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-156331
    VU6004909
    Activator 99.40%
    VU6004909 is a blood-brain barrier penetrated mGlu1 positive allosteric modulator (PAM), with the EC50s of 25.7 nM and 31 nM for human mGlu1 and rat mGlu1, respectively. VU6004909 reduces dorsolateral striatal dopamine (DA) release in vivo and displays antipsychotic efficacy.
    VU6004909
  • HY-18760
    LY2812223
    Agonist ≥98.0%
    LY2812223 is a highly potent, functionally selective mGlu2 receptor agonist with mGlu2 binding affinity for mGlu2 and mGlu3 (Ki=144 nM and 156 nM, respectively).
    LY2812223
  • 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-110255
    AZD 2066
    Antagonist 99.8%
    AZD-2066 is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 activates the BDNF/trkB signaling pathway. AZD 2066 can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease.
    AZD 2066
  • 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-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-114978
    VU0424465
    Agonist 98.28%
    VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons.
    VU0424465
  • HY-121793
    Roemerine
    99.61%
    Roemerine is an alkaloid that has been identified from the leaves of Fibraurea recisa Pierre. Roemerine exhibits antibacterial, anticancer, and antidepressant activities, can reverse the multidrug resistance phenotype in cultured cells, and exerts antibacterial effects by regulating the cAMP signaling pathway. Additionally, Roemerine influences neuronal activity by increasing BDNF protein expression and modulating the serotonergic and glutamatergic systems. Roemerine holds promise for research in the fields of cancer, infections, and neurological diseases.
    Roemerine
  • HY-108011
    Naftazone
    Inhibitor ≥99.0%
    Naftazone is a naphthoquinone derivative, it can be used for the research of venous insufciency. Naftazone protects blood vessels, increases venous tonicity and capillary resistance, and improves lymphatic and venous circulation.
    Naftazone
  • 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-100405
    FTIDC
    Inhibitor
    FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1.
    FTIDC
  • HY-100728
    BMT-145027
    Inhibitor
    BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
    BMT-145027
  • HY-14417A
    (1R,2S)-VU0155041
    Agonist
    (1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.
    (1R,2S)-VU0155041
  • HY-107457A
    AZD-8529 mesylate
    Agonist 99.63%
    AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
    AZD-8529 mesylate
  • HY-16617
    Auglurant
    Inhibitor 99.40%
    Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration.
    Auglurant
  • HY-18941B
    (rel)-Eglumegad
    Agonist
    (rel)-Eglumegad ((rel)-LY354740) is a relative configuration of Eglumegad (HY-18941). Eglumegad is a highly potent and selective group II (mGlu2/3) receptor agonist with EC50s of 5 and 24 nM for transfected human mGlu2 and mGlu3 receptors, respectively.
    (rel)-Eglumegad
  • HY-116855
    TASP0433864
    Modulator 99.9%
    TASP0433864 is a selective positive allosteric modulator (PAM) of metabotropic glutamate 2 (mGlu2) receptor with EC50 values of 199 nM and 206 nM against human and rat mGlu2 receptors, respectively. TASP0433864 has antipsychotic activity.
    TASP0433864
  • 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-107516
    (S)-3,4-DCPG
    Agonist ≥98.0%
    (S)-3,4-DCPG is a selective agonist of metabotropic glutamate receptor 8a (mGluR8a) with an EC50 of 31 nM in AV12-664 cells expressing human mGluR8.
    (S)-3,4-DCPG
  • HY-100781B
    L-AP4 monohydrate
    Agonist ≥99.0%
    L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively.
    L-AP4 monohydrate
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