FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2041176759> ?p ?o ?g. }

• W2041176759 endingPage "82" @default.
• W2041176759 startingPage "73" @default.
• W2041176759 abstract "Inhibition of the delayed-rectifier potassium channel current, human ether-a-go-go (hERG), by pharmaceutical agents can lead to acquired long QT syndrome and the generation of potentially lethal arrhythmias and sudden death. There remains an unmet need for higher-throughput assays to screen compounds in preclinical development for the potential to block hERG and cause QT prolongation. We evaluated the rubidium efflux assay for its ability to determine block of the hERG potassium channel. hERG-transfected human embryonic kidney-293 cells were cultured on 96-well assay plates and loaded with rubidium ion by incubating in media in which potassium was replaced by 5.4 mM Rb+. Cells were exposed to test compounds and then depolarized with a K+ channel opening buffer containing 50 mM K+. The supernatant was removed, and cells were lysed using 0.1% Triton X-100. Concentration–response curves were generated for test agents by determining the Rb+ efflux using a flame atomic absorption spectrometer. Multiple trials with cisapride yielded 50% inhibitory concentration values between 308.1 ± 11 nM to 456.3 ± 24 nM for inhibition of Rb+ efflux and a Z factor of 0.80 ± 0.07 (n = 5 plates, 12 wells per plate). The values for inhibition of the hERG channel exhibited a rightward shift in potency as compared to those measured using electrophysiological techniques. In addition, we evaluated 19 blinded compounds at 10 µM in the Rb+ efflux assay, and compared results to those using patch clamp electrophysiology and the dofetilide displacement binding assay. The dofetilide displacement binding assay yielded a good correlation with electrophysiological measurements of hERG block. The rubidium efflux assay lacked sensitivity to consistently identify significant channel blockade. In conclusion, the rubidium efflux assay provides a higher-throughput means to identify potent hERG channel blocking agents, but lacks the sensitivity required to accurately determine the potency of blockade." @default.
• W2041176759 created "2016-06-24" @default.
• W2041176759 creator A5030549867 @default.
• W2041176759 creator A5038826323 @default.
• W2041176759 creator A5044218868 @default.
• W2041176759 creator A5045901294 @default.
• W2041176759 creator A5049370671 @default.
• W2041176759 creator A5084104321 @default.
• W2041176759 date "2006-02-01" @default.
• W2041176759 modified "2023-10-03" @default.
• W2041176759 title "Evaluation of the Rubidium Efflux Assay for Preclinical Identification of hERG Blockade" @default.
• W2041176759 cites W138008385 @default.
• W2041176759 cites W1963748793 @default.
• W2041176759 cites W1966746671 @default.
• W2041176759 cites W1968098810 @default.
• W2041176759 cites W1975869151 @default.
• W2041176759 cites W1976692785 @default.
• W2041176759 cites W1982022164 @default.
• W2041176759 cites W1982655809 @default.
• W2041176759 cites W1991001144 @default.
• W2041176759 cites W1995849691 @default.
• W2041176759 cites W2000392878 @default.
• W2041176759 cites W2006427735 @default.
• W2041176759 cites W2006964534 @default.
• W2041176759 cites W2007253395 @default.
• W2041176759 cites W2011345948 @default.
• W2041176759 cites W2014886686 @default.
• W2041176759 cites W2015646729 @default.
• W2041176759 cites W2015724771 @default.
• W2041176759 cites W2020935478 @default.
• W2041176759 cites W2021438486 @default.
• W2041176759 cites W2024225383 @default.
• W2041176759 cites W2025043418 @default.
• W2041176759 cites W2032734987 @default.
• W2041176759 cites W2039562809 @default.
• W2041176759 cites W2051669906 @default.
• W2041176759 cites W2063122799 @default.
• W2041176759 cites W2067647989 @default.
• W2041176759 cites W2068168026 @default.
• W2041176759 cites W2093130113 @default.
• W2041176759 cites W2094181752 @default.
• W2041176759 cites W2096495312 @default.
• W2041176759 cites W2101260051 @default.
• W2041176759 cites W2105408251 @default.
• W2041176759 cites W2107763854 @default.
• W2041176759 cites W2116843606 @default.
• W2041176759 cites W2121175754 @default.
• W2041176759 cites W2122459721 @default.
• W2041176759 cites W2125755907 @default.
• W2041176759 cites W2155422485 @default.
• W2041176759 cites W2158965509 @default.
• W2041176759 cites W2170592109 @default.
• W2041176759 cites W2507911969 @default.
• W2041176759 cites W4248937884 @default.
• W2041176759 doi "https://doi.org/10.1089/adt.2006.4.73" @default.
• W2041176759 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/16506891" @default.
• W2041176759 hasPublicationYear "2006" @default.
• W2041176759 type Work @default.
• W2041176759 sameAs 2041176759 @default.
• W2041176759 citedByCount "27" @default.
• W2041176759 countsByYear W20411767592013 @default.
• W2041176759 countsByYear W20411767592014 @default.
• W2041176759 countsByYear W20411767592015 @default.
• W2041176759 countsByYear W20411767592018 @default.
• W2041176759 countsByYear W20411767592021 @default.
• W2041176759 countsByYear W20411767592022 @default.
• W2041176759 countsByYear W20411767592023 @default.
• W2041176759 crossrefType "journal-article" @default.
• W2041176759 hasAuthorship W2041176759A5030549867 @default.
• W2041176759 hasAuthorship W2041176759A5038826323 @default.
• W2041176759 hasAuthorship W2041176759A5044218868 @default.
• W2041176759 hasAuthorship W2041176759A5045901294 @default.
• W2041176759 hasAuthorship W2041176759A5049370671 @default.
• W2041176759 hasAuthorship W2041176759A5084104321 @default.
• W2041176759 hasConcept C118441451 @default.
• W2041176759 hasConcept C12554922 @default.
• W2041176759 hasConcept C126322002 @default.
• W2041176759 hasConcept C146403970 @default.
• W2041176759 hasConcept C147944092 @default.
• W2041176759 hasConcept C170493617 @default.
• W2041176759 hasConcept C178790620 @default.
• W2041176759 hasConcept C185263204 @default.
• W2041176759 hasConcept C185592680 @default.
• W2041176759 hasConcept C200082930 @default.
• W2041176759 hasConcept C2777796741 @default.
• W2041176759 hasConcept C2778457506 @default.
• W2041176759 hasConcept C2779362680 @default.
• W2041176759 hasConcept C43617362 @default.
• W2041176759 hasConcept C517785266 @default.
• W2041176759 hasConcept C526903357 @default.
• W2041176759 hasConcept C55493867 @default.
• W2041176759 hasConcept C71924100 @default.
• W2041176759 hasConcept C83743174 @default.
• W2041176759 hasConcept C86803240 @default.
• W2041176759 hasConcept C98274493 @default.
• W2041176759 hasConceptScore W2041176759C118441451 @default.
• W2041176759 hasConceptScore W2041176759C12554922 @default.
• W2041176759 hasConceptScore W2041176759C126322002 @default.

• next