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

mGluR

Metabotropic glutamate receptors

mGluR

Related Products

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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-101164
    MAP4
    		Antagonist
    MAP4 is a selective group III mGluR antagonist in some electrophysiological systems.
    MAP4
  • HY-169808
    BOMA
    		Antagonist
    BOMA (Compound 7) is a potent and selective metabotropic glutamate receptor 5 (mGluR 5) antagonist with an IC50 value of 3 nM and an Ki value of 3 nM. BOMA is promising for research of various pain states, including acute, persistent and chronic pain, inflammatory pain and neuropathic pain.
    BOMA
  • HY-173032
    VU6033685
    		Agonist
    VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8%.
    VU6033685
  • HY-103556
    YM-202074 fumarate
    		Antagonist
    YM-202074 fumarate is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 fumarate binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 fumarate has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models.
    YM-202074 fumarate
  • HY-147529
    mGluR2 modulator 3
    		Modulator
    mGluR2 modulator 3 (compound 1) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice.
    mGluR2 modulator 3
  • HY-147530
    mGluR2 modulator 4
    		Inhibitor
    mGluR2 modulator 4 (compound 47) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.8 μM. mGluR2 modulator 4 can be used for researching antipsychotic.
    mGluR2 modulator 4
  • HY-119765
    VU0366248
    		Modulator
    VU0366248 is a mGlu5 negative allosteric modulator.
    VU0366248
  • HY-115796
    VU0477886
    		Activator
    VU0477886 is a metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator with potent activating activity on mGlu4 (EC50 = 95nM, 89% Glu Max), good pharmacokinetic characteristics (brain: plasma Kp = 1.3), and significant therapeutic efficacy in Parkinson's disease models.
    VU0477886
  • HY-12629
    PF470
    		Inhibitor
    PF470 (PF-06297470) is a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) with significant efficacy in Parkinson's disease models, but clinical development was halted due to potential issues found in toxicology studies.
    PF470
  • HY-P1077
    CALP1
    		Inhibitor 98.44%
    CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity.
    CALP1
  • HY-100823
    (1S,3R)-ACPD
    		Agonist
    (1S,3R)-ACPD is a mGluR agonist that can depolarize pyramidal cells.
    (1S,3R)-ACPD
  • HY-103562
    DMeOB
    		Inhibitor 98.55%
    DMeOB (3,3'-Dimethoxybenzaldazine) is a mGluR5 receptor negative allosteric modulator with an IC50 of 3 μM. DMeOB displays reversible non-competitive inhibition of mGlu5-mediated responses.
    DMeOB
  • HY-110304
    NPEC-caged-LY379268
    		Agonist
    NPEC-caged-LY379268 is a type II mGluR agonist.
    NPEC-caged-LY379268
  • HY-158376
    mGluR7-IN-1
    		Inhibitor
    mGluR7-IN-1 (compound 2Z) is a mGluR3 inhibitor.
    mGluR7-IN-1
  • HY-103559
    HexylHIBO
    		Antagonist ≥98.0%
    HexylHIBO is a potent group I mGluR antagonist with Kbs of 140 and 110 μM at mGlu1a and mGlu5a receptors, respectively. HexylHIBO decreased sEPSC in rat.
    HexylHIBO
  • HY-169835
    1-Benzyl-APDC
    1-Benzyl-APDC acts as an agonist for mGluR6, with an EC50 of 20 μM in CHO cells. 1-Benzyl-APDC is a weak antagonist of mGluR2, with an IC50 of 200 μM.
    1-Benzyl-APDC
  • HY-14417B
    VU0155041 sodium
    		Agonist
    VU0155041 sodium is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD).
    VU0155041 sodium
  • HY-108546
    L-AP3
    		Antagonist
    L-AP3, metabotropic glutamate receptor (mGluR) antagonist, inhibits D-phosphoserine and L-phosphoserine with IC50s of 368 μM and 2087 μM, respectively.
    L-AP3
  • HY-101241
    MPPG
    		Antagonist
    MPPG is a potent and selective L-AP4-sensitive receptor antagonist with an kD value of 9.2 μM, being tested on the neonatal rat spinal cord.
    MPPG
  • HY-103551
    (±)-LY395756
    		Agonist
    (±)-LY395756 is an agonist of mGlu2 receptor and an antagonist of mGlu3 receptor. (±)-LY395756 can distinguish the native mGlu2 and mGlu3 receptors.
    (±)-LY395756
Cat. No. Product Name / Synonyms Application Reactivity
mGluR Isoform Comparison

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