Potent and selective mGlu1
receptor negative allosteric modulator (IC50
values are 5.8 and 6200 nM for mGlu1
respectively). Also acts as an mGlu1
receptor inverse agonist (IC50
= 7 nM) in the absence of ligand. Exhibits no effect at group II/III mGlu receptors. Inhibits L-glutamate-induced increases in intracellular calcium in mGlu1
-expressing CHO cells. Inhibits nociceptive behavior, and exhibits anxiolytic and antipsychotic effects in vivo
. Orally active.
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All Tocris products are intended for laboratory research use only.
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