Matches in SemOpenAlex for { <https://semopenalex.org/work/W2079951203> ?p ?o ?g. }
Showing items 1 to 93 of
93
with 100 items per page.
- W2079951203 endingPage "1566" @default.
- W2079951203 startingPage "1559" @default.
- W2079951203 abstract "Few muscarinic antagonists differentiate between the M4 and M2 muscarinic receptors. In a structure activity study, aimed at discovering leads for the development of a M4 muscarinic receptor-selective antagonist, we have synthesized and tested at cloned muscarinic receptors the binding of a group of dioxolane- or oxadiazole-dialkyl amines, and compared them to our compound 1, which contains the furan nucleus. Although none of these agents were particularly potent at M4 receptors (Kd values were typically 30-70 nM), furan derivatives (-)1 and (+)1 were significantly more potent at M4 receptors than at M2 receptors (approximately 3- and 4-fold, respectively). The dioxolane derivatives 12b and 12c were more than 10-fold selective for the M4 versus the M2 receptors, while the dioxolane derivative 12e was 15-fold more potent at M4 receptors than for M2 receptors. However, these agents bound to M3 receptors with potencies like that for the M4 receptor, so they are not M4-selective. The M4/M2 relative selectivities of some of our compounds are similar to the better hexahydrosiladifenidol derivatives, and may provide some important structural clues for the development of potent and selective M4 antagonists." @default.
- W2079951203 created "2016-06-24" @default.
- W2079951203 creator A5004138315 @default.
- W2079951203 creator A5025985537 @default.
- W2079951203 creator A5029940808 @default.
- W2079951203 creator A5034828655 @default.
- W2079951203 creator A5040696130 @default.
- W2079951203 creator A5043145057 @default.
- W2079951203 creator A5044603408 @default.
- W2079951203 date "2000-07-01" @default.
- W2079951203 modified "2023-10-15" @default.
- W2079951203 title "Design, synthesis and binding at cloned muscarinic receptors of N -[5-(1′-substituted-acetoxymethyl)-3-oxadiazolyl] and N -[4-(1′-substituted-acetoxymethyl)-2-dioxolanyl] dialkyl amines" @default.
- W2079951203 cites W1970599746 @default.
- W2079951203 cites W1970677828 @default.
- W2079951203 cites W1972417956 @default.
- W2079951203 cites W1982382054 @default.
- W2079951203 cites W2000258624 @default.
- W2079951203 cites W2019885736 @default.
- W2079951203 cites W2023707016 @default.
- W2079951203 cites W2032408087 @default.
- W2079951203 cites W2048055029 @default.
- W2079951203 cites W2064516222 @default.
- W2079951203 cites W2068385142 @default.
- W2079951203 cites W2074631079 @default.
- W2079951203 cites W2089548988 @default.
- W2079951203 cites W2223822401 @default.
- W2079951203 cites W2326462449 @default.
- W2079951203 cites W2742860702 @default.
- W2079951203 cites W2951542840 @default.
- W2079951203 cites W2952409455 @default.
- W2079951203 cites W4244570032 @default.
- W2079951203 doi "https://doi.org/10.1016/s0968-0896(00)00092-4" @default.
- W2079951203 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/10976504" @default.
- W2079951203 hasPublicationYear "2000" @default.
- W2079951203 type Work @default.
- W2079951203 sameAs 2079951203 @default.
- W2079951203 citedByCount "17" @default.
- W2079951203 countsByYear W20799512032016 @default.
- W2079951203 countsByYear W20799512032019 @default.
- W2079951203 countsByYear W20799512032020 @default.
- W2079951203 countsByYear W20799512032021 @default.
- W2079951203 countsByYear W20799512032022 @default.
- W2079951203 countsByYear W20799512032023 @default.
- W2079951203 crossrefType "journal-article" @default.
- W2079951203 hasAuthorship W2079951203A5004138315 @default.
- W2079951203 hasAuthorship W2079951203A5025985537 @default.
- W2079951203 hasAuthorship W2079951203A5029940808 @default.
- W2079951203 hasAuthorship W2079951203A5034828655 @default.
- W2079951203 hasAuthorship W2079951203A5040696130 @default.
- W2079951203 hasAuthorship W2079951203A5043145057 @default.
- W2079951203 hasAuthorship W2079951203A5044603408 @default.
- W2079951203 hasConcept C116289061 @default.
- W2079951203 hasConcept C155647269 @default.
- W2079951203 hasConcept C170493617 @default.
- W2079951203 hasConcept C185592680 @default.
- W2079951203 hasConcept C207723603 @default.
- W2079951203 hasConcept C2776666804 @default.
- W2079951203 hasConcept C2776885963 @default.
- W2079951203 hasConcept C33789571 @default.
- W2079951203 hasConcept C55493867 @default.
- W2079951203 hasConcept C71240020 @default.
- W2079951203 hasConceptScore W2079951203C116289061 @default.
- W2079951203 hasConceptScore W2079951203C155647269 @default.
- W2079951203 hasConceptScore W2079951203C170493617 @default.
- W2079951203 hasConceptScore W2079951203C185592680 @default.
- W2079951203 hasConceptScore W2079951203C207723603 @default.
- W2079951203 hasConceptScore W2079951203C2776666804 @default.
- W2079951203 hasConceptScore W2079951203C2776885963 @default.
- W2079951203 hasConceptScore W2079951203C33789571 @default.
- W2079951203 hasConceptScore W2079951203C55493867 @default.
- W2079951203 hasConceptScore W2079951203C71240020 @default.
- W2079951203 hasIssue "7" @default.
- W2079951203 hasLocation W20799512031 @default.
- W2079951203 hasLocation W20799512032 @default.
- W2079951203 hasOpenAccess W2079951203 @default.
- W2079951203 hasPrimaryLocation W20799512031 @default.
- W2079951203 hasRelatedWork W1972692739 @default.
- W2079951203 hasRelatedWork W1991634597 @default.
- W2079951203 hasRelatedWork W1999663284 @default.
- W2079951203 hasRelatedWork W2014913952 @default.
- W2079951203 hasRelatedWork W2023374499 @default.
- W2079951203 hasRelatedWork W2041005648 @default.
- W2079951203 hasRelatedWork W2043159065 @default.
- W2079951203 hasRelatedWork W2068300678 @default.
- W2079951203 hasRelatedWork W2081309033 @default.
- W2079951203 hasRelatedWork W2087314051 @default.
- W2079951203 hasVolume "8" @default.
- W2079951203 isParatext "false" @default.
- W2079951203 isRetracted "false" @default.
- W2079951203 magId "2079951203" @default.
- W2079951203 workType "article" @default.