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-176420
    VU6031545
    Modulator
    VU6031545 is a potent mGlu 5 negative allosteric modulator with an IC50 of 15 nM. VU6031545 has excellent brain penetrant and oral bioavailability in rats.
    VU6031545
  • HY-117697
    Lu AF11205
    Agonist
    Lu AF11205 is a mGlu5 receptor positive allosteric modulator with activity modulating mGlu5 receptor activity. Optimization of Lu AF11205 resulted in a series of potent fused thiazole analogs whose structures and activities were influenced by substituents and which could affect receptor function in cell lines expressing mGlu5 receptors.
    Lu AF11205
  • HY-13239A
    LY2979165 free base
    Agonist
    LY2979165 free base is the alanine proagent of 2812223, a selective and potent orthosteric mGlu2 receptor agonist.
    LY2979165 free base
  • HY-116067
    VU0404251
    Modulator
    VU0404251 is a highly potent positive allosteric modulator of mGlu for the study of psychosis.
    VU0404251
  • HY-131287
    MGS0028
    Agonist
    MGS0028 is a selective metabotropic glutamate 2/3 (mGlu2/3) receptor agonist. MGS0028 can be used for psychiatric disorders research.
    MGS0028
  • HY-103575A
    MFZ 10-7 hydrochloride
    Antagonist
    MFZ 10-7 hydrochloride is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5. MFZ 10-7 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MFZ 10-7 hydrochloride
  • HY-176122
    VU6024945
    Inhibitor
    VU6024945 is an orally active negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGlu5 NAM) with an IC50 value of 110 nM. VU6024945 can be used in the research of anti-anxiety, anti-depression and Parkinson's disease and other neurological diseases.
    VU6024945
  • HY-163831
    AZ12559322
    Modulator
    AZ12559322 is a positive allosteric modulator of mGluR2, with the Ki value of 1.31 nM. AZ12559322 can be used in neurological research.
    AZ12559322
  • HY-18679
    TC-N 22A
    Agonist
    TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo.
    TC-N 22A
  • HY-103557
    Ro 64-5229
    Antagonist
    Ro 64-5229 is a selective, non-competitive mGlu2 antagonist. RO 64-5229 reduces the presynaptic inhibitory effect of Neuroligin 1.
    Ro 64-5229
  • HY-101247
    MTPG
    Antagonist
    MTPG is a potent mGluR2 and mGluR3 antagonist. MTPG can block the induction of brain ischemic tolerance induced by cerebral ischemic preconditioning. MTPG also significantly attenuates the inhibitory effect of L-CCG-1 on the KCl-evoked dopamine release.
    MTPG
  • HY-103549
    Z-Cyclopentyl-AP4
    Agonist
    Z-Cyclopentyl-AP4 is a kainate-type glutamate receptor agonist (orthosteric agonist). Z-Cyclopentyl-AP4 is more selective for mGlu4 than mGlu8.
    Z-Cyclopentyl-AP4
  • HY-107513
    BAY 36-7620
    Antagonist
    BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research.
    BAY 36-7620
  • HY-120727
    VU0364289
    Activator 99.52%
    VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC50 of 1.6 μM. VU0364289 shows excellent central nervous system penetration. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research.
    VU0364289
  • HY-135464
    (±)-LY367385
    Antagonist 98.0%
    (±)-LY367385 is the racemate of LY367385. LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with > 100 μM for mGlu5a.
    (±)-LY367385
  • HY-120662
    GSK1331268
    Agonist
    GSK1331268 is a selective, orally active agonist for mGluR2 with a pEC50 of 6.9. GSK1331268 exhibits good blood-brain barrier penetration. GSK1331268 regulates glutamate signaling, and can be used in research of neurodegenerative and neuropsychiatric diseases.
    GSK1331268
  • HY-162117
    LBG30300
    Agonist
    LBG30300 is a subtype-selective mGlu2 receptor agonist EC50 0.6 nM. LBG30300 is blood-brain barrier permeable.
    LBG30300
  • HY-107506
    Ro 67-4853
    Agonist 99.90%
    Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation.
    Ro 67-4853
  • HY-114589
    VU0240382
    Modulator
    VU0240382 is a metabotropic glutamate receptor subtype 5 modulator whose activity differs depending on whether it has allosteric agonist activity. VU0240382 with allosteric agonist activity can activate mGlu(5) receptors in cell lines, but has no agonist activity in natural systems and has similar efficacy to mGlu(5) modulators without allosteric agonist activity in animal models.
    VU0240382
  • HY-120068
    VU0418506
    Modulator
    VU0418506 is a selective positive allosteric modulator of mGlu4, with EC50 values of 68 nM and 46 nM for hmGlu4 and rmGlu4, respectively. VU0418506 exhibits antiparkinsonian activity.
    VU0418506
Cat. No. Product Name / Synonyms Application Reactivity

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