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-16951
    VU-1545
    		Agonist 99.00%
    VU-1545 is a metabotropic glutamate receptor 5 positive allosteric modulator (mGluR5 PAM) with a Ki of 156 nM and an EC50 of 9.6 nM.
    VU-1545
  • HY-16654
    ML254
    		Modulator
    ML254 is a potent mGlu5 potentiator, with EC50 and pEC50 of 9.3 nM and 8.03 nM for rat mGlu5, respectively. ML254 can be used for researching schizophrenia. ML254 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ML254
  • 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-102091A
    (2R,4R)-APDC hydrate
    		Agonist 98.0%
    (2R,4R)-APDC hydrate ((2R,4R)-4-Aminopyrrolidine-2,4-dicarboxylic acid hydrate) is a group II metabotropic glutamate receptor (mGluR) agonist. (2R,4R)-APDC hydrate affects cell proliferation by inhibiting glutamate release, enhancing motor responses produced by D1 receptor activation, or reducing brain-derived neurotrophic factor (BDNF) levels. (2R,4R)-APDC hydrate can be used in the study of epilepsy and other neurological diseases.
    (2R,4R)-APDC hydrate
  • HY-132219
    N,N-Dipropyldopamine hydrobromide
    		Inhibitor 98.22%
    N. N-dipropyrldopamine is a potent inhibitor of glutamate release and has anticancer activity. The increase of glutamate secretion leads to cancer-induced bone pain (CIBP). N. N-dipropyrldopamine plays an analgesic role in CIBP.
    N,N-Dipropyldopamine hydrobromide
  • 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-114863
    PHCCC(4Me)
    		Modulator 99.99%
    PHCCC(4Me) (THCCC), a PHCCC analog, is a dual mGluR2 (IC50 of 1.5 μM) negative allosteric modulator and mGluR3 (EC50 of 8.9 μM) positive allosteric modulator.
    PHCCC(4Me)
  • HY-131289
    LY3020371
    		Antagonist
    LY3020371 is a potent and selective antagonist of glutamate (mGlu) 2/3 receptor, with Kis of 5.26 and 2.50 nM for hmGluR2 and hmGluR3, respectively. LY3020371 can be used for the research of depression.
    LY3020371
  • HY-N0390S15
    L-Glutamine-d4
    		Agonist
    L-Glutamine-d4 (L-Glutamic acid 5-amide-d4) is the deuterium labeled L-Glutamine (HY-N0390). L-Glutamine 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-d<sub>4</sub>
  • HY-15442
    Biphenylindanone A
    		Agonist 99.12%
    Biphenylindanone A (BINA) is a selective human mGluR2 (hmGluR2) potentiator for the treatment of many neurological disorders.
    Biphenylindanone A
  • HY-100588A
    VU0364770 hydrochloride
    		Agonist 99.70%
    VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride 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 hydrochloride 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 hydrochloride
  • HY-100617A
    (RS)-4CPG
    		Antagonist 99.04%
    (RS)-4CPG ((RS)-4-Carboxyphenylglycine) is a type I metabotropic glutamate receptor antagonist with activity in blocking LTP induction. In mice lacking IP3R1, (RS)-4CPG (500μM) nearly blocked long-term potentiation (LTP) induced by type I metabotropic glutamate receptor activation, with LTP of 117.6±1.7% (n = 8) in IP3R1(-/-) mice and 116.9±1.8% (n = 5) in IP3R1(+/+) mice.
    (RS)-4CPG
  • HY-103561
    DCB
    		Modulator 98.81%
    DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of themetabotropic glutamate receptor metabotropic glutamate receptor subtype 5 (mGluR5) . DCB blocks the positive allosteric regulation of mGluRs (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB). DCB shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB).
    DCB
  • HY-14866
    Raseglurant
    		Modulator 99.65%
    Raseglurant (ADX-10059) is a mGlu5 receptor negative allosteric modulator. Raseglurant is effective against migraine. Raseglurant reduces the Haloperidol (HY-14538)-induced catalepsy in mice.
    Raseglurant
  • HY-110191
    VU0469650
    		Modulator 98.70%
    VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM.
    VU0469650
  • HY-102091
    (2R,4R)-APDC
    		Agonist
    (2R,4R)-APDC is a group II metabotropic glutamate receptor (mGluR) agonist. (2R,4R)-APDC affects cell proliferation by inhibiting glutamate release, enhancing motor responses produced by D1 receptor activation, or reducing brain-derived neurotrophic factor (BDNF) levels. (2R,4R)-APDC can be used in the study of epilepsy and other neurological diseases.
    (2R,4R)-APDC
  • 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-110255A
    AZD 2066 hydrate
    		Antagonist ≥99.0%
    AZD-2066 hydrate is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 hydrate activates the BDNF/trkB signaling pathway. AZD 2066 hydrate can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease.
    AZD 2066 hydrate
  • HY-14419
    TCN238
    		Modulator 99.57%
    TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM.
    TCN238
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
mGluR Isoform Comparison

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