Chemical Name: 4-Fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide
Biological ActivityPotent and selective negative allosteric modulator of mGlu1 receptors (IC50 = 5.1 nM). Displays >1300-fold selectivity for mGlu1 over other metabotropic glutamate receptors (IC50 values are 7 μM and >10 μM for mGlu5 and mGlu2 or mGlu8, respectively). Antagonizes methamphetamine-induced locomotion in mice.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator.
Wu et al.
Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist.
Satoh et al.
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