2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. mGluR
  5. mGluR Antagonist

mGluR Antagonist

mGluR Isoform Comparison

mGluR Antagonists (56):

Cat. No. Product Name Effect Purity
  • HY-70059
    LY341495
    		Antagonist 99.50%
    LY341495 is a metabotropic glutamate receptor (mGluR) antagonist with IC50s of 21 nM, 14 nM, 7.8 μM, 8.2 μM, 170 nM, 990 nM, 22 μM for mGlu2, mGlu3, mGlu1a, mGlu5a, mGlu8, mGlu7, and mGlu4 receptors, respectively.
  • HY-14609
    MPEP Hydrochloride
    		Antagonist 99.93%
    MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects.
  • HY-13206
    MTEP hydrochloride
    		Antagonist 99.81%
    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.
  • HY-107515A
    LY367385 hydrochloride
    		Antagonist 98.05%
    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.
  • HY-15257
    Mavoglurant
    		Antagonist 99.72%
    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.
  • HY-108710
    VU0650786
    		Antagonist 99.97%
    VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents.
  • HY-100407
    JNJ16259685
    		Antagonist 98.10%
    JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
  • HY-15445
    CTEP
    		Antagonist 99.19%
    CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors.
  • HY-100371
    (RS)-MCPG
    		Antagonist 99.05%
    (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.
  • HY-133555
    mGluR2 antagonist 1
    		Antagonist 99.06%
    mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability.
  • HY-14859
    Dipraglurant
    		Antagonist 99.99%
    Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant mGluR5 negative allosteric modulator (NAM), with an IC50 of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo.
  • HY-100406
    (S)-MCPG
    		Antagonist 99.61%
    (S)-MCPG ((+)-MCPG) is a potent group I/II metabotropic glutamate receptor (mGluRs) antagonist and the active isomer of (RS)-MCPG (HY-100371). (S)-MCPG can be used for the study of the function of mGluRs in spatial learning.
  • HY-100382
    FPTQ
    		Antagonist 99.88%
    FPTQ is potent mGluR1 antagonist with IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively. FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo.
  • HY-123820
    LY3020371 hydrochloride
    		Antagonist 99.13%
    LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM. LY3020371 hydrochloride exerts an antidepressant-like signature in vivo.
  • HY-100402
    CFMTI
    		Antagonist ≥98.0%
    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.
  • HY-100409
    PHCCC
    		Antagonist 99.96%
    PHCCC is a Group I mGluR antagonist with an IC50 of 3 μM. PHCCC is a selective positive modulator of mGlu4 receptor. Antiparkinsonian effect.
  • HY-103111
    MMPIP hydrochloride
    		Antagonist 99.03%
    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.
  • HY-11095
    NPS 2390
    		Antagonist 98.83%
    NPS 2390 is a noncompetitive antagonist of mGluR1 and mGluR5. NPS 2390 is also a potent CaSR (calcium-sensing receptor) inhibitor.
  • HY-101478
    Fenobam
    		Antagonist 99.91%
    Fenobam is a selective, orally active, and brain-penetrant mGluR5 antagonist acting at an allosteric modulatory site (Kds of 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively). Fenobam displays inverse agonist activity which blocks the mGlu5 receptor basal activity with an IC50 of 84 nM. Fenobam exerts anxiolytic activity.
  • HY-101226
    MSOP
    		Antagonist
    MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent KD of 51 μM for the L-AP4-sensitive presynaptic mGluR.