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-103566
    LY456236
    Antagonist 99.81%
    LY456236 is a selective, non-competitive and orally active mGlu1 receptor antagonist that inhibits phosphoinositide hydrolysis with an IC50 of 0.145 μM. LY456236 also inhibits EGFR with an IC50 of 0.91 μM.
    LY456236
  • HY-107505A
    CBiPES
    Agonist 99.74%
    CBiPES is a potent mGlu2 positive allosteric modulator with an EC50 value of 92.8 nM. CBiPES attenuates stress-induced hyperthermia and Phencyclidine-induced hyperlocomotor activity. CBiPES can be used for research of neurological diseases, such as Parkinson's disease (PD).
    CBiPES
  • HY-107514
    (RS)-PPG
    Agonist 99.76%
    (RS)-PPG is a potent and selective agonist for group III mGluRs. The EC50s of 5.2 μM, 4.7 μM, 185 μM, and 0.2 μM for hmGluR4a, hmGluR6, hmGluR7b, and hmGluR8a, respectively. Anticonvulsive and neuroprotective activity.
    (RS)-PPG
  • HY-110146
    XAP044
    Antagonist 99.99%
    XAP044 is a potent and selective antagonist of mGlu7. The metabotropic glutamate receptor subtype 7 (mGlu7) is an important presynaptic regulator of neurotransmission in the mammalian CNS. XAP044 demonstrates good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy in rodent behavioral paradigms.
    XAP044
  • HY-100743
    DL-AP4
    Antagonist ≥98.0%
    DL-AP4 (2-Amino-4-phosphonobutyric acid) is a glutamate antagonist. DL-AP4 behaves as a competitive inhibitor of glutamate binding with an apparent Kd of 66 μM. DL-AP4 can be used for the research of central nervous system and visual system.
    DL-AP4
  • HY-155352
    mGluR5 antagonist-1
    Antagonist 98.80%
    mGluR5 antagonist-1 is an orally active mGluR5 antagonist with an IC50 value of 11.5 nM. mGluR5 antagonist-1 has anti-depressant effect. mGluR5 antagonist-1 can be used for the study of depressive disorder.
    mGluR5 antagonist-1
  • HY-103568
    YM-298198 hydrochloride
    Antagonist 99.61%
    YM-298198 hydrochloride is a high-affinity, selective, orally active, and non-competitive antagonist of metabotropic glutamate receptor type 1 (mGluR1). YM-298198 hydrochloride can be used for the research of neurological disorders.
    YM-298198 hydrochloride
  • HY-18162
    JNJ-42153605
    Modulator 99.24%
    JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.
    JNJ-42153605
  • HY-107481
    Fasoracetam
    Activator 99.24%
    Fasoracetam (NS 105) is the activator of metabotropic glutamate receptor (mGluR). Fasoracetam (NS 105) has the potential for the research of attention-deficit hyperactivity disorder (ADHD) and Alzheimer's disease (AD).
    Fasoracetam
  • HY-130553
    β-Spaglumic acid
    Antagonist 99.97%
    β-Spaglumic acid (β-NAAG) is a competitive NAAG peptidase inhibitor (Ki=1 µM) that protects spinal cord neurons from excitotoxicity and hypoxic damage. β-Spaglumic acid is also a selective mGluR3 antagonist (mGluR3 receptor functions to regulate activity-dependent synaptic potentiation in the hippocampus). β-Spaglumic acid can be used in neuroprotection-related studies.
    β-Spaglumic acid
  • HY-110141
    ABP688
    Antagonist 98.02%
    ABP688 is a high affinity human mGluR5 antagonist with anKi of 1.7 nM. Radioisotope-labeled ABP688 can be used as a PET tracer for clinical imaging of the mGlu5 receptor.
    ABP688
  • HY-12510
    Methoxy-PEPy
    Antagonist 98.19%
    Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM.
    Methoxy-PEPy
  • HY-122808
    (-)-Camphoric acid
    ≥98.0%
    (-)-Camphoric acid is the less active enantiomer of Camphoric acid. Camphoric acid stimulates osteoblast differentiation and induces glutamate receptor expression. Camphoric acid also significantly induced the activation of NF-κB and AP-1.
    (-)-Camphoric acid
  • HY-121848
    VU0155094
    Modulator 98.14%
    VU0155094 is a positive allosteric modulator with differential activity at the various group III mGluRs.
    VU0155094
  • HY-122647
    Valiglurax
    Modulator 98.96%
    Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positive allosteric modulator with EC50 values of 64.6 nM and 197 nM for hmGlu4/Gqi5 and rmGlu4 GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease.
    Valiglurax
  • HY-124984
    ML353
    Modulator 98.07%
    ML353 is a selective ligand of mGlu5 silent allosteric modulator (SAM) with an Ki value of 18.2 nM. ML353 improves the affinity of common allosteric sites, 20-fold higher than the previous mGlu5 SAM tool compound 5mpep. ML353 has potential applications in solving the intrinsic activity of SAM in vivo or as a agent blocker. ML353 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ML353
  • HY-100402
    CFMTI
    Antagonist ≥98.0%
    CFMTI inhibits L-glutamate-induced intracellular Ca2+ mobilization in CHO cells expressing human and rat mGluR1a, with IC50s of 2.6 and 2.3 nM, respectively.
    CFMTI
  • HY-N0390S3
    L-Glutamine-13C5,15N2,d5
    Agonist 99.91%
    L-Glutamine-13C5,15N2,d5 is the deuterium, 13C-, and 15-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-<sup>13</sup>C<sub>5</sub>,<sup>15</sup>N<sub>2</sub>,d<sub>5</sub>
  • HY-136587
    Oxomemazine
    Antagonist 99.18%
    Oxomemazine is a phenothiazine-based histamine H1-receptor blocker. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites. Oxomemazine is an antihistamine and anticholinergic agent used for the study of cough treatment. Oxomemazine is protective against anaphylactic microshock in guinea pigs.
    Oxomemazine
  • HY-107509
    LY2389575 hydrochloride
    Modulator 99.93%
    LY2389575 hydrochloride is a selective and noncompetitive mGlu3 negative allosteric modulator (NAM), with an IC50 value of 190 nM. LY2389575 hydrochloride induces an increase in Mrc1 levels. LY2389575 hydrochloride also independently amplifies Amyloid beta (Aβ) toxicity and can be used in study of Alzheimer's disease.
    LY2389575 hydrochloride
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