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-103575R
    MFZ 10-7 (Standard)
    Antagonist
    MFZ 10-7 (Standard) is the analytical standard of MFZ 10-7 (HY-103575). This product is intended for research and analytical applications. MFZ 10-7 is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5. MFZ 10-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MFZ 10-7 (Standard)
  • HY-107510
    YM-230888
    Antagonist
    YM-230888 is an orally active, selective and allosteric mGlu1 receptor antagonist with a Ki of 13 nM. YM-230888 inhibits mGlu1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 13 nM. YM-230888 shows antinociceptive response in Streptozotocin (HY-13753)-induced hyperalgesia models. YM-230888 significantly reduces pain parameters in complete Freund's adjuvant (HY-153808)-induced arthritic pain models.
    YM-230888
  • HY-103572R
    MNI137 (Standard)
    Modulator
    MNI137 (Standard) is the analytical standard of MNI137 (HY-103572). This product is intended for research and analytical applications. MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization.
    MNI137 (Standard)
  • HY-107515AR
    LY367385 hydrochloride (Standard)
    Antagonist
    LY367385 hydrochloride (Standard) is the analytical standard of LY367385 (hydrochloride) (HY-107515A). This product is intended for research and analytical applications. LY367385 hydrochloride is a highly selective and potent mGluR1a antagonist. LY367385 hydrochloride has an IC50 of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 hydrochloride has neuroprotective, anticonvulsant and antiepileptic effects.
    LY367385 hydrochloride (Standard)
  • HY-123667
    NCFP
    Modulator
    NCFP is a metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulator (PAM). NCFP can be used in the study of central nervous system diseases.
    NCFP
  • HY-101364AR
    CHPG sodium salt (Standard)
    Agonist
    CHPG (sodium salt) (Standard) is the analytical standard of CHPG (sodium salt). This product is intended for research and analytical applications. CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways..
    CHPG sodium salt (Standard)
  • HY-103111R
    MMPIP hydrochloride (Standard)
    Antagonist
    MMPIP hydrochloride (Standard) is the analytical standard of MMPIP hydrochloride (HY-103111). This product is intended for research and analytical applications. MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.
    MMPIP hydrochloride (Standard)
  • HY-107457AR
    AZD-8529 mesylate (Standard)
    Agonist
    AZD-8529 mesylate (Standard) is the analytical standard of AZD-8529 (mesylate) (HY-107457A). This product is intended for research and analytical applications. AZD-8529 mesylate 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 mesylate (Standard)
  • HY-180871
    GRM1 modulator-1
    GRM1 modulator-1 is a GRM1 modulator.
    GRM1 modulator-1
  • HY-107508R
    VU-29 (Standard)
    Agonist
    VU-29 (Standard) is the analytical standard of VU-29 (HY-107508). This product is intended for research and analytical applications. VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM).
    VU-29 (Standard)
  • HY-103565AR
    AMN082 free base (Standard)
    Agonist
    AMN082 (free base) (Standard) is the analytical standard of AMN082 (free base). This product is intended for research and analytical applications. AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
    AMN082 free base (Standard)
  • HY-108703AR
    Foliglurax monohydrochloride (Standard)
    Agonist
    Foliglurax monohydrochloride (Standard) is the analytical standard of Foliglurax (monohydrochloride) (HY-108703A). This product is intended for research and analytical applications. Foliglurax monohydrochloride (PXT002331 monohydrochloride) 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 monohydrochloride (Standard)
  • HY-100838A
    L-CCG-I
    Agonist
    L-CCG-I is an extended isomer of conformationally restricted glutamate analog. L-CCG-I also is a potent agonist for mGluR2 with an EC50 value of 0.3 nM. L-CCG-I can be used for the research of mGluR family.
    L-CCG-I
  • HY-103565R
    AMN082 (Standard)
    Agonist
    AMN082 (Standard) is the analytical standard of AMN082. This product is intended for research and analytical applications. 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 (Standard)
  • HY-107982R
    VU6005649 (Standard)
    Agonist
    VU6005649 (Standard) is the analytical standard of VU6005649 (HY-107982). This product is intended for research and analytical applications. VU6005649 is a blood-brain-barrier penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.
    VU6005649 (Standard)
  • HY-107505AR
    CBiPES (Standard)
    Agonist
    CBiPES (Standard) is the analytical standard of CBiPES (HY-107505A). This product is intended for research and analytical applications. CBiPES is a potent mGlu2 positive allosteric modulator with an EC50 value of 92.8 nM. CBiPES attenuates stress-induced hyperthermia and Phencyclidine-induced hyperlocomotor activity. CBiPES can be used for research of neurological diseases, such as ParKinson's disease (PD).
    CBiPES (Standard)
  • HY-100588AR
    VU0364770 hydrochloride (Standard)
    Agonist
    VU0364770 (hydrochloride) (Standard) is the analytical standard of VU0364770 (hydrochloride) (HY-100588A). This product is intended for research and analytical applications. 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 (Standard)
  • HY-103566R
    LY456236 (Standard)
    Antagonist
    LY456236 (Standard) is the analytical standard of LY456236 (HY-103566). This product is intended for research and analytical applications. LY456236 is a selective, non-competitive and orally active antagonist of glutamate receptor 1 (mGlu1), which can inhibit phosphatidylinositol hydrolysis with an IC50 of 0.145 μM. LY456236 can also inhibit EGFR, with an IC50 of 0.918 μM. LY456236 has anticonvulsant effects and blocks cell proliferation by inhibiting the MAPK pathway, reversing the anti-apoptotic effect of DHPG (HY-12598A). LY456236 can be used in epilepsy research.
    LY456236 (Standard)
  • HY-131642
    L-γ-Carboxyglutamic acid
    Antagonist
    L-γ-Carboxyglutamic acid (H-Gla-OH) is a mGluR2 antagonist with an IC50 of 102 μM. L-γ-Carboxyglutamic acid binds to the mGluR2 receptor site via the overlapping extended amino acid conformation of its amino and carboxyl groups with glutamic acid, and its additional acidic group locates in a restricted region, thereby blocking the full activation of the receptor. L-γ-Carboxyglutamic acid can be used for the research of neurological disorders.
    L-γ-Carboxyglutamic acid
  • HY-124393
    GRN-529
    Modulator
    GRN-529 is a negative allosteric modulator (NAM) for mGluR5. GRN-259 modulates sleep-wake activity, and exhibits anxiolytic efficacy in rats.
    GRN-529
Cat. No. Product Name / Synonyms Application Reactivity

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