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- NCIT_C118314 IAO_0000115 "An orally bioavailable, blood brain barrier (BBB) penetrating, chlorinated analog of the endogenous neuromodulator kynurenic acid and prodrug of 7-chlorokynurenic acid (7-Cl-KYNA), a N-methyl-D-aspartate receptor (NMDA-R) antagonist at the glycine-coagonist (GlyB) site, with potential anti-hyperalgesic, neuroprotective and anti-epileptic activities. Unlike 7-Cl-KYNA, L-4-chlorokynurenine, upon oral administration, crosses the BBB and is enzymatically converted, through transamination, within activated astrocytes located at sites of injury in the central nervous system (CNS) to its active metabolite, 7-Cl-KYNA, which allows for high levels of this active metabolite at these specific sites. In turn, 7-Cl-KYNA selectively binds to and blocks the GlyB site within the NMDA receptors. This inhibits both NMDA-R overstimulation by the excitatory neurotransmitter glutamate and NMDA-R-mediated excitotoxicity, which prevents neuronal damage and induces analgesia. In addition, another metabolite, 4-chloro-3-hydroxyanthranilic acid, inhibits the synthesis of quinolinic acid, an endogenous NMDA receptor agonist, thereby further preventing excitotoxic damage. Compared to conventional NMDA-R antagonists, NMDA-R GlyB-specific antagonists appear to have fewer side effects." @default.
- NCIT_C118314 NCIT_NHC0 "C118314" @default.
- NCIT_C118314 NCIT_P106 "Organic Chemical" @default.
- NCIT_C118314 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C118314 NCIT_P107 "L-4-chlorokynurenine" @default.
- NCIT_C118314 NCIT_P108 "L-4-chlorokynurenine" @default.
- NCIT_C118314 NCIT_P207 "C3896652" @default.
- NCIT_C118314 NCIT_P210 "153152-32-0" @default.
- NCIT_C118314 NCIT_P319 "77XLH9L40B" @default.
- NCIT_C118314 NCIT_P322 "CTRP" @default.
- NCIT_C118314 NCIT_P322 "FDA" @default.
- NCIT_C118314 NCIT_P329 "764586" @default.
- NCIT_C118314 NCIT_P330 "764586" @default.
- NCIT_C118314 NCIT_P399 "764586" @default.
- NCIT_C118314 normalizedInformationContent "100" @default.
- NCIT_C118314 referenceCount "1" @default.
- NCIT_C118314 hasExactSynonym "4-Cl-KYN" @default.
- NCIT_C118314 hasExactSynonym "AV-101" @default.
- NCIT_C118314 hasExactSynonym "L-4-C1-KYN" @default.
- NCIT_C118314 hasExactSynonym "L-4-chlorokynurenine" @default.
- NCIT_C118314 inSubset NCIT_C116977 @default.
- NCIT_C118314 inSubset NCIT_C116978 @default.
- NCIT_C118314 inSubset NCIT_C176424 @default.
- NCIT_C118314 inSubset NCIT_C63923 @default.
- NCIT_C118314 type Class @default.
- NCIT_C118314 isDefinedBy ncit.owl @default.
- NCIT_C118314 label "L-4-chlorokynurenine" @default.
- NCIT_C118314 subClassOf NCIT_C118314 @default.
- NCIT_C118314 subClassOf NCIT_C1509 @default.
- NCIT_C118314 subClassOf NCIT_C1908 @default.
- NCIT_C118314 subClassOf NCIT_C1909 @default.
- NCIT_C118314 subClassOf NCIT_C241 @default.
- NCIT_C118314 subClassOf NCIT_C26170 @default.
- NCIT_C118314 subClassOf NCIT_C78272 @default.