FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2314809969> ?p ?o ?g. }

• W2314809969 endingPage "7381" @default.
• W2314809969 startingPage "7367" @default.
• W2314809969 abstract "JDTic analogues 4–15 which have the hydroxyl groups replaced with other groups were synthesized and their in vitro efficacy at the μ, δ, and κ opioid receptors determined and compared to JDTic using [35S]GTPγS assays. Compounds 4, 5, 6, 13, 14, and 15 had Ke = 0.024, 0.01, 0.039, 0.02, 0.11, and 0.041 nM compared to the Ke = 0.02 nM for JDTic at the κ receptor and were highly selective for the κ receptor relative to the μ and δ opioid receptors. Unexpectedly, replacement of the 3-hydroxyl substituent of the 4-(3-hydroxyphenyl) group of JDTic with a H, F, or Cl substituent leads to potent and selective KOR antagonists. In vitro studies to determine various ADME properties combined with calculated TPSA, clogP, and logBB values suggests that the potent and selective κ opioid receptors 4, 5, 13, and 14 deserve consideration for further development toward potential drugs for CNS disorders." @default.
• W2314809969 created "2016-06-24" @default.
• W2314809969 creator A5001577561 @default.
• W2314809969 creator A5015241846 @default.
• W2314809969 creator A5032415692 @default.
• W2314809969 creator A5036778176 @default.
• W2314809969 creator A5048775903 @default.
• W2314809969 creator A5050854855 @default.
• W2314809969 creator A5058616888 @default.
• W2314809969 creator A5072992197 @default.
• W2314809969 creator A5087801455 @default.
• W2314809969 date "2014-08-25" @default.
• W2314809969 modified "2023-10-09" @default.
• W2314809969 title "Design, Synthesis, and Biological Evaluation of (3<i>R</i>)-1,2,3,4-Tetrahydro-7-hydroxy-<i>N</i>-[(1<i>S</i>)-1-[[(3<i>R</i>,4<i>R</i>)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) Analogues: In Vitro Pharmacology and ADME Profile" @default.
• W2314809969 cites W1490652616 @default.
• W2314809969 cites W1963557453 @default.
• W2314809969 cites W1964695406 @default.
• W2314809969 cites W1980320291 @default.
• W2314809969 cites W1988423754 @default.
• W2314809969 cites W1997780054 @default.
• W2314809969 cites W1998364591 @default.
• W2314809969 cites W2000392878 @default.
• W2314809969 cites W2007376383 @default.
• W2314809969 cites W2010158373 @default.
• W2314809969 cites W2010222907 @default.
• W2314809969 cites W2014055152 @default.
• W2314809969 cites W2014829336 @default.
• W2314809969 cites W2015615284 @default.
• W2314809969 cites W2016634408 @default.
• W2314809969 cites W2021431618 @default.
• W2314809969 cites W2023924110 @default.
• W2314809969 cites W2024791543 @default.
• W2314809969 cites W2028747491 @default.
• W2314809969 cites W2031438476 @default.
• W2314809969 cites W2031553055 @default.
• W2314809969 cites W2053745640 @default.
• W2314809969 cites W2054092950 @default.
• W2314809969 cites W2062407720 @default.
• W2314809969 cites W2064105524 @default.
• W2314809969 cites W2071801806 @default.
• W2314809969 cites W2074473216 @default.
• W2314809969 cites W2074631079 @default.
• W2314809969 cites W2078811884 @default.
• W2314809969 cites W2090267505 @default.
• W2314809969 cites W2092710687 @default.
• W2314809969 cites W2117024164 @default.
• W2314809969 cites W2134344823 @default.
• W2314809969 cites W2162194843 @default.
• W2314809969 cites W2170190816 @default.
• W2314809969 cites W2174767736 @default.
• W2314809969 cites W2313091937 @default.
• W2314809969 cites W2325883349 @default.
• W2314809969 cites W2334557001 @default.
• W2314809969 cites W4255010565 @default.
• W2314809969 cites W4322696862 @default.
• W2314809969 doi "https://doi.org/10.1021/jm5008177" @default.
• W2314809969 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4161151" @default.
• W2314809969 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/25133923" @default.
• W2314809969 hasPublicationYear "2014" @default.
• W2314809969 type Work @default.
• W2314809969 sameAs 2314809969 @default.
• W2314809969 citedByCount "21" @default.
• W2314809969 countsByYear W23148099692015 @default.
• W2314809969 countsByYear W23148099692016 @default.
• W2314809969 countsByYear W23148099692017 @default.
• W2314809969 countsByYear W23148099692018 @default.
• W2314809969 countsByYear W23148099692020 @default.
• W2314809969 countsByYear W23148099692021 @default.
• W2314809969 crossrefType "journal-article" @default.
• W2314809969 hasAuthorship W2314809969A5001577561 @default.
• W2314809969 hasAuthorship W2314809969A5015241846 @default.
• W2314809969 hasAuthorship W2314809969A5032415692 @default.
• W2314809969 hasAuthorship W2314809969A5036778176 @default.
• W2314809969 hasAuthorship W2314809969A5048775903 @default.
• W2314809969 hasAuthorship W2314809969A5050854855 @default.
• W2314809969 hasAuthorship W2314809969A5058616888 @default.
• W2314809969 hasAuthorship W2314809969A5072992197 @default.
• W2314809969 hasAuthorship W2314809969A5087801455 @default.
• W2314809969 hasBestOaLocation W23148099691 @default.
• W2314809969 hasConcept C114373084 @default.
• W2314809969 hasConcept C170493617 @default.
• W2314809969 hasConcept C185592680 @default.
• W2314809969 hasConcept C202751555 @default.
• W2314809969 hasConcept C2778689049 @default.
• W2314809969 hasConcept C2779886867 @default.
• W2314809969 hasConcept C2781063702 @default.
• W2314809969 hasConcept C55493867 @default.
• W2314809969 hasConcept C69366308 @default.
• W2314809969 hasConcept C71240020 @default.
• W2314809969 hasConceptScore W2314809969C114373084 @default.
• W2314809969 hasConceptScore W2314809969C170493617 @default.
• W2314809969 hasConceptScore W2314809969C185592680 @default.
• W2314809969 hasConceptScore W2314809969C202751555 @default.
• W2314809969 hasConceptScore W2314809969C2778689049 @default.
• W2314809969 hasConceptScore W2314809969C2779886867 @default.
• W2314809969 hasConceptScore W2314809969C2781063702 @default.
• W2314809969 hasConceptScore W2314809969C55493867 @default.
• W2314809969 hasConceptScore W2314809969C69366308 @default.

• next