Matches in SemOpenAlex for { <https://semopenalex.org/work/W4310053510> ?p ?o ?g. }
- W4310053510 endingPage "265" @default.
- W4310053510 startingPage "255" @default.
- W4310053510 abstract "Abstract The GluN2C subunit exists predominantly, but not exclusively in NMDA receptors within the cerebellum. Antagonists such as UBP1700 and positive allosteric modulators including PYD-106 and 3-acylamino-2-aminopropionic acid derivatives such as UA3-10 (( R )-2-amino-3-{[5-(2-bromophenyl)thiophen-2-yl]carboxamido}propionic acid) represent promising tool compounds to investigate the role of GluN2C-containing NMDA receptors in the signal transduction in the brain. However, due to its high polarity the bioavailability and CNS penetration of the amino acid UA3-10 are expected to be rather low. Herein, three ester prodrugs 12a – c of the NMDA receptor glycine site agonist UA3-10 were prepared and pharmacokinetically characterized. The esters 12a – c showed higher lipophilicity (higher log D 7.4 values) than the acid UA3-10 but almost the same binding at human serum albumin. The acid UA3-10 was rather stable upon incubation with mouse liver microsomes and NADPH, but the esters 12a – c were fast hydrolyzed to afford the acid UA3-10. Incubation with pig liver esterase and mouse serum led to rapid hydrolysis of the esters 12a – c . The isopropyl ester 12c showed a promising log D 7.4 value of 3.57 and the highest stability in the presence of pig liver esterase and mouse serum. These results demonstrate that ester prodrugs of UA3-10 can potentially afford improved bioavailability and CNS penetration." @default.
- W4310053510 created "2022-11-30" @default.
- W4310053510 creator A5015251858 @default.
- W4310053510 creator A5017404448 @default.
- W4310053510 creator A5023656482 @default.
- W4310053510 creator A5038609213 @default.
- W4310053510 creator A5040260186 @default.
- W4310053510 creator A5056393768 @default.
- W4310053510 creator A5058963077 @default.
- W4310053510 creator A5060261417 @default.
- W4310053510 creator A5083917382 @default.
- W4310053510 creator A5086657090 @default.
- W4310053510 date "2022-11-25" @default.
- W4310053510 modified "2023-10-02" @default.
- W4310053510 title "<i>In vitro</i> ADME characterization of a very potent 3-acylamino-2-aminopropionic acid-derived GluN2C-NMDA receptor agonist and its ester prodrugs" @default.
- W4310053510 cites W1918304474 @default.
- W4310053510 cites W1966515122 @default.
- W4310053510 cites W1978901759 @default.
- W4310053510 cites W1994187396 @default.
- W4310053510 cites W2001575559 @default.
- W4310053510 cites W2012641732 @default.
- W4310053510 cites W2024380057 @default.
- W4310053510 cites W2037852973 @default.
- W4310053510 cites W2039974695 @default.
- W4310053510 cites W2053484514 @default.
- W4310053510 cites W2057620319 @default.
- W4310053510 cites W2065771857 @default.
- W4310053510 cites W2089094370 @default.
- W4310053510 cites W2107339318 @default.
- W4310053510 cites W2108909652 @default.
- W4310053510 cites W2139976683 @default.
- W4310053510 cites W2142978864 @default.
- W4310053510 cites W2185095623 @default.
- W4310053510 cites W2548809643 @default.
- W4310053510 cites W2560726081 @default.
- W4310053510 cites W2590999072 @default.
- W4310053510 cites W2623595717 @default.
- W4310053510 cites W2771915833 @default.
- W4310053510 cites W2802553559 @default.
- W4310053510 cites W2811141452 @default.
- W4310053510 cites W2891053092 @default.
- W4310053510 cites W2939714463 @default.
- W4310053510 cites W2945412053 @default.
- W4310053510 cites W2974847145 @default.
- W4310053510 cites W3001398113 @default.
- W4310053510 cites W3160177497 @default.
- W4310053510 cites W3214054678 @default.
- W4310053510 doi "https://doi.org/10.1515/hsz-2022-0229" @default.
- W4310053510 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36427206" @default.
- W4310053510 hasPublicationYear "2022" @default.
- W4310053510 type Work @default.
- W4310053510 citedByCount "2" @default.
- W4310053510 countsByYear W43100535102023 @default.
- W4310053510 crossrefType "journal-article" @default.
- W4310053510 hasAuthorship W4310053510A5015251858 @default.
- W4310053510 hasAuthorship W4310053510A5017404448 @default.
- W4310053510 hasAuthorship W4310053510A5023656482 @default.
- W4310053510 hasAuthorship W4310053510A5038609213 @default.
- W4310053510 hasAuthorship W4310053510A5040260186 @default.
- W4310053510 hasAuthorship W4310053510A5056393768 @default.
- W4310053510 hasAuthorship W4310053510A5058963077 @default.
- W4310053510 hasAuthorship W4310053510A5060261417 @default.
- W4310053510 hasAuthorship W4310053510A5083917382 @default.
- W4310053510 hasAuthorship W4310053510A5086657090 @default.
- W4310053510 hasBestOaLocation W43100535102 @default.
- W4310053510 hasConcept C108215921 @default.
- W4310053510 hasConcept C170493617 @default.
- W4310053510 hasConcept C181199279 @default.
- W4310053510 hasConcept C185592680 @default.
- W4310053510 hasConcept C201399114 @default.
- W4310053510 hasConcept C2777261171 @default.
- W4310053510 hasConcept C2778938600 @default.
- W4310053510 hasConcept C55493867 @default.
- W4310053510 hasConcept C67018056 @default.
- W4310053510 hasConcept C71240020 @default.
- W4310053510 hasConcept C94412978 @default.
- W4310053510 hasConceptScore W4310053510C108215921 @default.
- W4310053510 hasConceptScore W4310053510C170493617 @default.
- W4310053510 hasConceptScore W4310053510C181199279 @default.
- W4310053510 hasConceptScore W4310053510C185592680 @default.
- W4310053510 hasConceptScore W4310053510C201399114 @default.
- W4310053510 hasConceptScore W4310053510C2777261171 @default.
- W4310053510 hasConceptScore W4310053510C2778938600 @default.
- W4310053510 hasConceptScore W4310053510C55493867 @default.
- W4310053510 hasConceptScore W4310053510C67018056 @default.
- W4310053510 hasConceptScore W4310053510C71240020 @default.
- W4310053510 hasConceptScore W4310053510C94412978 @default.
- W4310053510 hasFunder F4320320879 @default.
- W4310053510 hasFunder F4320332161 @default.
- W4310053510 hasIssue "4" @default.
- W4310053510 hasLocation W43100535101 @default.
- W4310053510 hasLocation W43100535102 @default.
- W4310053510 hasLocation W43100535103 @default.
- W4310053510 hasOpenAccess W4310053510 @default.
- W4310053510 hasPrimaryLocation W43100535101 @default.
- W4310053510 hasRelatedWork W1991066523 @default.
- W4310053510 hasRelatedWork W2016004951 @default.
- W4310053510 hasRelatedWork W2032733139 @default.