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-100588R
    VU0364770 (Standard)
    Agonist
    VU0364770 (Standard) is the analytical standard of VU0364770 (HY-100588). This product is intended for research and analytical applications. 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 (Standard)
  • HY-100371R
    (RS)-MCPG (Standard)
    Antagonist
    (RS)-MCPG (Standard) is the analytical standard of (RS)-MCPG. This product is intended for research and analytical applications. (RS)-MCPG (alpha-MCPG) is a competitive and selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. (RS)-MCPG blocks theta-burst stimulation (TBS)-induced shifts in both juvenile and neonatal rat hippocampal neurons.
    (RS)-MCPG (Standard)
  • HY-15446R
    Basimglurant (Standard)
    Inhibitor
    Basimglurant (RG7090; RO4917523) (Standard) is the analytical standard of Basimglurant. This product is intended for research and analytical applications. Basimglurant is a selective, orally active, blood-brain barrier permeable negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), with a Ki of 1.4 nM (against [3H]-ABP688 (HY-110141)) and 35.6 nM (against [3H]-MPEP (HY-14609A)). Basimglurant inhibits mGlu5-mediated signaling pathways and receptor constitutive activity, regulates dopamine levels in the nucleus accumbens, exerts anxiolytic, antidepressant-like, analgesic and arousal-promoting effects, and alters δ-wave power during non-rapid eye movement sleep. Basimglurant can be used in research on depression, fragile X syndrome, anxiety disorders, etc.
    Basimglurant (Standard)
  • HY-129274
    RO4988546
    Modulator
    RO4988546 is a negative allosteric modulator (NAM) that targets metabotropic glutamate receptors 2 and 3 (mGlu2, mGlu3). RO4988546 can reduce the binding of [3h]-LY354740 at the positive binding site, while affecting the receptor's G protein coupling and intracellular signaling. RO4988546 can be used in the development of antidepressants and cognitive enhancers.
    RO4988546
  • HY-11041
    LSP1-2111
    Agonist
    LSP1-2111 is a phosphinic glutamate derivative that agonists metabotropic glutamate (mGlu) receptor.
    LSP1-2111
  • HY-13206R
    MTEP hydrochloride (Standard)
    Antagonist
    MTEP (hydrochloride) (Standard) is the analytical standard of MTEP (hydrochloride). This product is intended for research and analytical applications. MTEP hydrochloride is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP hydrochloride shows antidepressant and anxiolytic-like effects. MTEP hydrochloride can be used for Parkinson's disease research.
    MTEP hydrochloride (Standard)
  • HY-100840
    (S)-4C3HPG
    Modulator
    (S)-4C3HPG ((S)-4-Carboxy-3-hydroxyphenylglycine) is an antagonist of metabotropic glutamate receptor 1a (mGluR 1a) and an agonist of GluR2. (S)-4C3HPG has the anticonvulsant activity and protects against audiogenic seizures in DBA/2 mice.
    (S)-4C3HPG
  • HY-100840
    (S)-4C3HPG
    Antagonist
    (S)-4C3HPG ((S)-4-Carboxy-3-hydroxyphenylglycine) is an antagonist of metabotropic glutamate receptor 1a (mGluR 1a) and an agonist of GluR2. (S)-4C3HPG has the anticonvulsant activity and protects against audiogenic seizures in DBA/2 mice.
    (S)-4C3HPG
  • HY-100840
    (S)-4C3HPG
    Agonist
    (S)-4C3HPG ((S)-4-Carboxy-3-hydroxyphenylglycine) is an antagonist of metabotropic glutamate receptor 1a (mGluR 1a) and an agonist of GluR2. (S)-4C3HPG has the anticonvulsant activity and protects against audiogenic seizures in DBA/2 mice.
    (S)-4C3HPG
  • HY-118256A
    (Rac)-LSN2814617
    Control
    (Rac)-LSN2814617 is a racemate of LSN2814617 (HY-118256).
    (Rac)-LSN2814617
  • HY-103558R
    LY379268 (Standard)
    Agonist
    LY379268 (Standard) is the analytical standard of LY379268 (HY-103558). This product is intended for research and analytical applications. LY379268 is a potent, selective and brain-penetrant mGlu2/3R agonist with EC50 values of 2.69 nM (mGlu2) and 4.48 nM (mGlu3). LY379268 has no activity on human mGlu 1a, 4a, 5a or 7a receptors. LY379268 has antioxidant and neuroprotective effects.
    LY379268 (Standard)
  • HY-167633
    Oxomemazine hydrochloride
    Antagonist
    Oxomemazine hydrochloride is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine hydrochloride is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki= 84 nM, M1 receptor) and low (Ki= 1.65 μM, M2 receptor) affinity sites[1]. Oxomemazine hydrochloride an antihistamine and anticholinergic agent used for the study of cough treatment.
    Oxomemazine hydrochloride
  • HY-101387A
    ACPT-II
    Agonist
    ACPT-II is an antagonist of group III mGluRs with diverse biological activities including neuroprotective, anticonvulsant, and anxiolytic-like effects.
    ACPT-II
  • HY-125717
    VU0029251
    Antagonist
    VU0029251 is a mGluR5 partial antagonist (Ki: 1.07 μM). VU0029251 inhibits glutamate induced calcium mobilization in HEK293 cell membranes expressing rat mGluR5 (IC50: 1.7 μM).
    VU0029251
  • HY-15257R
    Mavoglurant (Standard)
    Antagonist
    Mavoglurant (Standard) is the analytical standard of Mavoglurant. This product is intended for research and analytical applications. Mavoglurant (AFQ056) is a potent, selective, non-competitive and orally active mGluR5 antagonist, with an IC50 of 30 nM. Mavoglurant shows a >300 fold selectivity for the mGluR5 over all targets (238) tested. Mavoglurant can be used for the research of Fragile X syndrome (FXS), and L-dopa induced dyskinesias in Parkinson's disease. Mavoglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Mavoglurant (Standard)
  • HY-135441
    PF-06422913
    Inhibitor
    PF-06422913 is an orally active, potent and selective metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
    PF-06422913
  • HY-107509R
    LY2389575 hydrochloride (Standard)
    Modulator
    LY2389575 hydrochloride (Standard) is the analytical standard of LY2389575 (hydrochloride) (HY-107509). This product is intended for research and analytical applications. LY2389575 hydrochloride is a selective and noncompetitive mGlu3 negative allosteric modulator (NAM), with an IC50 value of 190 nM. LY2389575 hydrochloride induces an increase in Mrc1 levels. LY2389575 hydrochloride also independently amplifies Amyloid beta (Aβ) toxicity and can be used in study of Alzheimer's disease.
    LY2389575 hydrochloride (Standard)
  • HY-100366R
    Lu AF21934 (Standard)
    Agonist
    Lu AF21934 (Standard) is the analytical standard of Lu AF21934 (HY-100366). This product is intended for research and analytical applications. Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor.
    Lu AF21934 (Standard)
  • HY-107507R
    Ro 01-6128 (Standard)
    Modulator
    Ro 01-6128 (Standard) is the analytical standard of Ro 01-6128 (HY-107507). This product is intended for research and analytical applications. Ro 01-6128 is a positive allosteric modulator of mGluR1.
    Ro 01-6128 (Standard)
  • HY-100402R
    CFMTI (Standard)
    Antagonist
    CFMTI (Standard) is the analytical standard of CFMTI (HY-100402). This product is intended for research and analytical applications. CFMTI inhibits L-glutamate-induced intracellular Ca2+ mobilization in CHO cells expressing human and rat mGluR1a, with IC50s of 2.6 and 2.3 nM, respectively.
    CFMTI (Standard)
Cat. No. Product Name / Synonyms Application Reactivity

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