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CFMTI is a metabotropic glutamate receptor 1 (mGluR1) allosteric antagonist (IC50 = 2.6 nM in CHO cells expressing the human receptor).1,2 It is selective for mGluR1 over mGluR5 by greater than 2,000-fold, as well as over mGluR2, -4, -6, -7, or -8 at 10 µM in CHO cells expressing the human receptors.2 CFTMI reduces methamphetamine-induced hyperlocomotion in mice when administered orally at doses ranging from 1 to 10 mg/kg.
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1. Discovery and biological profile of isoindolinone derivatives as novel metabotropic glutamate receptor 1 antagonists: A potential treatment for psychotic disorders. Bioorg. Med. Chem. Lett. 19(18), 5310-5313 (2009).
2. Unique antipsychotic activities of the selective metabotropic glutamate receptor 1 allosteric antagonist 2-