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. mGluR Agonist

    LY-404039 is a drug used in scientific research that acts as a selective agonist for the metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3. It has anxiolytic and antipsychotic effects in animal studies, but without causing sedation. Early human trials using a prodrug form of LY-404,039 called LY-214,0023 have also given encouraging results.
  3. mGluR2 modulator

    BINA is a selective positive allosteric modulator of mGlu2 (EC50 = 33.2 nM in CHO cells expressing human mGlu2).
  4. 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.

  5. mGluR5 antagonists

    Dipraglurant (ADX 48621) is a mGluR5 antagonists with IC50 of 0.021 μM.
  6. 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.
  7. mGlu2 agonist

    LY2979165 is a mGlu2 agonist.
  8. mGluR5 PAM

    VU 0357121 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor 5 (mGlu5) with EC50 = 33 nM, 92% Glumax.
  9. CTEP is a highly potent, selective and orally bioavailable allosteric antagonist of mGlu5 receptor with an IC50 of 2.2 nM.
  10. 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.
  11. 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.
  12. mGluR5 positive allosteric modulator

    BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
  13. 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).
  14. 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.
  15. GluR modulator

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

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

    JNJ-40411813 is a novel mGluR2 PAM.
  18. 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.
  19. 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.
  20. 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.
  21. mGluR antagonist

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

    SIB 1893 is a highly selective non-competitive antagonist for the metabotropic glutamate mGlu5 receptor subtype.
  23. 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.
  24. 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).
  25. 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.
  26. mGluR-2 modulator

    JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 receptor.
  27. mGluR1 modulator

    CPPHA is a selective positive allosteric modulator of mGluR5 receptor.
  28. mGlu5 antagonist

    MTEP hydrochloride is a potent, selective and non-competitive mGlu5 antagonist with IC50 and Ki of 5 nM and 16 nM, respectively.
  29. Noopept is a medication promoted and prescribed in Russia and neighbouring countries as a nootropic.
  30. mGluR1 antagonist

    DL-AP3, a racemic preparation of D-AP3 and L-AP3, is an inhibitor of phosphoserine phosphatase and an antagonist of the metabotropic glutamate receptor (mGluR), blocking phosphoinositide turnover mediated by the mGluR.
  31. glutamate receptors agonist

    (S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA).
  32. mGlu2 receptor modulator

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

    VU0364289 is a novel N-aryl piperazine mGlu5 positive allosteric modulator.
  34. 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.
  35. 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.
  36. mGlu5 modulator

    VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM.
  37. mGlu3 receptor agonist

    LY2794193 is a highly potent and selective mGlu3 receptor agonist (hmGlu3 Ki=0.927 nM??EC50=0.47 nM; hmGlu2 Ki=412 nM??EC50=47.5 nM).
  38. mGlu2/3 antagonist

    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.
  39. CNS penetrant modulator

    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.
  40. mGluR5 antagonist

    AZD 2066 is a selective, orally active and brain-penetrant mGluR5 antagonist, with analgesia activity.
  41. mGluR5 antagonist

    AZD 9272 is a brain penetrant mGluR5 antagonist.
  42. mGluR4 modulator

    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.
  43. mGluR2 modulator

    AZD-8529 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.
  44. mGluR5 antagonist

    Fenobam is a selective, orally active, and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively).
  45. group III mGluR antagonist

    MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent KD of 51 μM for the L-AP4-sensitive presynaptic mGluR.
  46. 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.

  47. 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.
  48. mGluR1 receptors Modulator

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

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

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

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