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-13239
    LY2979165
    Agonist 98.10%
    LY2979165 is the alanine proagent of 2812223, a selective and potent orthosteric mGlu2 receptor agonist.
    LY2979165
  • HY-15393
    VU 0357121
    Agonist 99.73%
    VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC50 of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes.
    VU 0357121
  • HY-15129R
    O-Phospho-L-serine (Standard)
    Agonist
    O-Phospho-L-serine (Standard) (L-Serine O-phosphate (Standard)) is the analytical standard of O-Phospho-L-serine (HY-15129). This product is intended for research and analytical applications. O-Phospho-L-serine is the immediate precursor to L-cystein 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 (Standard)
  • HY-105040
    Pomaglumetad methionil
    Agonist
    Pomaglumetad methionil (LY2140023 hydrate) is an oral methionine prodrug of the potent specific mGlu2/3 receptor agonist LY404039 (HY-50906). Pomaglumetad methionil is well-tolerated and has a distinct safety profile, and can be used for schizophrenia.
    Pomaglumetad methionil
  • HY-131336
    MGS0274
    Agonist
    MGS0274, an ester-based lipophilic proagent of a metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, shows improved oral bioavailability. MGS0274 has the potential for the research of schizophrenia.
    MGS0274
  • HY-157998
    mG2N001
    Modulator
    mG2N001 is a negative allosteric modulator (NAM) (IC50: 93 nM) of the metabotropic glutamate receptor mGluR2 and binds to mGluR2 as an antagonist (Ki: 63 nM). mG2N001 is microparticle- and plasma-stable, and its radioisotope [11C]mG2N001 can be used in PET imaging. [11C]mG2N001 has good brain heterogeneity and brain penetration, and can selectively accumulate in mGluR2-rich regions, producing high-contrast brain images.
    mG2N001
  • HY-18941C
    Eglumegad hydrochloride
    Agonist 99.63%
    Eglumegad (LY354740) hydrochloride is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively. Eglumegad hydrochloride protects neurons from NMDA toxicity. Eglumegad hydrochloride has anxiolytic- and antipsychotic-like effects.
    Eglumegad hydrochloride
  • HY-112814
    VU6001376
    VU6001376 is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4 PAM) with an EC50 of 50.1 nM.
    VU6001376
  • HY-108703
    Foliglurax
    Agonist
    Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 79 nM. Antiparkinsonian effect.
    Foliglurax
  • HY-119941
    VU0652835
    Inhibitor
    VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM.
    VU0652835
  • HY-120527
    VU0463841
    Antagonist
    VU0463841 is a potent, selective and brain-penetrant mGlu5 negative allosteric modulator (NAM) with an IC50 of 13 nM. VU0463841 is ineffective against mGlu1-4 and mGlu7-8. VU0463841 has the potential for the Cocaine addiction research.
    VU0463841
  • HY-117132
    YM-202074
    Antagonist
    YM-202074 is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 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 has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models.
    YM-202074
  • HY-131019
    JF-NP-26
    Inhibitor
    JF-NP-26, an inactive photocaged derivative of raseglurant, is the first caged mGlu5 receptor negative allosteric modulator. Uncaging of JF-NP-26 is elicited with light pulses in the visible spectrum (405 nm). JF-NP-26 induces light-dependent analgesia in models of inflammatory and neuropathic pain in freely behaving animals.
    JF-NP-26
  • HY-103567
    Desmethyl-YM-298198 hydrochloride
    Antagonist
    Desmethyl-YM-298198 hydrochloride is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC50: 16 nM). Desmethyl-YM-298198 hydrochloride has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice.
    Desmethyl-YM-298198 hydrochloride
  • HY-107517
    UBP 1112
    Antagonist
    UBP 1112 is a selective group III mGluR antagonist, with a Kd of 5.1 μM.UBP 1112 shows 96-fold affinity for group III over group II mGlu receptor (Kd, 488 μM), and shows no significant activity at group I mGlu receptor or iGlu receptor.
    UBP 1112
  • HY-118256
    LSN2814617
    Modulator
    LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research.
    LSN2814617
  • HY-123433
    JNJ-40068782
    Modulator
    JNJ-40068782 is a potent positive allosteric modulator of the mGlu2 receptor, with the IC50 of 38 nM.
    JNJ-40068782
  • HY-168028
    mGluR2 modulator 5
    Modulator
    mGluR2 modulator 5 (Compound 11) is an orally active, selective mGluR2 negative allosteric modulator with an IC50 of 8.9 nM. Pharmacokinetic studies in rats show that mGluR2 modulator 5 can effectively cross the blood-brain barrier. It can modulate cognitive and neurological functions in mood disorders and is suitable for research in the field of neurodegenerative diseases.
    mGluR2 modulator 5
  • HY-124406
    A-794282
    Antagonist
    A-794282 is a compound with analgesic activity and is a selective mGlu1 receptor antagonist that significantly reduces pain behaviors in a postoperative pain model, but motor side effects may occur at higher doses.
    A-794282
  • HY-107503
    MMPIP
    Antagonist
    MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.
    MMPIP
Cat. No. Product Name / Synonyms Application Reactivity

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