FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2153758876> ?p ?o ?g. }

• W2153758876 endingPage "89" @default.
• W2153758876 startingPage "81" @default.
• W2153758876 abstract "We have identified a series of 1H-imidazo-[4,5-c]quinolines as selective allosteric enhancers of human A3 adenosine receptors. Several of these compounds potentiated both the potency and maximal efficacy of agonist-induced responses and selectively decreased the dissociation of the agonist N6-(4-amino-3-[125I]iodobenzyl)-5'-N-methylcarboxamidoadenosine from human A3 adenosine receptors. There was no effect on the dissociation of the antagonist [3H]8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2.1-i]purin-5-one (PSB-11) from the A3 receptors, as well as [3H]N6-[(R)-phenylisopropyl]adenosine from rat brain A1 receptors and [3H]2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine from rat striatal A2A receptors, suggesting the selective enhancement of agonist binding at A3 receptors. The analogs were tested as antagonists of competitive binding at human A3 receptors, and K(i) values ranging from 120 nM to 101 microM were observed; as for many allosteric modulators of G protein-coupled receptors, an orthosteric effect was also present. The most promising leads from the present set of analogs seem to be the 2-cyclopentyl-1H-imidazo[4,5-c]quinoline derivatives, of which the 4-phenylamino analog DU124183 had the most favorable degree of allosteric modulation versus receptor antagonism. The inhibition of forskolin-stimulated cyclic AMP accumulation in intact cells that express human A3 receptors was employed as a functional index of A3 receptor activation. The enhancer DU124183 caused a marked leftward shift of the concentration-response curve of the A3 receptor agonists in the presence of antagonist and, surprisingly, a potentiation of the maximum agonist efficacy by approximately 30%. Thus, we have identified a novel structural lead for developing allosteric enhancers of A3 adenosine receptors; such enhancers may be useful for treating brain ischemia and other hypoxic conditions." @default.
• W2153758876 created "2016-06-24" @default.
• W2153758876 creator A5005878960 @default.
• W2153758876 creator A5036007966 @default.
• W2153758876 creator A5065525958 @default.
• W2153758876 creator A5080573103 @default.
• W2153758876 creator A5086091458 @default.
• W2153758876 creator A5091587615 @default.
• W2153758876 date "2002-07-01" @default.
• W2153758876 modified "2023-10-16" @default.
• W2153758876 title "Selective Allosteric Enhancement of Agonist Binding and Function at Human A₃ Adenosine Receptors by a Series of Imidazoquinoline Derivatives" @default.
• W2153758876 cites W1590230654 @default.
• W2153758876 cites W1940520978 @default.
• W2153758876 cites W1971472068 @default.
• W2153758876 cites W1991255999 @default.
• W2153758876 cites W1992958260 @default.
• W2153758876 cites W2035974703 @default.
• W2153758876 cites W2056549985 @default.
• W2153758876 cites W2069602349 @default.
• W2153758876 cites W2071203240 @default.
• W2153758876 cites W2074631079 @default.
• W2153758876 cites W2075101183 @default.
• W2153758876 cites W2092036055 @default.
• W2153758876 cites W2113630547 @default.
• W2153758876 cites W2117790622 @default.
• W2153758876 cites W2128635872 @default.
• W2153758876 cites W2166225079 @default.
• W2153758876 cites W2176076159 @default.
• W2153758876 cites W2282615337 @default.
• W2153758876 cites W2311816167 @default.
• W2153758876 cites W2336542886 @default.
• W2153758876 cites W2345346183 @default.
• W2153758876 cites W2398650198 @default.
• W2153758876 cites W2415202487 @default.
• W2153758876 cites W3182215044 @default.
• W2153758876 cites W4293247451 @default.
• W2153758876 cites W4297819556 @default.
• W2153758876 cites W2441528649 @default.
• W2153758876 doi "https://doi.org/10.1124/mol.62.1.81" @default.
• W2153758876 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3953617" @default.
• W2153758876 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/12065758" @default.
• W2153758876 hasPublicationYear "2002" @default.
• W2153758876 type Work @default.
• W2153758876 sameAs 2153758876 @default.
• W2153758876 citedByCount "61" @default.
• W2153758876 countsByYear W21537588762012 @default.
• W2153758876 countsByYear W21537588762014 @default.
• W2153758876 countsByYear W21537588762016 @default.
• W2153758876 countsByYear W21537588762017 @default.
• W2153758876 countsByYear W21537588762018 @default.
• W2153758876 countsByYear W21537588762019 @default.
• W2153758876 countsByYear W21537588762022 @default.
• W2153758876 countsByYear W21537588762023 @default.
• W2153758876 crossrefType "journal-article" @default.
• W2153758876 hasAuthorship W2153758876A5005878960 @default.
• W2153758876 hasAuthorship W2153758876A5036007966 @default.
• W2153758876 hasAuthorship W2153758876A5065525958 @default.
• W2153758876 hasAuthorship W2153758876A5080573103 @default.
• W2153758876 hasAuthorship W2153758876A5086091458 @default.
• W2153758876 hasAuthorship W2153758876A5091587615 @default.
• W2153758876 hasBestOaLocation W21537588762 @default.
• W2153758876 hasConcept C16587737 @default.
• W2153758876 hasConcept C166342909 @default.
• W2153758876 hasConcept C170493617 @default.
• W2153758876 hasConcept C182683403 @default.
• W2153758876 hasConcept C185592680 @default.
• W2153758876 hasConcept C2776038425 @default.
• W2153758876 hasConcept C2776991684 @default.
• W2153758876 hasConcept C2778938600 @default.
• W2153758876 hasConcept C38533456 @default.
• W2153758876 hasConcept C55493867 @default.
• W2153758876 hasConcept C58732023 @default.
• W2153758876 hasConcept C67907053 @default.
• W2153758876 hasConcept C71240020 @default.
• W2153758876 hasConcept C86803240 @default.
• W2153758876 hasConcept C86811712 @default.
• W2153758876 hasConcept C98274493 @default.
• W2153758876 hasConceptScore W2153758876C16587737 @default.
• W2153758876 hasConceptScore W2153758876C166342909 @default.
• W2153758876 hasConceptScore W2153758876C170493617 @default.
• W2153758876 hasConceptScore W2153758876C182683403 @default.
• W2153758876 hasConceptScore W2153758876C185592680 @default.
• W2153758876 hasConceptScore W2153758876C2776038425 @default.
• W2153758876 hasConceptScore W2153758876C2776991684 @default.
• W2153758876 hasConceptScore W2153758876C2778938600 @default.
• W2153758876 hasConceptScore W2153758876C38533456 @default.
• W2153758876 hasConceptScore W2153758876C55493867 @default.
• W2153758876 hasConceptScore W2153758876C58732023 @default.
• W2153758876 hasConceptScore W2153758876C67907053 @default.
• W2153758876 hasConceptScore W2153758876C71240020 @default.
• W2153758876 hasConceptScore W2153758876C86803240 @default.
• W2153758876 hasConceptScore W2153758876C86811712 @default.
• W2153758876 hasConceptScore W2153758876C98274493 @default.
• W2153758876 hasIssue "1" @default.
• W2153758876 hasLocation W21537588761 @default.
• W2153758876 hasLocation W21537588762 @default.
• W2153758876 hasLocation W21537588763 @default.
• W2153758876 hasLocation W21537588764 @default.

• next