Overview

  • Product namemGlu Antagonists Kit
    See all Metabotropic glutamate receptor kits
  • SpecificityA collection of 6 antagonists for mGlu receptor subtypes. Products are freeze-dried to an exact weight so that addition of 1 ml or 0.5 ml of solvent provides a stock solution of 5 mM or 10 mM, respectively. The kit contains LY 341495 sodium salt (ab120400), (R,S)-MCPG sodium salt (ab120252), LY 367385 sodium salt (ab120418), YM 298198 hydrochloride (ab120015), MTEP hydrochloride (ab120035) and MMPIP (ab120245).
  • Product overview

    A collection of 6 antagonists for mGlu receptor subtypes. Products are freeze-dried to an exact weight so that addition of 1 ml or 0.5 ml of solvent provides a stock solution of 5 mM or 10 mM, respectively. The kit contains LY 341495 sodium salt (ab120400), (R,S)-MCPG sodium salt (ab120252), LY 367385 sodium salt (ab120418), YM 298198 hydrochloride (ab120015), MTEP hydrochloride (ab120035) and MMPIP (ab120245).

     

    Receptor

    Description

     

    All mGlu
    (mGlu1,2,3,4,5,6,7,8)

     

    LY 341495 sodium salt:

     

    Very selective nanomolar potent antagonist for group II mGlu receptors. Also a relatively potent antagonist for group III mGlu receptors at high nanomolar to low micromolar concentrations. Kd values are 1.67, 0.75, 31.6, 72.7, 14 nM at human mGlu2, mGlu3, mGlu6, mGlu7a, and human mGlu8a receptors, respectively. IC50 values are 7.8, 8.2 and 22 µM for mGlu1a, mGlu5a and mGlu4 receptors, respectively. Readily brain penetrant and active in vivo.

     

    Suggested Solvent: Water

     

    Goup I & II

     

    (R,S)-MCPG sodium salt:

     

    Group I / group II metabotropic glutamate receptor antagonist. Water soluble form.

     

    Suggested Solvent: Water

     

    mGlu1

     

    LY 367385 sodium salt:

     

    Potent, selective mGlu1a antagonist. Neuroprotective and anticonvulsant in vivo.

     

    Suggested Solvent: Water

     

     

    mGlu1

     

    YM298198 hydrochloride:

     

    Potent, selective, water-soluble, non-competitive mGlu1 antagonist (IC50 = 16 nM) Selective over mGlu2,3,4,5,6 and 7 and ionotropic receptors (IC50 > 10 µM). Orally active analgesic in vivo.

     

    Suggested Solvent: Water

     

    mGlu5

     

    MTEP hydrochloride:

     

    Brain penetrant, potent, selective and non-competitive mGlu5 receptor antagonist (IC50 = 5 nM in Ca2+-flux assay; Ki = 16 nM). In vivo anxiolytic, devoid of side effects seen with MPEP and benzodiazepines.

     

    Suggested Solvent: Water

     

    mGlu7

     

    MMPIP:

     

    Potent, selective allosteric antagonist at mGlu7 receptors. Inhibits agonist-induced intracellular calcium mobilisation and cAMP accumulation (IC50 values are 26 and 610 nM). Also displays intrinsic activity; increasing forskolin-induced cAMP accumulation in the absence of an agonist. Exhibits no significant activity at mGluR1, mGluR2, mGluR3, mGluR4, mGluR5, and mGluR8.

     

    Suggested Solvent: DMSO

     

     

  • Notes

    KIT

Properties

  • RelevanceMetabotropic Glutamate Receptor contains a Periplasmic Binding Protein Type 1 region, which belongs to Type 1 periplasmic binding fold superfamily. This model and hierarchy represent the ligand binding domains of the LacI family of transcriptional regulators, periplasmic binding proteins of the ABC-type transport systems.

References for mGlu Antagonists Kit (ab120322)

ab120322 has not yet been referenced specifically in any publications.

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Please note: All products are "FOR RESEARCH USE ONLY AND ARE NOT INTENDED FOR DIAGNOSTIC OR THERAPEUTIC USE"