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-118179
    VU0486321
    		Agonist 99.30%
    VU0486321 is a compound in a class of mGlu1 positive allosteric modulators (PAMs). VU0486321 maintains acceptable mGlu1 PAM potency, DMPK profile, CNS permeability, and mGluR selectivity.
    VU0486321
  • HY-103574
    Raseglurant hydrochloride
    		Modulator 99.69%
    Raseglurant hydrochloride is a negative allosteric modulator of mGluR5. Raseglurant hydrochloride can be used in study migraine.
    Raseglurant hydrochloride
  • HY-107503
    MMPIP
    		Antagonist 99.38%
    MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.
    MMPIP
  • HY-N0390S10
    L-Glutamine-1,2-13C2
    		Agonist 98.0%
    L-Glutamine-1,2-13C2 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-1,2-<sup>13</sup>C<sub>2</sub>
  • 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
  • HY-141848A
    (S,S)-BMS-984923
    		98.19%
    (S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC50 >1μM for mGluR5 receptor. BMS-984923 is a potent mGluR5 silent allosteric modulator. (S,S)-BMS-984923 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    (S,S)-BMS-984923
  • HY-103572
    MNI137
    		Modulator
    MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization.
    MNI137
  • HY-110180
    VU0409106
    		Inhibitor 99.76%
    VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB).
    VU0409106
  • HY-15129S
    O-Phospho-L-serine-13C3,15N
    		Modulator 99.19%
    O-Phospho-L-serine-13C3,15N is the 13C- and 15N-labeled O-Phospho-L-serine. 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.
    O-Phospho-L-serine-<sup>13</sup>C<sub>3</sub>,<sup>15</sup>N
  • 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-107508
    VU-29
    		Agonist 99.63%
    VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM).
    VU-29
  • HY-119097
    LY456066
    		Antagonist 99.0%
    LY456066 is a selective non-competitive metabotropic glutamate receptors (mGluR1) antagonist with an IC50 value of 52.0 nM. LY456066 is effective in rodent models of anxiolysis and nociception. LY456066 reduces hyperalgesia and the amount of licking and flinching following formalin injection, which is promising for research of analgesics for chronic pain.
    LY456066
  • 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 99.91%
    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-14418
    VU0361737
    		Agonist 99.65%
    VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM), with EC50s of 240 nM and 110 nM for human and rat mGluR4 receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research.
    VU0361737
  • 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-103565A
    AMN082 free base
    		Agonist 98.37%
    AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
    AMN082 free base
  • HY-115483
    VU0477573
    		Modulator
    VU0477573 is a brain-penetrant partial negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGluR5). VU0477573 exhibits neuroprotective and anxiolytic effects. VU0477573 can be used for the research of neurological disease, such as Parkinson disease.
    VU0477573
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
mGluR Isoform Comparison

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