Randomized, double-blind, placebo-controlled, dose-escalation study: Investigation of the safety, pharmacokinetics, and antihyperalgesic activity of l-4-chlorokynurenine in healthy volunteers.

•AV-101 is an oral prodrug producing a potent brain NMDAR GlyB-site antagonism.•AV-101 has excellent safety profile, similar to placebo.•AV-101 exhibited nonsignificant decreases in allodynia and hyperalgesia.•Reports of feelings of well-being with AV-101 suggest anti-depressant activity.