FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1821708052> ?p ?o ?g. }

• W1821708052 endingPage "914" @default.
• W1821708052 startingPage "904" @default.
• W1821708052 abstract "Recent studies have shown that sigma-1 receptor orthodox agonists can inhibit neuroinflammation. SKF83959 (3-methyl-6-chloro-7,8-hydroxy-1-[3-methylphenyl]-2,3,4,5-tetrahydro-1H-3-benzazepine), an atypical dopamine receptor-1 agonist, has been recently identified as a potent allosteric modulator of sigma-1 receptor. Here, we investigated the anti-inflammatory effects of SKF83959 in lipopolysaccharide (LPS)-stimulated BV2 microglia. Our results indicated that SKF83959 significantly suppressed the expression/release of the pro-inflammatory mediators, such as tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), inducible nitric oxide synthase (iNOS), and inhibited the generation of reactive oxygen species. All of these responses were blocked by selective sigma-1 receptor antagonists (BD1047 or BD1063) and by ketoconazole (an inhibitor of enzyme cytochrome c17 to inhibit the synthesis of endogenous dehydroepiandrosterone, DHEA). Additionally, we found that SKF83959 promoted the binding activity of DHEA with sigma-1 receptors, and enhanced the inhibitory effects of DHEA on LPS-induced microglia activation in a synergic manner. Furthermore, in a microglia-conditioned media system, SKF83959 inhibited the cytotoxicity of conditioned medium generated by LPS-activated microglia toward HT-22 neuroblastoma cells. Taken together, our study provides the first evidence that allosteric modulation of sigma-1 receptors by SKF83959 inhibits microglia-mediated inflammation. SKF83959 is a potent allosteric modulator of sigma-1 receptor. Our results indicated that SKF83959 enhanced the activity of endogenous dehydroepiandrosterone (DHEA) in a synergic manner, and inhibited the activation of BV2 microglia and the expression/release of the pro-inflammatory mediators, such as tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), inducible nitric oxide synthase (iNOS)." @default.
• W1821708052 created "2016-06-24" @default.
• W1821708052 creator A5009833697 @default.
• W1821708052 creator A5016577575 @default.
• W1821708052 creator A5080479959 @default.
• W1821708052 creator A5080696164 @default.
• W1821708052 creator A5085155028 @default.
• W1821708052 creator A5088829033 @default.
• W1821708052 date "2015-06-19" @default.
• W1821708052 modified "2023-10-17" @default.
• W1821708052 title "Allosteric modulation of sigma-1 receptors by SKF83959 inhibits microglia-mediated inflammation" @default.
• W1821708052 cites W1536787393 @default.
• W1821708052 cites W1673643619 @default.
• W1821708052 cites W1915946375 @default.
• W1821708052 cites W1967720787 @default.
• W1821708052 cites W1969176034 @default.
• W1821708052 cites W1972010974 @default.
• W1821708052 cites W1976917710 @default.
• W1821708052 cites W1980430640 @default.
• W1821708052 cites W1981373150 @default.
• W1821708052 cites W1981909057 @default.
• W1821708052 cites W1986948791 @default.
• W1821708052 cites W1990990523 @default.
• W1821708052 cites W2003129702 @default.
• W1821708052 cites W2006841841 @default.
• W1821708052 cites W2012753124 @default.
• W1821708052 cites W2012940091 @default.
• W1821708052 cites W2013715494 @default.
• W1821708052 cites W2023998778 @default.
• W1821708052 cites W2027467386 @default.
• W1821708052 cites W2029283970 @default.
• W1821708052 cites W2030215768 @default.
• W1821708052 cites W2032237444 @default.
• W1821708052 cites W2036968390 @default.
• W1821708052 cites W2037874188 @default.
• W1821708052 cites W2047645758 @default.
• W1821708052 cites W2052981250 @default.
• W1821708052 cites W2055487345 @default.
• W1821708052 cites W2074649788 @default.
• W1821708052 cites W2075762292 @default.
• W1821708052 cites W2077727405 @default.
• W1821708052 cites W2082448556 @default.
• W1821708052 cites W2084263537 @default.
• W1821708052 cites W2090515281 @default.
• W1821708052 cites W2092015384 @default.
• W1821708052 cites W2093330856 @default.
• W1821708052 cites W2103479914 @default.
• W1821708052 cites W2106105150 @default.
• W1821708052 cites W2108730203 @default.
• W1821708052 cites W2113902650 @default.
• W1821708052 cites W2127936752 @default.
• W1821708052 cites W2130833418 @default.
• W1821708052 cites W2158988264 @default.
• W1821708052 doi "https://doi.org/10.1111/jnc.13182" @default.
• W1821708052 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26031312" @default.
• W1821708052 hasPublicationYear "2015" @default.
• W1821708052 type Work @default.
• W1821708052 sameAs 1821708052 @default.
• W1821708052 citedByCount "55" @default.
• W1821708052 countsByYear W18217080522016 @default.
• W1821708052 countsByYear W18217080522017 @default.
• W1821708052 countsByYear W18217080522018 @default.
• W1821708052 countsByYear W18217080522019 @default.
• W1821708052 countsByYear W18217080522020 @default.
• W1821708052 countsByYear W18217080522021 @default.
• W1821708052 countsByYear W18217080522022 @default.
• W1821708052 countsByYear W18217080522023 @default.
• W1821708052 crossrefType "journal-article" @default.
• W1821708052 hasAuthorship W1821708052A5009833697 @default.
• W1821708052 hasAuthorship W1821708052A5016577575 @default.
• W1821708052 hasAuthorship W1821708052A5080479959 @default.
• W1821708052 hasAuthorship W1821708052A5080696164 @default.
• W1821708052 hasAuthorship W1821708052A5085155028 @default.
• W1821708052 hasAuthorship W1821708052A5088829033 @default.
• W1821708052 hasBestOaLocation W18217080521 @default.
• W1821708052 hasConcept C103133801 @default.
• W1821708052 hasConcept C126322002 @default.
• W1821708052 hasConcept C134018914 @default.
• W1821708052 hasConcept C166342909 @default.
• W1821708052 hasConcept C170493617 @default.
• W1821708052 hasConcept C178790620 @default.
• W1821708052 hasConcept C17991360 @default.
• W1821708052 hasConcept C185592680 @default.
• W1821708052 hasConcept C2776038425 @default.
• W1821708052 hasConcept C2776914184 @default.
• W1821708052 hasConcept C2776992908 @default.
• W1821708052 hasConcept C2777052854 @default.
• W1821708052 hasConcept C2777622882 @default.
• W1821708052 hasConcept C2777911890 @default.
• W1821708052 hasConcept C2778938600 @default.
• W1821708052 hasConcept C2779830541 @default.
• W1821708052 hasConcept C519581460 @default.
• W1821708052 hasConcept C55493867 @default.
• W1821708052 hasConcept C71315377 @default.
• W1821708052 hasConcept C71924100 @default.
• W1821708052 hasConcept C86803240 @default.
• W1821708052 hasConcept C98274493 @default.
• W1821708052 hasConceptScore W1821708052C103133801 @default.

• next