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LY2365109 is an inhibitor of glycine transporter 1a (GlyT1a; IC50 = 15.8 nM in BE2-C cells expressing the human transporter).1 It is selective for GlyT1a over GlyT2 (IC50 = >30 µM in RD cells expressing the human transporter). LY2365109 (10 mg/kg) induces locomotor hyperactivity, impaired gait, compulsive walking, and labored breathing, as well as impairs the ability to stand, in rats.1 It also prevents maximal electroshock-induced acute seizures in mice and decreases the number of seizures in an electroshock-induced rat model of chronic epilepsy when administered at doses of 30 and 10 mg/kg, respectively.2
WARNING This product is not for human or veterinary use.
1. Neurochemical and behavioral profiling of the selective GlyT1 inhibitors ALX5407 and LY2365109 indicate a preferential action in caudal vs. cortical brain areas. Neuropharmacology 55(5), 743-754 (2008).
2. Glycine transporter 1 is a target for the treatment of epilepsy. Neuropharmacology 99, 554-565 (2015).