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YM-298198 is a non-competitive antagonist of the metabotropic glutamate receptor type I (mGluR1; Ki = 19 nM).1 It is selective for mGluR1 over mGluR2-7 (IC50s = 0.016 and >10 μM, respectively). YM-298198 binds to rat cerebellum membranes (Ki = 20 nM). In vivo, YM-298198 (10 and 30 mg/kg, p.o.) increases nociceptive response latency in a mouse model of hyperalgesia induced by streptozotocin (Item No. 13104) without affecting motor coordination in a rotarod test. YM-298198 also reduces reinstatement of drug-seeking behavior induced by cocaine priming in rats.2
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1. Radioligand binding properties and pharmacological characterization of 6-
2. Group I metabotropic glutamate receptor-