Metabotropic Glutamate Receptors (mGluR)

Metabotropic glutamate receptor (mGluR) ligands include agonists, antagonists and allosteric modulators. Unlike ionotropic glutamate receptors, mGluRs are G protein-coupled receptors and tune synaptic transmission and neuronal excitability. The first mGluR was cloned from rat brain in 1991 and linked to phosphoinositide signaling. The eight subtypes form group I (mGluR1, mGluR5), group II (mGluR2, mGluR3) and group III (mGluR4, mGluR6, mGluR7, mGluR8). LY404039 is an mGluR2/3 agonist, and LY341495 is a broad mGluR antagonist most active at group II receptors. ADX-47273 is a positive allosteric modulator of mGluR5, whereas dipraglurant and CTEP are negative modulators of the same receptor.

1 Item

  • VU0424465
    Cat. No.
    A56865

    VU0424465

    VU0424465 is a potent partial agonist and positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 5 (mGlu5), primarily targeting intracellular calcium (iCa2+) mobilization. With a Ki value of 11.8 nM, VU0424465 demonstrates high affinity at the MPEP allosteric binding site. This compound also facilitates the activation of pERK1/2 in cortical neurons, making it a valuable tool for research into neurological disorders and signaling pathways associated with mGlu5 activation.

    5 mg
    $195.00
    10 mg
    $330.00
    All 5 sizes

1 Item

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