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7-Chlorokynurenic acid

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Title: 7-Chlorokynurenic acid  
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Subject: NMDA receptor antagonist, NMDA receptor antagonists, A.C.E. mixture, MMPIP, LY-344,545
Collection: Antidepressants, Aromatic Acids, Chloroarenes, Excitatory Amino Acid Reuptake Inhibitors, Nmda Receptor Antagonists, Quinolones
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7-Chlorokynurenic acid

7-Chlorokynurenic acid
Systematic (IUPAC) name
7-chloro-4-oxo-1H-quinoline-2-carboxylic acid
Identifiers
CAS Registry Number
ATC code None
PubChem CID:
ChemSpider
Synonyms 7-chlorokynurenate; 7-CTKA
Chemical data
Formula C10H6ClNO3
Molecular mass 223.61254 g/mol

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.[1] It produces ketamine-like rapid antidepressant effects in animal models of depression.[2] However, 7-CKA is unable to cross the blood-brain-barrier, and for this reason, is unsuitable for clinical use.[3] 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.[3][4] 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).[5]

See also

References

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