2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. mGluR

mGluR

Metabotropic glutamate receptors

mGluR

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mGluR (metabotropic glutamate receptor) is a type of glutamate receptor that are active through an indirect metabotropic process. They are members of thegroup C family of G-protein-coupled receptors, or GPCRs. Like all glutamate receptors, mGluRs bind with glutamate, an amino acid that functions as an excitatoryneurotransmitter. The mGluRs perform a variety of functions in the central and peripheral nervous systems: mGluRs are involved in learning, memory, anxiety, and the perception of pain. mGluRs are found in pre- and postsynaptic neurons in synapses of the hippocampus, cerebellum, and the cerebral cortex, as well as other parts of the brain and in peripheral tissues. Eight different types of mGluRs, labeled mGluR1 to mGluR8, are divided into groups I, II, and III. Receptor types are grouped based on receptor structure and physiological activity.

mGluR Isoform Specific Products:

mGluR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-107504
    VU0360172 hydrochloride
    		Agonist 98.94%
    VU0360172 hydrochloride is a potent and selective mGlu5 receptor positive allosteric modulator (PAM) with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 hydrochloride stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice.
    VU0360172 hydrochloride
  • HY-14554
    Pomaglumetad methionil anhydrous
    		Agonist
    Pomaglumetad methionil anhydrous (LY2140023) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. LY2140023 has the potential for schizophrenia research.
    Pomaglumetad methionil anhydrous
  • HY-120428
    VU0410425
    		Modulator
    VU0410425 is an mGlu1 negative allosteric modulator. VU0410425 exhibits potent inhibitory activity for rat mGlu1 with an IC50 value of 140 nM. VU0410425 can be used for the research of central nervous system disorders.
    VU0410425
  • HY-100617A
    (RS)-4CPG
    		Antagonist
    (RS)-4CPG ((RS)-4-Carboxyphenylglycine) is a type I metabotropic glutamate receptor antagonist with activity in blocking LTP induction. In mice lacking IP3R1, (RS)-4CPG (500μM) nearly blocked long-term potentiation (LTP) induced by type I metabotropic glutamate receptor activation, with LTP of 117.6±1.7% (n = 8) in IP3R1(-/-) mice and 116.9±1.8% (n = 5) in IP3R1(+/+) mice.
    (RS)-4CPG
  • HY-70059A
    (Rac)-LY341495
    		Control
    (Rac)-LY341495 is the isomers of LY341495 (HY-70059) can be used as control compounds in experiments. LY341495 is a metabotropic glutamate receptor (mGluR) antagonist with IC50s of 21 nM, 14 nM, 7.8 μM, 8.2 μM, 170 nM, 990 nM, 22 μM for mGlu2, mGlu3, mGlu1a, mGlu5a, mGlu8, mGlu7, and mGlu4 receptors, respectively.
    (Rac)-LY341495
  • HY-13206A
    MTEP
    		Antagonist
    MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research. MTEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MTEP
  • HY-103573
    VU 0360223
    		Modulator
    VU 0360223 is a potent metabotropic glutamate receptors (mGluR) negative allosteric modulator with an IC50 of 61 nM.
    VU 0360223
  • HY-124372
    JNJ-46356479
    		Modulator
    JNJ-46356479 is a selective and orally bioavailable mGlu2 receptor positive allosteric modulator (PAM), with the EC50 of 78 nM. JNJ-46356479 shows active in vivo.
    JNJ-46356479
  • HY-W714513
    VU0469650 hydrochloride
    		Modulator
    VU0469650 hydrochloride is a brain-penetrant negative allosteric modulator of metabotropic glutamate receptor 1 (mGluR1). VU0469650 hydrochloride inhibits glutamate-induced calcium flux in cells expressing human mGluR1 (IC50= 99 nM). VU0469650 hydrochloride is promising for research of central nervous system diseases such as anxiety, addiction, and epilepsy.
    VU0469650 hydrochloride
  • HY-126651
    Azotomycin
    		Antagonist
    Azotomycin is an L-glutamine analog. Azotomycin has antitumor activity.
    Azotomycin
  • HY-122487A
    Troriluzole hydrochloride
    		Modulator
    Troriluzole hydrochloride is a third-generation peptide precursor of Riluzole (HY-B0211) and is an orally active glutamate modulator. Troriluzole hydrochloride can reduce synaptic glutamate levels and enhance the uptake of synaptic glutamate. Troriluzole hydrochloride shows potential for treating Alzheimer's disease and Generalized Anxiety Disorder (GAD) .
    Troriluzole hydrochloride
  • HY-162860
    FO-4-15
    		Activator
    FO-4-15 is an mGluR1/CaMKIIα activator. FO-4-15 has a protective effect against H2O2 in human neuroblastoma (SH-SY5Y) cells. FO-4-15 can improve cognitive impairment in Alzheimer’s disease mice by activating the mGluR1/CaMKIIα pathway, and can reduce Aβ accumulation, hyperphosphorylated Tau, and synaptic damage.
    FO-4-15
  • HY-N0390S11
    L-Glutamine-2-13C
    		Agonist
    L-Glutamine-2-13C is the 13C-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells.
    L-Glutamine-2-<sup>13</sup>C
  • HY-170499
    VU6024578
    		Agonist
    VU6024578 (BI02982816) is a selective, orally active positive allosteric modulator (PAM) for metabotropic glutamate receptor (mGluR1), that activates human mGluR1 and rat mGluR1 with EC50 of 54 nM and 46 nM. VU6024578 exhibits antipsychotic activity in rats amphetamine-induced hyperactivity models and MK-801 (HY-15084B)-induced novel object recognition (NOR) models. VU6024578 is blood brain barrier penetrable.
    VU6024578
  • HY-19434A
    cis-ACPD
    		Agonist
    cis-ACPD is a potent agonist of NMDA receptor, with an IC50 of 3.3 μM. cis-ACPD is also a selective agonist of group II mGluR, with EC50s of 13 μM and 50 μM for mGluR2 and mGluR4, respectively.
    cis-ACPD
  • HY-14866
    Raseglurant
    		Modulator
    Raseglurant (ADX-10059) is a mGlu5 receptor negative allosteric modulator. Raseglurant is effective against migraine. Raseglurant reduces the Haloperidol (HY-14538)-induced catalepsy in mice.
    Raseglurant
  • HY-155088
    MK-8768
    		Inhibitor
    MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
    MK-8768
  • HY-W011417R
    Cinnabarinic acid (Standard)
    		Agonist
    Cinnabarinic acid (Standard) is the analytical standard of Cinnabarinic acid. This product is intended for research and analytical applications. Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis.
    Cinnabarinic acid (Standard)
  • HY-118238
    Remeglurant
    		Antagonist
    Remeglurant (MRZ-8456) acts as a selective, orally active and allosteric antagonist of the mGlu5 receptor, with an IC50 of 13 nM. Remeglurant (MRZ-8456) can be used in the research for dyskinesia in Parkinson’s disease (PD).
    Remeglurant
  • HY-119060
    FP0429
    		Agonist
    FP0429 is a full mGlu4 agonist and partial mGlu8 agonist with EC50 values of 48.3 μM and 56.2 μM, respectively.
    FP0429
Cat. No. Product Name / Synonyms Application Reactivity
mGluR Isoform Comparison

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