Metabotropic glutamate receptors (mGluR)

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  1. GluR inhibitor

    (-)-Huperzine A is a naturally occurring sesquiterpene alkaloid compound found in the firmoss Huperzia serrata.
  2. mGluR5 positive allosteric modulator

    BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
  3. mGlu4 receptors modulator

    VU 0361737 is a selective positive allosteric modulator at mGluR-4 (EC50 values are 240 and 110 nM at human and rat receptors respectively).
  4. mGlu5 receptor antagonist

    MPEP is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors.
  5. GluR modulator

    VU 0364439 is a positive allosteric modulator (PAM) of mGlu4 receptors (EC50 = 19.8 nM in vitro for human mGlu4).
  6. mGluR antagonist

    PHCCC is a group I metabotropic glutamate receptor antagonist (IC50 ~ 3 μM).
  7. mGluR2 PAM

    JNJ-40411813 is a novel mGluR2 PAM.
  8. mGlu2 receptor agonist

    LY 379268 is a highly selective group II mGlu receptor agonist (EC50 values are 2.69 and 4.48 nM for hmGlu2 and hmGlu3 respectively) that displays > 80-fold selectivity over group I and group III receptors.
  9. mGlu5 receptor antagonist

    MPEP is a potent, highly selective non-competitive antagonist at the mGlu5a receptor subtype (IC50 = 36 nM) while having no agonist or antagonist activities at the mGlu1b receptor at concentrations up to 30 uM.
  10. mGluR2 modulator

    BINA is a selective positive allosteric modulator of mGlu2 (EC50 = 33.2 nM in CHO cells expressing human mGlu2).
  11. mGluR5 modulator

    ADX-47273 is a drug used in scientific research which acts as a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5.

  12. mGluR5 antagonists

    Dipraglurant (ADX 48621) is a mGluR5 antagonists with IC50 of 0.021 μM.
  13. mGluR-2 antagonist

    LY 341495 has been shown to be a highly potent and selective group II metabotropic glutamate receptor (mGluR-2) antagonist with Ki / IC50 values are 2.3, 1.3, 173, 990, 6800, 8200 and 22000 nM for human mGluR-2, mGluR-3, mGluR-8 , mGluR-7a, mGluR-1a, mGluR-5a and mGluR-4a.
  14. mGlu2 agonist

    LY2979165 is a mGlu2 agonist.
  15. mGluR5 PAM

    VU 0357121 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor 5 (mGlu5) with EC50 = 33 nM, 92% Glumax.
  16. CTEP is a highly potent, selective and orally bioavailable allosteric antagonist of mGlu5 receptor with an IC50 of 2.2 nM.
  17. mGlu4 receptors modulator

    VU 0364770 is a positive allosteric modulator at mGlu4 receptors with EC50 value of 290 nM in mGlu4-expressing HEK 293 cells.
  18. mGlu4 receptor modulator

    Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4.
  19. Kainate receptor agonist

    Kainate class of ionotropic glutamate receptor agonist. Has been shown to induce seizures and neurodegeneration in vivo and has also been used to induce experimental epilepsy in rodents and to examine excitation-induced neuronal apoptosis mechanisms.
  20. mGluR antagonist

    SIB 1757 is a highly selective antagonist for the mGlu5 metabotropic glutamate receptor subtype.
  21. mGluR antagonist

    SIB 1893 is a highly selective non-competitive antagonist for the metabotropic glutamate mGlu5 receptor subtype.
  22. mGluR4 modulator

    VU6001376 is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4 PAM) with an EC50 of 50.1 nM.
  23. mGluR-1 antagonist

    A 841720 is a potent, non-competitive mGluR-1 antagonist that displays 34-fold selectivity over mGluR-5 (IC50 values are 10 and 342 nM respectively).
  24. NMDA& mGlu receptor agonist

    Ibotenic acid is a neuroexcitatory amino acid originally isolated from Amanita species that functions as a NMDA and metabotropic glutamate receptor agonist.
  25. mGluR-2 modulator

    JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 receptor.
  26. CNS penetrant mGlu7/8 receptor agonist

    VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.
  27. mGlu2 receptor modulator

    CBiPES hydrochloride is a selective positive allosteric modulator of the mGluR-2 with IC50 value of 98.2 nM
  28. mGluR5 Modulator

    VU0364289 is a novel N-aryl piperazine mGlu5 positive allosteric modulator.
  29. mGluR agonist

    (S)-3,5-DHPG is an agonist of the group I metabotropic glutamate receptors (mGluRs), binding both mGluR1a and mGluR5a (Ki = 0.9 and 3.9 uM, respectively) but not ionotropic glutamate receptors.
  30. mGlu1 receptor antagonist

    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.
  31. group I/group II mGluR antagonist

    (S)-MCPG is the active isomer of (RS)-MCPG, non-selective group I/group II metabotropic glutamate receptor antagonist.

  32. mGluR 1 antagonist

    FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a.
  33. mGluR1 receptors Modulator

    DFMTI is an allosteric negative modulator of mGluR1 receptors.
  34. mGlu1 receptors modulator

    Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors.
  35. mGluR 1 allosteric antagonist

    CFMTI is a potent and selective metabotropic glutamate receptor (mGluR) 1 allosteric antagonist with IC50 of 2.6 nM.
  36. mGluR agonist

    L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92±0.03, 4.6±0.2, 3.9±0.2, 2.7±0.2, 4.0±0.2, and 3.94±0.08 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.
  37. mGluR5 agonist

    CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells.
  38. mGluR1 antagonist

    FPTQ is mGluR1 antagonist with IC50 of 6 nM and 1.4 nM for human and mouse mGluR1 respectively.
  39. mGlu5 modulator

    JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC50 of 260 nM.
  40. metabotropic receptor agonist

    trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.
  41. group I/group II mGluR antagonist

    E4CPG is a novel group I/group II metabotropic glutamate receptor antagonist, more potent than (RS)-MCPG .
  42. group I/group II mGluR antagonist

    (RS)-MCPG is a non-selective group I/group II metabotropic glutamate receptor antagonist.
  43. mGluR4 PAM

    ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
  44. mGlu5 antagonist

    Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration.
  45. group II (mGlu2/3) receptor agonist

    Eglumegad (LY354740) 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.
  46. mGlu2 receptor agonist

    LY2812223 is a highly potent, functionally selective mGlu2 receptor agonist with mGlu2 binding affinity for mGlu2 and mGlu3 (Ki=144 nM and 156 nM, respectively).
  47. group III mGluR receptors agonist

    O-Phospho-L-serine is the immediate precursor to L-serine 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.
  48. mGlu4 receptor modulator

    TCN238 is a positive allosteric mGlu4 receptor modulator with an EC50 of 1 μM.
  49. mGlu5 receptor antagonist

    Mavoglurant is a structurally novel, non-competitive mGlu5 receptor antagonist, has an IC50 of 30 nM in a functional assay with human mGluR5.
  50. mGlu5 negative allosteric modulator

    Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.

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