YM 298198 hydrochloride
Chemical Name: 6-Amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide hydrochloride
Biological ActivityNon-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM); inactive at other mGlu receptor subtypes (mGlu2-7), 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.
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The protective signaling of metabotropic glutamate receptor 1 is mediated by sustained, β-arrestin-1-dependent ERK phosphorylation.
Emery et al.
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.
Citation for YM 298198 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for YM 298198 hydrochloride include:
1 Citation: Showing 1 - 1
Drebrin Isoforms Critically Regulate NMDAR- and mGluR-Dependent LTD Induction.
Authors: Yasuda Et al.
Front Cell Neurosci 2018;12:330
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