptake through the membrane-bound excitatory amino acid transporter (EAAT). This compound effectively inhibits L-glutamate and kainate receptor-mediated currents, making it valuable for research into neurophysiological processes. Additionally, due to its strong affinity for serum albumin, Evans Blue serves as a high molecular weight protein tracer and is widely used to investigate blood-brain barrier (BBB) permeability. -
mGlu1 Antagonist
LY456236 free base is a selective, non-competitive antagonist of the metabotropic glutamate receptor 1 (mGlu1), showing an IC50 for phosphatidylinositol hydrolysis of 0.145 μM. Additionally, it inhibits epidermal growth factor receptor (EGFR) activity with an IC50 of 0.918 μM. This compound effectively blocks cell proliferation by targeting the MAPK signaling pathway, counteracting the anti-apoptotic effects of DHPG. LY456236 free base is a valuable tool for research into epilepsy and other neurological disorders. -
mGlu4 Agonist
Cinnabarinic acid primarily functions as an orthosteric agonist of the mGlu4 receptor, selectively engaging with residues within its glutamate binding pocket, and exhibiting no significant activity on other mGlu receptors. As an endogenous metabolite of the kynurenine pathway of tryptophan, cinnabarinic acid plays a role in cell apoptosis. This compound is valuable in research exploring mGlu4 receptor signaling and its implications in neurological disorders. -
mGlu1 Antagonist
LY456236 is a selective, non-competitive antagonist of the metabotropic glutamate receptor 1 (mGlu1), exhibiting an IC50 of 0.145 μM for the inhibition of phosphatidylinositol hydrolysis. Additionally, it demonstrates inhibitory activity against EGFR with an IC50 of 0.918 μM. By targeting the MAPK pathway, LY456236 effectively blocks cell proliferation and reverses the anti-apoptotic effects of DHPG. This reagent is suitable for investigations in epilepsy and related neurological research. -
mGluR5 Antagonist
Fenobam hydrate is a selective mGluR5 antagonist with an IC50 of 84 nM, capable of crossing the blood-brain barrier. It exhibits Kd values of 54 nM and 31 nM for rat and human recombinant mGlu5 receptors, respectively. Fenobam hydrate demonstrates anxiolytic properties, inhibits self-administration behavior in rodent models, and induces apoptosis in cancer cells. This compound is valuable for research in neurological disorders, cancer biology, and addiction studies. -
mGluR2 Negative Allosteric Modulator
mG2N001 is a negative allosteric modulator of the metabotropic glutamate receptor mGluR2, exhibiting an IC50 of 93 nM and a binding affinity (Ki) of 63 nM. This compound demonstrates significant biological activity by modulating glutamatergic signaling pathways, making it valuable for neurological research. Additionally, its radioisotope [11C]mG2N001 is suitable for PET imaging, providing high brain heterogeneity and penetration, allowing for selective accumulation in mGluR2-rich regions, which enhances imaging contrast in neurobiological studies. -
mGluR5 Antagonist
AZD-2066 hydrochloride is a selective antagonist of the metabotropic glutamate receptor 5 (mGluR5) with the ability to penetrate the blood-brain barrier. This compound activates the brain-derived neurotrophic factor (BDNF) and trkB signaling pathway, making it relevant for research into neuropathic pain, major depressive disorder, and gastroesophageal reflux disease. AZD-2066 hydrochloride serves as a valuable tool for investigating the therapeutic potential of mGluR5 modulation in these conditions. -
mGlu5 Receptor NAM
STX107 is a negative allosteric modulator (NAM) of the metabotropic glutamate 5 (mGlu5) receptor, exhibiting a pKi of 8.32. This compound effectively inhibits glutamate-induced calcium mobilization, inositol monophosphate (IP1) accumulation, and ERK1/2 phosphorylation. Additionally, STX107 prevents glutamate-induced mGlu5 internalization, making it a valuable tool for researching mGlu5 receptor signaling pathways and potential therapeutic applications for neurological disorders. -
mGlu5 Agonist
VU0424465 is a potent partial agonist and positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 5 (mGlu5), primarily targeting intracellular calcium (iCa2+) mobilization. With a Ki value of 11.8 nM, VU0424465 demonstrates high affinity at the MPEP allosteric binding site. This compound also facilitates the activation of pERK1/2 in cortical neurons, making it a valuable tool for research into neurological disorders and signaling pathways associated with mGlu5 activation. -
mGluR5 Negative Allosteric Modulator
VU0477573, a partial negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGluR5), demonstrates brain penetrance and engages in neuroprotective and anxiolytic activities. This compound is of significant interest in the research of neurological disorders, including Parkinson's disease, providing insights into potential therapeutic strategies targeting mGluR5. -
mGlu7 Modulator
VU6010608 is a negative allosteric modulator of the metabotropic glutamate receptor 7 (mGlu7), with an IC50 value of 0.76 μM, and effectively crosses the blood-brain barrier. This compound has been shown to inhibit long-term potentiation (LTP) of Schaffer-collateral CA1 synapses in mouse brain slices induced by high-frequency stimulation. VU6010608 is suitable for research applications investigating neurological disorders and the modulation of synaptic plasticity. -
mGluR1/5 Agonist
DHPG is a potent agonist for metabotropic glutamate receptors mGluR1 and mGluR5, with an EC50 of 60 nM for mGluR1. Its activation triggers the phospholipase C (PLC) signaling pathway, subsequently activating protein kinase C (PKC). DHPG is widely utilized in research to explore synaptic transmission, neuroplasticity, and the therapeutic potential of targeting mGluR signaling in neurological disorders. -
mGluRs Positive Allosteric Modulator
VU0422288 is a positive allosteric modulator of group III metabotropic glutamate receptors (mGluRs). It demonstrates inhibitory activity with EC50 values of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively, as established in calcium mobilization assays. This compound has potential applications in addressing deficits in contextual fear memory, social recognition, and apneas in models of Rett syndrome. -
mGluR1a Antagonist
LY367385 hydrochloride is a selective antagonist of the metabotropic glutamate receptor 1a (mGluR1a). It exhibits a potent inhibitory effect on quisqualate-induced phosphoinositide hydrolysis, with an IC50 value of 8.8 μM. This compound has demonstrated neuroprotective properties and exhibits anticonvulsant and antiepileptic effects, making it valuable for research in neurological disorders and related pharmacological studies.
