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**4-Chlorokynurenine** is a small molecule prodrug that is orally active and able to cross the blood-brain barrier. It is converted in the central nervous system by kynurenine aminotransferase in astrocytes into its active metabolite, 7-chlorokynurenic acid. This metabolite acts as an antagonist at the glycine co-agonist site of NMDA receptors. The drug was primarily investigated for its potential as a rapid-onset antidepressant and for neuropathic pain. Preclinical studies also suggested possible efficacy in neurodegenerative diseases such as Huntington's disease. Development was initially conducted by Artemis Neuroscience (later acquired by VistaGen), with clinical trials reaching Phase II/III for depression but failing to show efficacy over placebo[1][6][10].
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