FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2057011012> ?p ?o ?g. }

• W2057011012 endingPage "4773" @default.
• W2057011012 startingPage "4762" @default.
• W2057011012 abstract "Studies have shown that functionalized amino acids (FAA) exhibit outstanding activity in the maximal electroshock-induced seizure (MES) test in rodents. Affinity labels patterned in part after the potent antiepileptic (R)-N-benzyl-2-acetamido-3-methoxypropionamide ((R)-2) have been prepared as mechanistic probes to learn the pharmacological basis for FAA function. The chemical reactivity of the affinity labels with nucleophiles was assessed, and the labels were evaluated in in vitro radioligand assays and in the MES tests in rodents. The affinity labels did not bind to receptors known to effect seizure spread. Three affinity labels, (R,S)-N-benzyl-2-acetamido-6-isothiocyanatohexanamide ((R,S)-5), (R)-N-(4-isothiocyanatobenzyl)-2-acetamido-3-methoxypropionamide ((R)-6), and (R)-N-(3-isothiocyanatobenzyl)-2-acetamido-3-methoxypropionamide ((R)-7), possessed excellent in vivo anticonvulsant activity and exhibited maximal activity at later time periods than typically observed for FAA. The anticonvulsant activity of 6 and 7 resided primarily in the (R)-enantiomer and the activity of (R)-6 and (R)-7 in rats (po) exceeded that of phenytoin. The chemical properties, pharmacological profile, and marked stereospecificity associated with 6 and 7 anticonvulsant activity make these compounds useful pharmacological tools for the study of the mode of action of FAA." @default.
• W2057011012 created "2016-06-24" @default.
• W2057011012 creator A5009918729 @default.
• W2057011012 creator A5031331094 @default.
• W2057011012 creator A5035547619 @default.
• W2057011012 date "2002-09-06" @default.
• W2057011012 modified "2023-09-23" @default.
• W2057011012 title "Design and Evaluation of Affinity Labels of Functionalized Amino Acid Anticonvulsants" @default.
• W2057011012 cites W1526242994 @default.
• W2057011012 cites W1716380650 @default.
• W2057011012 cites W1972704129 @default.
• W2057011012 cites W1974806272 @default.
• W2057011012 cites W1976302097 @default.
• W2057011012 cites W2013676686 @default.
• W2057011012 cites W2017207360 @default.
• W2057011012 cites W2026520412 @default.
• W2057011012 cites W2034883233 @default.
• W2057011012 cites W2056417306 @default.
• W2057011012 cites W2059481292 @default.
• W2057011012 cites W2062783995 @default.
• W2057011012 cites W2063832955 @default.
• W2057011012 cites W2066607517 @default.
• W2057011012 cites W2075477816 @default.
• W2057011012 cites W2126590439 @default.
• W2057011012 cites W2147873829 @default.
• W2057011012 cites W2151209974 @default.
• W2057011012 cites W2318380866 @default.
• W2057011012 cites W2323471917 @default.
• W2057011012 cites W2951639807 @default.
• W2057011012 cites W4252724300 @default.
• W2057011012 doi "https://doi.org/10.1021/jm020225f" @default.
• W2057011012 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/12361404" @default.
• W2057011012 hasPublicationYear "2002" @default.
• W2057011012 type Work @default.
• W2057011012 sameAs 2057011012 @default.
• W2057011012 citedByCount "22" @default.
• W2057011012 countsByYear W20570110122013 @default.
• W2057011012 countsByYear W20570110122014 @default.
• W2057011012 countsByYear W20570110122017 @default.
• W2057011012 crossrefType "journal-article" @default.
• W2057011012 hasAuthorship W2057011012A5009918729 @default.
• W2057011012 hasAuthorship W2057011012A5031331094 @default.
• W2057011012 hasAuthorship W2057011012A5035547619 @default.
• W2057011012 hasConcept C114373084 @default.
• W2057011012 hasConcept C116073593 @default.
• W2057011012 hasConcept C142724271 @default.
• W2057011012 hasConcept C150903083 @default.
• W2057011012 hasConcept C15744967 @default.
• W2057011012 hasConcept C161790260 @default.
• W2057011012 hasConcept C169760540 @default.
• W2057011012 hasConcept C170493617 @default.
• W2057011012 hasConcept C185592680 @default.
• W2057011012 hasConcept C187921627 @default.
• W2057011012 hasConcept C193042331 @default.
• W2057011012 hasConcept C202751555 @default.
• W2057011012 hasConcept C204787440 @default.
• W2057011012 hasConcept C207001950 @default.
• W2057011012 hasConcept C2775858608 @default.
• W2057011012 hasConcept C2776910235 @default.
• W2057011012 hasConcept C2778186239 @default.
• W2057011012 hasConcept C2778337148 @default.
• W2057011012 hasConcept C2778938600 @default.
• W2057011012 hasConcept C38533456 @default.
• W2057011012 hasConcept C486523 @default.
• W2057011012 hasConcept C55493867 @default.
• W2057011012 hasConcept C67847695 @default.
• W2057011012 hasConcept C71240020 @default.
• W2057011012 hasConcept C71924100 @default.
• W2057011012 hasConcept C86803240 @default.
• W2057011012 hasConcept C98274493 @default.
• W2057011012 hasConceptScore W2057011012C114373084 @default.
• W2057011012 hasConceptScore W2057011012C116073593 @default.
• W2057011012 hasConceptScore W2057011012C142724271 @default.
• W2057011012 hasConceptScore W2057011012C150903083 @default.
• W2057011012 hasConceptScore W2057011012C15744967 @default.
• W2057011012 hasConceptScore W2057011012C161790260 @default.
• W2057011012 hasConceptScore W2057011012C169760540 @default.
• W2057011012 hasConceptScore W2057011012C170493617 @default.
• W2057011012 hasConceptScore W2057011012C185592680 @default.
• W2057011012 hasConceptScore W2057011012C187921627 @default.
• W2057011012 hasConceptScore W2057011012C193042331 @default.
• W2057011012 hasConceptScore W2057011012C202751555 @default.
• W2057011012 hasConceptScore W2057011012C204787440 @default.
• W2057011012 hasConceptScore W2057011012C207001950 @default.
• W2057011012 hasConceptScore W2057011012C2775858608 @default.
• W2057011012 hasConceptScore W2057011012C2776910235 @default.
• W2057011012 hasConceptScore W2057011012C2778186239 @default.
• W2057011012 hasConceptScore W2057011012C2778337148 @default.
• W2057011012 hasConceptScore W2057011012C2778938600 @default.
• W2057011012 hasConceptScore W2057011012C38533456 @default.
• W2057011012 hasConceptScore W2057011012C486523 @default.
• W2057011012 hasConceptScore W2057011012C55493867 @default.
• W2057011012 hasConceptScore W2057011012C67847695 @default.
• W2057011012 hasConceptScore W2057011012C71240020 @default.
• W2057011012 hasConceptScore W2057011012C71924100 @default.
• W2057011012 hasConceptScore W2057011012C86803240 @default.
• W2057011012 hasConceptScore W2057011012C98274493 @default.
• W2057011012 hasIssue "21" @default.

• next