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-12598
    (S)-3,5-DHPG
    		Agonist ≥99.0%
    (S)-3,5-DHPG is a weak, but selective group I metabotropic glutamate receptors (mGluRs) agonist with Ki values of 0.9 µM and 3.9 µM for mGluR1a and mGluR5a, respectively. (S)-3,5-DHPG exhibits anxiolytic activity in rats subjected to hypoxia.
    (S)-3,5-DHPG
  • HY-107982
    VU6005649
    		Agonist 99.53%
    VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.
    VU6005649
  • HY-103565
    AMN082
    		Agonist 99.73%
    AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
    AMN082
  • HY-14418
    VU0361737
    		Agonist 99.79%
    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-107457
    AZD-8529
    		Agonist 98.02%
    AZD-8529 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
  • HY-100366
    Lu AF21934
    		Agonist 99.75%
    Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor.
    Lu AF21934
  • HY-W011417
    Cinnabarinic acid
    		Agonist 98.74%
    Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis.
    Cinnabarinic acid
  • HY-122559
    BMS-984923
    		Modulator 99.94%
    BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling.
    BMS-984923
  • HY-P1077A
    CALP1 TFA
    		Inhibitor 98.30%
    CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity.
    CALP1 TFA
  • HY-100588
    VU0364770
    		Agonist 99.93%
    VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
    VU0364770
  • HY-101478
    Fenobam
    		Antagonist 99.91%
    Fenobam is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction.
    Fenobam
  • HY-107507
    Ro 01-6128
    		Modulator 99.87%
    Ro 01-6128 is a positive allosteric modulator of mGluR1.
    Ro 01-6128
  • HY-18654
    ADX88178
    		Agonist 99.69%
    ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
    ADX88178
  • HY-153615
    CVN636
    		Agonist 99.47%
    CVN636 is a potent, orally active and selective mGluR7 allosteric agonist with an EC50 value of 7 nM for hu mGluR7. CVN636 has central nervous system (CNS) permeability.
    CVN636
  • HY-13058
    ADX-47273
    		Agonist 99.34%
    ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC50 of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities.
    ADX-47273
  • HY-15476
    VU 0364439
    		Agonist 98.65%
    VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.
    VU 0364439
  • HY-114403
    VU6012962
    		Modulator 99.92%
    VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM.
    VU6012962
  • HY-123820
    LY3020371 hydrochloride
    		Antagonist 99.13%
    LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM. LY3020371 hydrochloride exerts an antidepressant-like signature in vivo.
    LY3020371 hydrochloride
  • 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-110190
    VU0422288
    		Modulator 99.88%
    VU0422288 (ML396) is a positive allosteric modulator of group III mGluRs. VU0422288 inhibits mGluRs with EC50s of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively in calcium mobilization assays. VU0422288 reverses deficits in contextual fear memory, social recognition, and apneas in Rett syndrome (RTT) model mice.
    VU0422288
Cat. No. Product Name / Synonyms Application Reactivity
mGluR Isoform Comparison

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