FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2080296082> ?p ?o ?g. }

• W2080296082 endingPage "131" @default.
• W2080296082 startingPage "119" @default.
• W2080296082 abstract "We have previously shown that (RS)-2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid (APPA, 2) is a functional partial agonist at the (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) subtype of excitatory amino acid receptors, reflecting that (S)-APPA is a full agonist and (R)-APPA a competitive antagonist at AMPA receptors. We have now synthesized and pharmacologically characterized (RS)-2-amino-3-[3-hydroxy-5-(2-fluorophenyl)isoxazol-4-yl]propioni c acid (2-F-APPA, 5a), 3-F-APPA (5b), 4-F-APPA (5c), (S)-4-F-APPA (6), (R)-4-F-APPA (7), and the fully and partially, respectively, saturated APPA (2) analogues, (RS)-2-amino-3-(3-hydroxy-5-cyclohexylisoxazol-4-yl)propionic acid (5d) and compound 5e containing a 1-cyclohexenyl ring. The absolute stereochemistry of 6 and 7 was established on the basis of comparative circular dichroism studies on 6, 7, and (S)- and (R)-APPA. 4-F-APPA (5c), (S)-4-F-APPA (6), 5d, and 5e were shown to selectively inhibit [3H]AMPA binding and to activate AMPA receptors. Whereas (S)-4-F-APPA (6) showed full AMPA receptor agonism, (R)-4-F-APPA (7) was an AMPA receptor antagonist. Co-administration of (S)- and (R)-4-F-APPA to the rat cortical wedge preparation produced functional partial AMPA receptor agonism. Semi empirical calculations showed that the magnitude of the torsional angle of the bond connecting the two rings in the series of nonannulated bicyclic AMPA analogues appears to be of importance for the potency and efficacy of these compounds." @default.
• W2080296082 created "2016-06-24" @default.
• W2080296082 creator A5015304992 @default.
• W2080296082 creator A5017298756 @default.
• W2080296082 creator A5021253711 @default.
• W2080296082 creator A5024658792 @default.
• W2080296082 creator A5035022102 @default.
• W2080296082 creator A5037689709 @default.
• W2080296082 creator A5039983849 @default.
• W2080296082 creator A5049222147 @default.
• W2080296082 creator A5061614697 @default.
• W2080296082 creator A5091820810 @default.
• W2080296082 date "1998-01-01" @default.
• W2080296082 modified "2023-09-24" @default.
• W2080296082 title "Aryl and cycloalkyl analogues of AMPA: synthetic, pharmacological and stereochemical aspects" @default.
• W2080296082 cites W1964030958 @default.
• W2080296082 cites W1966751481 @default.
• W2080296082 cites W1967823179 @default.
• W2080296082 cites W1976334156 @default.
• W2080296082 cites W1988836643 @default.
• W2080296082 cites W1991919876 @default.
• W2080296082 cites W1995814885 @default.
• W2080296082 cites W1996779761 @default.
• W2080296082 cites W2001214950 @default.
• W2080296082 cites W2001671746 @default.
• W2080296082 cites W2003951116 @default.
• W2080296082 cites W2010341693 @default.
• W2080296082 cites W2012849156 @default.
• W2080296082 cites W2016099147 @default.
• W2080296082 cites W2019105891 @default.
• W2080296082 cites W2019698272 @default.
• W2080296082 cites W2025569153 @default.
• W2080296082 cites W2028302519 @default.
• W2080296082 cites W2047275938 @default.
• W2080296082 cites W2048152070 @default.
• W2080296082 cites W2052850418 @default.
• W2080296082 cites W2054953297 @default.
• W2080296082 cites W2069413522 @default.
• W2080296082 cites W2069607377 @default.
• W2080296082 cites W2069698898 @default.
• W2080296082 cites W2077623126 @default.
• W2080296082 cites W2078698570 @default.
• W2080296082 cites W2081018793 @default.
• W2080296082 cites W2086174713 @default.
• W2080296082 cites W2090297487 @default.
• W2080296082 cites W2105930062 @default.
• W2080296082 cites W2951893301 @default.
• W2080296082 cites W2952903778 @default.
• W2080296082 doi "https://doi.org/10.1016/s0968-0896(97)10017-7" @default.
• W2080296082 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/9502111" @default.
• W2080296082 hasPublicationYear "1998" @default.
• W2080296082 type Work @default.
• W2080296082 sameAs 2080296082 @default.
• W2080296082 citedByCount "10" @default.
• W2080296082 countsByYear W20802960822021 @default.
• W2080296082 crossrefType "journal-article" @default.
• W2080296082 hasAuthorship W2080296082A5015304992 @default.
• W2080296082 hasAuthorship W2080296082A5017298756 @default.
• W2080296082 hasAuthorship W2080296082A5021253711 @default.
• W2080296082 hasAuthorship W2080296082A5024658792 @default.
• W2080296082 hasAuthorship W2080296082A5035022102 @default.
• W2080296082 hasAuthorship W2080296082A5037689709 @default.
• W2080296082 hasAuthorship W2080296082A5039983849 @default.
• W2080296082 hasAuthorship W2080296082A5049222147 @default.
• W2080296082 hasAuthorship W2080296082A5061614697 @default.
• W2080296082 hasAuthorship W2080296082A5091820810 @default.
• W2080296082 hasConcept C160268369 @default.
• W2080296082 hasConcept C170493617 @default.
• W2080296082 hasConcept C185592680 @default.
• W2080296082 hasConcept C24961977 @default.
• W2080296082 hasConcept C2776885963 @default.
• W2080296082 hasConcept C2778938600 @default.
• W2080296082 hasConcept C515207424 @default.
• W2080296082 hasConcept C55493867 @default.
• W2080296082 hasConcept C58732023 @default.
• W2080296082 hasConcept C61174792 @default.
• W2080296082 hasConcept C71240020 @default.
• W2080296082 hasConceptScore W2080296082C160268369 @default.
• W2080296082 hasConceptScore W2080296082C170493617 @default.
• W2080296082 hasConceptScore W2080296082C185592680 @default.
• W2080296082 hasConceptScore W2080296082C24961977 @default.
• W2080296082 hasConceptScore W2080296082C2776885963 @default.
• W2080296082 hasConceptScore W2080296082C2778938600 @default.
• W2080296082 hasConceptScore W2080296082C515207424 @default.
• W2080296082 hasConceptScore W2080296082C55493867 @default.
• W2080296082 hasConceptScore W2080296082C58732023 @default.
• W2080296082 hasConceptScore W2080296082C61174792 @default.
• W2080296082 hasConceptScore W2080296082C71240020 @default.
• W2080296082 hasIssue "1" @default.
• W2080296082 hasLocation W20802960821 @default.
• W2080296082 hasLocation W20802960822 @default.
• W2080296082 hasOpenAccess W2080296082 @default.
• W2080296082 hasPrimaryLocation W20802960821 @default.
• W2080296082 hasRelatedWork W1988160149 @default.
• W2080296082 hasRelatedWork W1990655162 @default.
• W2080296082 hasRelatedWork W1994883692 @default.
• W2080296082 hasRelatedWork W2044216960 @default.
• W2080296082 hasRelatedWork W2080160290 @default.

• next