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

mGluR

Metabotropic glutamate receptors

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-128099
    mGluR7 antagonist-2
    Antagonist
    mGluR7 antagonist-2 (compound 1) is a potent and selective metabotropic glutamate receptor 7 (mGluR7) allosteric antagonist (IC50 = 20 nM). mGluR7 antagonist-2 shows high selectivity over other mGluRs (mGluR1/2/3/4/5/6/8).
    mGluR7 antagonist-2
  • HY-103551A
    LY 541850
    Antagonist
    LY 541850 is claimed from human ionotropic and metabotropic glutamate (mGlu) receptors expressed in non-neuronal cells. LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively.
    LY 541850
  • HY-115782
    VU6001192
    Inhibitor
    VU6001192 is a potent and selective mGlu2 (metabotropic glutamate receptor 2) negative allosteric modulator. VU6001192 has potent inhibitory activity against the mGlu2 receptor (IC50 = 207 nM), but no activity against the mGlu3 receptor and the other 6 mGlu subtypes. VU6001192 can be used for the research of neurological disease, such as depression.
    VU6001192
  • 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-131293
    MGS0008
    Agonist
    MGS0008 is an orally active and brain-penetrant metabotropic glutamate receptor 2/3 (mGlu2/3) agonist with EC50 values of 29.4 nM and 45.4 nM for mGluR2 and mGluR3, respectively. MGS0008 is promising for research of central nervous system disorders, including schizophrenia, anxiety, and neurodegenerative diseases.
    MGS0008
  • HY-19021
    ADD-17014
    Antagonist
    ADD-17014 is a L-Glu antagonist. ADD-17014 impairs presynaptic excitatory amino acid L-Glu neurotransmission. ADD-17014 is a prodrug of its β-amino alcohol metabolite, and the metabolite acts as a NMDA receptor antagonist by binding to the MK-801 site located inside the NMDA receptor or ion channel. ADD-17014 has an anticonvulsant and anti-ischemic activity. ADD-17014 can be used for neurodegenerative diseases like Parkinson’s disease, Alzheimer’s disease and stroke research.
    ADD-17014
  • 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-177302
    mGluR2 modulator 6
    Modulator
    mGluR2 modulator 6 (Compound 25-a) is a mGluR2 modulator. mGluR2 modulator 6 has anticonvulsant activity in the 6Hz epilepsy model, and the effect is better when combined with Levetiracetam (HY-B0106). mGluR2 modulator 6 can be used in the research of epilepsy.
    mGluR2 modulator 6
  • HY-114891
    R214127
    Antagonist
    R214127 is a selective mGlu1 receptor antagonist with IC50 values of 6 and 14 nM for rat and human mGlu1a. R214127 acts on a site from the glutamate binding pocket, and competes for the same transmembrane segment VII as other noncompetitive mGlu1 antagonists.
    R214127
  • 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-175100
    HexylHIBO hydrobromide
    Antagonist
    HexylHIBO hydrobromide is a potent group I mGluR antagonist with Kbs of 140 μM and 110 μM at mGlu1a and mGlu5a receptors, respectively. HexylHIBO hydrobromide does not inhibits mGlu2 and mGlu4a. HexylHIBO hydrobromide decreases spontaneous excitatory postsynaptic currents (sEPSCs) in rat.
    HexylHIBO hydrobromide
  • 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 99.45%
    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 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-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-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
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