YM 298198 hydrochloride

Biological Activity

YM 298198 hydrochloride is a non-competitive antagonist with high affinity and selectivity for mGlu₁ receptors (K_i = 19 nM); inactive at other mGlu receptor subtypes (mGlu_2-7), ionotropic receptors and glutamate transporters (IC₅₀ > 10 μM). Inhibits glutamate-induced IP production more potently than CPCCOEt (IC₅₀ values are 16 nM and 6.3 μM respectively), and is orally active in vivo, demonstrating an antinociceptive effect in hyperalgesic mice.

Desmethyl Derivative also available.

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.

Additional Information

Background References

1. The protective signaling of metabotropic glutamate receptor 1 is mediated by sustained, β-arrestin-1-dependent ERK phosphorylation.
   Emery et al.
   J.Biol.Chem., 2010;285:26041
2. Radioligand binding properties and pharmacological characterization of 6-Amino-N-cyclohexyl-N,3-dimethyl-thiazolo[3,2-a]-benzimidazole-2-carboxamide (YM-298198), a high-affinity, selective and noncompetitive antagonist of metabo
   Kohara et al.
   J.Pharmacol.Exp.Ther., 2005;315:163

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