LY2365109 (hydrochloride)

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. Perry, K.W., Falcone, J.F., Fell, M.J., et al. 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. Shen, H.-Y., van Vliet, E.A., Bright, K.-A., et al. Glycine transporter 1 is a target for the treatment of epilepsy. Neuropharmacology 99, 554-565 (2015).