Potent and selective glycine transporter type 2 (GlyT2) inhibitor (IC50
= 16 nM for hGlyT2). Displays no activity at GlyT1 or 56 other common biological targets (≥ 100 μ
M), in a glycine uptake assay in CHO cells. Ameliorates mechanical allodynia after partial sciatic nerve ligation injury in mice.
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Spinal antiallodynia action of glycine transporter inhibitors in neuropathic pain models in mice.
Morita K, Motoyama N, Kitayama T et al.
J Pharmacol Exp Ther.
The first potent and selective inhibitors of the glycine transporter type 2.
Caulfield et al.