FTIDC

Biological Activity

FTIDC is a potent and selective mGlu₁ receptor negative allosteric modulator (IC₅₀ values are 5.8 and 6200 nM for mGlu₁ and mGlu₅ 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.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1 antagonist.
   Ito et al.
   Bioorg.Med.Chem., 2008;16:9817
2. Pharmacological effects of the metabotropic glutamate receptor 1 antagonist compared with those of the metabotropic glutamate receptor 5 antagonist and metabotropic glutamate receptor 2/3 agonist in rodents: detailed investigations with a selective allost
   Satow et al.
   J.Pharmacol.Exp.Ther., 2008;326:577
3. Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(
   Suzuki et al.
   J.Pharmacol.Exp.Ther., 2007;321:1144

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