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-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-114978
    VU0424465
    Agonist 99.84%
    VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons.
    VU0424465
  • HY-108011
    Naftazone
    Inhibitor 99.0%
    Naftazone is a naphthoquinone derivative, it can be used for the research of venous insufciency. Naftazone protects blood vessels, increases venous tonicity and capillary resistance, and improves lymphatic and venous circulation.
    Naftazone
  • 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-18162
    JNJ-42153605
    Modulator 98.76%
    JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.
    JNJ-42153605
  • 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-110141
    ABP688
    Antagonist 98.02%
    ABP688 is a high affinity human mGluR5 antagonist with anKi of 1.7 nM. Radioisotope-labeled ABP688 can be used as a PET tracer for clinical imaging of the mGlu5 receptor.
    ABP688
  • HY-101387
    rel-ACPT-I
    Agonist 99.0%
    rel-ACPT-I is an agonist of group III mGluRs with diverse biological activities including neuroprotective, anticonvulsant, and anxiolytic-like effects.
    rel-ACPT-I
  • HY-100841
    (Rac)-3-Hydroxyphenylglycine
    Control 99.14%
    (Rac)-3-Hydroxyphenylglycine (3HPG) is a racemic mixture of (S)-3-hydroxyphenylglycine and (R)-3-hydroxyphenylglycine. (S)-3-Hydroxyphenylglycine is a potent and selective mGluR1 agonist.
    (Rac)-3-Hydroxyphenylglycine
  • HY-100728
    BMT-145027
    Inhibitor
    BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
    BMT-145027
  • HY-14417A
    (1R,2S)-VU0155041
    Agonist
    (1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.
    (1R,2S)-VU0155041
  • HY-101311
    UPF-523
    Antagonist 99.89%
    UPF-523 (AIDA), a rigid (carboxyphenyl) glycine derivative, is a relatively potent and selective antagonist of group I metabotropic glutamate receptors (mGlu1a) with an IC50 of 214 μM. But UPF-523 has no effect on group II (mGlu2), group III (mGlu4) receptors or ionotropic glutamate receptors. UPF-523 has the potential for the research of the acute arthritis.
    UPF-523
  • HY-122647
    Valiglurax
    Modulator 98.96%
    Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positive allosteric modulator with EC50 values of 64.6 nM and 197 nM for hmGlu4/Gqi5 and rmGlu4 GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease.
    Valiglurax
  • HY-18941B
    (rel)-Eglumegad
    Agonist
    (rel)-Eglumegad ((rel)-LY354740) is a relative configuration of Eglumegad (HY-18941). Eglumegad is a highly potent and selective group II (mGlu2/3) receptor agonist with EC50s of 5 and 24 nM for transfected human mGlu2 and mGlu3 receptors, respectively.
    (rel)-Eglumegad
  • HY-124984
    ML353
    Modulator 98.07%
    ML353 is a selective ligand of mGlu5 silent allosteric modulator (SAM) with an Ki value of 18.2 nM. ML353 improves the affinity of common allosteric sites, 20-fold higher than the previous mGlu5 SAM tool compound 5mpep. ML353 has potential applications in solving the intrinsic activity of SAM in vivo or as a agent blocker. ML353 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ML353
  • HY-103564
    ACDPP
    Antagonist 99.0%
    ACDPP is a specific mGluR5 antagonist. ACDPP partially bolcks the increase of fragile X mental retardation protein (FMRP) caused by DHPG (HY-12598A) (group I mGluR Agonist).
    ACDPP
  • HY-116855
    TASP0433864
    Modulator 99.9%
    TASP0433864 is a selective positive allosteric modulator (PAM) of metabotropic glutamate 2 (mGlu2) receptor with EC50 values of 199 nM and 206 nM against human and rat mGlu2 receptors, respectively. TASP0433864 has antipsychotic activity.
    TASP0433864
  • HY-103571
    VU0285683
    Antagonist 99.76%
    VU0285683 is a selective mGluR5 positive allosteric modulator (PAM). VU0285683 has anxiolytic-like activity in rodent models for anxiety.
    VU0285683
  • HY-100781B
    L-AP4 monohydrate
    Agonist 99.0%
    L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively.
    L-AP4 monohydrate
  • HY-136587
    Oxomemazine
    Antagonist 99.18%
    Oxomemazine is a phenothiazine-based histamine H1-receptor blocker. Oxomemazine 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. Oxomemazine is an antihistamine and anticholinergic agent used for the study of cough treatment. Oxomemazine is protective against anaphylactic microshock in guinea pigs.
    Oxomemazine
Cat. No. Product Name / Synonyms Application Reactivity

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