Matches in SemOpenAlex for { <https://semopenalex.org/work/W2110667060> ?p ?o ?g. }
Showing items 1 to 85 of
85
with 100 items per page.
- W2110667060 endingPage "809" @default.
- W2110667060 startingPage "798" @default.
- W2110667060 abstract "BackgroundCNS 7056 is a new short-acting esterase-metabolized benzodiazepine. We report the first pharmacokinetic (PK) and pharmacodynamic (PD) study of CNS 7056 and its inactive metabolite CNS 7054 in sheep.MethodsThe stability of CNS 7056 in blood samples was examined ex vivo. Six sheep were prepared with physiological instrumentation, and were given doses of 0.37, 0.74, and 1.47 mg kg−1 (2 min infusion) of CNS 7056 in alternating order on separate days.ResultsCNS 7056 was degraded in warm whole sheep blood (23% over 2 h), but not in plasma or blood stored on ice. Using non-compartmental analysis (NCA), CNS 7056 had a mean (sd) clearance of 4.52 (0.96) litre min−1 and a terminal half-life of 21.3 (10.9) min. There was a rapid conversion of CNS 7056 to its metabolite CNS 7054, which had a terminal half-life of 22.5 (3.4) min. The arterial kinetics of CNS 7056 could be described by a three-compartment model, with volumes of 1.9, 3.9, and 79 litre, a clearance of 4.2 litre min−1, and inter-compartmental clearances of 2.85 and 1.44 litre min−1, while the metabolite could be described by a two-compartment model. Cardiac output was an important covariate. Sedation as measured by the alpha power band of the EEG showed rapid onset and offset. The t1/2,ke0 for sedation was 1.78 min, and the EC50 was 0.10 µg ml−1.ConclusionsCNS 7056 has PK–PD properties compatible with its potential human use as a short-acting i.v. sedative." @default.
- W2110667060 created "2016-06-24" @default.
- W2110667060 creator A5004722292 @default.
- W2110667060 creator A5013474890 @default.
- W2110667060 creator A5028000845 @default.
- W2110667060 creator A5080848550 @default.
- W2110667060 creator A5089827696 @default.
- W2110667060 date "2010-12-01" @default.
- W2110667060 modified "2023-09-27" @default.
- W2110667060 title "Pharmacokinetics and pharmacodynamics of the short-acting sedative CNS 7056 in sheep" @default.
- W2110667060 cites W1985568051 @default.
- W2110667060 cites W1986883903 @default.
- W2110667060 cites W1989148061 @default.
- W2110667060 cites W2006324425 @default.
- W2110667060 cites W2021762465 @default.
- W2110667060 cites W2022341507 @default.
- W2110667060 cites W2031407102 @default.
- W2110667060 cites W2031426306 @default.
- W2110667060 cites W2078079779 @default.
- W2110667060 cites W2078981011 @default.
- W2110667060 cites W2079200443 @default.
- W2110667060 cites W2092295114 @default.
- W2110667060 cites W2101682651 @default.
- W2110667060 cites W2122387610 @default.
- W2110667060 cites W2161451816 @default.
- W2110667060 cites W4232189731 @default.
- W2110667060 doi "https://doi.org/10.1093/bja/aeq260" @default.
- W2110667060 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/20926479" @default.
- W2110667060 hasPublicationYear "2010" @default.
- W2110667060 type Work @default.
- W2110667060 sameAs 2110667060 @default.
- W2110667060 citedByCount "34" @default.
- W2110667060 countsByYear W21106670602012 @default.
- W2110667060 countsByYear W21106670602014 @default.
- W2110667060 countsByYear W21106670602015 @default.
- W2110667060 countsByYear W21106670602016 @default.
- W2110667060 countsByYear W21106670602017 @default.
- W2110667060 countsByYear W21106670602018 @default.
- W2110667060 countsByYear W21106670602020 @default.
- W2110667060 countsByYear W21106670602021 @default.
- W2110667060 countsByYear W21106670602022 @default.
- W2110667060 countsByYear W21106670602023 @default.
- W2110667060 crossrefType "journal-article" @default.
- W2110667060 hasAuthorship W2110667060A5004722292 @default.
- W2110667060 hasAuthorship W2110667060A5013474890 @default.
- W2110667060 hasAuthorship W2110667060A5028000845 @default.
- W2110667060 hasAuthorship W2110667060A5080848550 @default.
- W2110667060 hasAuthorship W2110667060A5089827696 @default.
- W2110667060 hasBestOaLocation W21106670601 @default.
- W2110667060 hasConcept C111113717 @default.
- W2110667060 hasConcept C112705442 @default.
- W2110667060 hasConcept C126322002 @default.
- W2110667060 hasConcept C2776814716 @default.
- W2110667060 hasConcept C2777477808 @default.
- W2110667060 hasConcept C71924100 @default.
- W2110667060 hasConcept C98274493 @default.
- W2110667060 hasConceptScore W2110667060C111113717 @default.
- W2110667060 hasConceptScore W2110667060C112705442 @default.
- W2110667060 hasConceptScore W2110667060C126322002 @default.
- W2110667060 hasConceptScore W2110667060C2776814716 @default.
- W2110667060 hasConceptScore W2110667060C2777477808 @default.
- W2110667060 hasConceptScore W2110667060C71924100 @default.
- W2110667060 hasConceptScore W2110667060C98274493 @default.
- W2110667060 hasIssue "6" @default.
- W2110667060 hasLocation W21106670601 @default.
- W2110667060 hasLocation W21106670602 @default.
- W2110667060 hasOpenAccess W2110667060 @default.
- W2110667060 hasPrimaryLocation W21106670601 @default.
- W2110667060 hasRelatedWork W1492229869 @default.
- W2110667060 hasRelatedWork W1758514097 @default.
- W2110667060 hasRelatedWork W1976890451 @default.
- W2110667060 hasRelatedWork W1998356222 @default.
- W2110667060 hasRelatedWork W1998510265 @default.
- W2110667060 hasRelatedWork W2010116591 @default.
- W2110667060 hasRelatedWork W2056938528 @default.
- W2110667060 hasRelatedWork W2227061539 @default.
- W2110667060 hasRelatedWork W2594910449 @default.
- W2110667060 hasRelatedWork W2992709639 @default.
- W2110667060 hasVolume "105" @default.
- W2110667060 isParatext "false" @default.
- W2110667060 isRetracted "false" @default.
- W2110667060 magId "2110667060" @default.
- W2110667060 workType "article" @default.