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Oleoyl-D-lysine is an inhibitor of glycine transporter 2a (GlyT2a).1 It selectively inhibits GlyT2a (IC50 = 48.3 nM) over GlyT1b (IC50 = >3,000 nM) in Xenopus oocytes expressing the human transporters. Oleoyl-D-lysine (30 mg/kg, i.p.) reduces allodynia in a nerve ligation rat model of neuropathic pain.
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1. Development of an N-