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7-Chlorokynurenic acid
7-Chlorokynurenic acid (7-CKA) is a drug that acts as a potent and selective noncompetitive antagonist of the glycine site of the NMDA receptor. It produces ketamine-like rapid antidepressant effects in animal models of depression. However, 7-CKA is unable to cross the blood-brain-barrier, and for this reason, is unsuitable for clinical use. As a result, a centrally-penetrant prodrug of 7-CKA, 4-chlorokynurenine (AV-101), has been developed for use in humans, and is being studied in clinical trials as a potential treatment for major depressive disorder.〔 In addition to antagonizing the NMDA receptor, 7-CKA also acts as a potent inhibitor of the reuptake of glutamate into synaptic vesicles (or as a vesicular glutamate reuptake inhibitor), an action that it mediates via competitive blockade of vesicular glutamate transporters (Ki = 0.59 mM).
==See also==
* 5,7-Dichlorokynurenic acid
* Evans blue
* Kynurenic acid
* Xanthurenic acid
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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