FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1973137274> ?p ?o ?g. }

• W1973137274 endingPage "36" @default.
• W1973137274 startingPage "29" @default.
• W1973137274 abstract "Nociceptin/orphanin FQ (N/OFQ) was recently identified as the endogenous ligand for the opioid-receptor like (ORL1) receptor. Although the ORL1 receptor shows sequence homology with the opioid receptors, the nociceptin/ORL1 ligand-receptor system has very distinct pharmacological actions compared to the opioid receptor system. Recently, several small-molecule ORLI receptor ligands were reported by pharmaceutical companies. Most of these ligands had close structural similarities with known neuroleptics and opiates. In this study, we screened several available neuroleptics and opiates for their binding affinity and functional activity at ORL1 and the opioid receptors. We also synthesized several analogs of known opiates with modified piperidine N-substituents in order to characterize the ORL1 receptor ligand binding pocket. Substitution with the large, lipophilic cyclooctylmethyl moiety increased ORL1 receptor affinity and decreased mu receptor affinity and efficacy in the fentanyl series of ligands but had a different effect in the oripavine class of opiate ligands. Our results indicate that opiates and neuroleptics may be good starting points for ORL1 receptor ligand design, and the selectivity may be modulated by appropriate structural modifications." @default.
• W1973137274 created "2016-06-24" @default.
• W1973137274 creator A5012856412 @default.
• W1973137274 creator A5020423575 @default.
• W1973137274 creator A5027392977 @default.
• W1973137274 creator A5048254801 @default.
• W1973137274 creator A5056342025 @default.
• W1973137274 creator A5060911267 @default.
• W1973137274 creator A5090313381 @default.
• W1973137274 date "2001-09-01" @default.
• W1973137274 modified "2023-09-25" @default.
• W1973137274 title "Characterization of opiates, neuroleptics, and synthetic analogs at ORL1 and opioid receptors" @default.
• W1973137274 cites W1497141468 @default.
• W1973137274 cites W1971447101 @default.
• W1973137274 cites W1973370124 @default.
• W1973137274 cites W1983587230 @default.
• W1973137274 cites W1989963064 @default.
• W1973137274 cites W2008451776 @default.
• W1973137274 cites W2025068387 @default.
• W1973137274 cites W2025891907 @default.
• W1973137274 cites W2027145077 @default.
• W1973137274 cites W2033715015 @default.
• W1973137274 cites W2039648325 @default.
• W1973137274 cites W2041340772 @default.
• W1973137274 cites W2048606952 @default.
• W1973137274 cites W2052233342 @default.
• W1973137274 cites W2057304163 @default.
• W1973137274 cites W2064420586 @default.
• W1973137274 cites W2065031733 @default.
• W1973137274 cites W2074631079 @default.
• W1973137274 cites W2092371036 @default.
• W1973137274 cites W2094167697 @default.
• W1973137274 cites W2108871319 @default.
• W1973137274 cites W2118218199 @default.
• W1973137274 cites W2120823854 @default.
• W1973137274 cites W2163811098 @default.
• W1973137274 cites W2211878186 @default.
• W1973137274 cites W2398500408 @default.
• W1973137274 cites W2949256074 @default.
• W1973137274 doi "https://doi.org/10.1016/s0014-2999(01)01282-1" @default.
• W1973137274 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3852903" @default.
• W1973137274 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/11779034" @default.
• W1973137274 hasPublicationYear "2001" @default.
• W1973137274 type Work @default.
• W1973137274 sameAs 1973137274 @default.
• W1973137274 citedByCount "57" @default.
• W1973137274 countsByYear W19731372742012 @default.
• W1973137274 countsByYear W19731372742013 @default.
• W1973137274 countsByYear W19731372742014 @default.
• W1973137274 countsByYear W19731372742015 @default.
• W1973137274 countsByYear W19731372742017 @default.
• W1973137274 countsByYear W19731372742018 @default.
• W1973137274 countsByYear W19731372742019 @default.
• W1973137274 countsByYear W19731372742020 @default.
• W1973137274 countsByYear W19731372742021 @default.
• W1973137274 countsByYear W19731372742022 @default.
• W1973137274 countsByYear W19731372742023 @default.
• W1973137274 crossrefType "journal-article" @default.
• W1973137274 hasAuthorship W1973137274A5012856412 @default.
• W1973137274 hasAuthorship W1973137274A5020423575 @default.
• W1973137274 hasAuthorship W1973137274A5027392977 @default.
• W1973137274 hasAuthorship W1973137274A5048254801 @default.
• W1973137274 hasAuthorship W1973137274A5056342025 @default.
• W1973137274 hasAuthorship W1973137274A5060911267 @default.
• W1973137274 hasAuthorship W1973137274A5090313381 @default.
• W1973137274 hasBestOaLocation W19731372742 @default.
• W1973137274 hasConcept C116569031 @default.
• W1973137274 hasConcept C125439840 @default.
• W1973137274 hasConcept C170493617 @default.
• W1973137274 hasConcept C185592680 @default.
• W1973137274 hasConcept C2778140631 @default.
• W1973137274 hasConcept C2779886867 @default.
• W1973137274 hasConcept C2781063702 @default.
• W1973137274 hasConcept C55493867 @default.
• W1973137274 hasConcept C71240020 @default.
• W1973137274 hasConcept C71924100 @default.
• W1973137274 hasConcept C88016717 @default.
• W1973137274 hasConcept C98274493 @default.
• W1973137274 hasConceptScore W1973137274C116569031 @default.
• W1973137274 hasConceptScore W1973137274C125439840 @default.
• W1973137274 hasConceptScore W1973137274C170493617 @default.
• W1973137274 hasConceptScore W1973137274C185592680 @default.
• W1973137274 hasConceptScore W1973137274C2778140631 @default.
• W1973137274 hasConceptScore W1973137274C2779886867 @default.
• W1973137274 hasConceptScore W1973137274C2781063702 @default.
• W1973137274 hasConceptScore W1973137274C55493867 @default.
• W1973137274 hasConceptScore W1973137274C71240020 @default.
• W1973137274 hasConceptScore W1973137274C71924100 @default.
• W1973137274 hasConceptScore W1973137274C88016717 @default.
• W1973137274 hasConceptScore W1973137274C98274493 @default.
• W1973137274 hasIssue "1" @default.
• W1973137274 hasLocation W19731372741 @default.
• W1973137274 hasLocation W19731372742 @default.
• W1973137274 hasLocation W19731372743 @default.
• W1973137274 hasLocation W19731372744 @default.
• W1973137274 hasOpenAccess W1973137274 @default.
• W1973137274 hasPrimaryLocation W19731372741 @default.
• W1973137274 hasRelatedWork W1965663693 @default.

• next