FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2168278440> ?p ?o ?g. }

• W2168278440 endingPage "27" @default.
• W2168278440 startingPage "17" @default.
• W2168278440 abstract "The beta-adrenergic receptor ligand (S)-4-(3-(2'-[18F]-fluoroethylamino)-2-hydroxypropoxy)-carbazol ((S)-[18F]-fluoroethylcarazolol) was prepared by reaction of [18F]-fluoroethylamine with the corresponding (S)-epoxide and was evaluated in rats by studying its pharmacokinetics and its binding profile both in vitro and in vivo. In vitro, (S)-fluoroethylcarazolol binds preferentially to beta-adrenoceptors (pK(i)=9.3 for beta(1) and 9.4 for beta(2)) and has less affinity to 5HT(1A) and 5HT(1D) receptors (pK(i)=6.7 and 5.2). In vivo, standard uptake values (SUVs) up to 0.63+/-0.07 in cortical regions were found after 60 min. Metabolites (90%) appeared within 10 min in plasma, whereas, in brain 70-75% parent compound was found after 60 min. Clearance from plasma occurred within 5 min. Cerebral uptake could be blocked by 'cold' fluoroethylcarazolol in every region, except medulla. Uptake was also blocked by propranolol and pindolol, but not by WAY 100635. ICI 89406 hardly lowered [18F] levels in brain. ICI 118551 reduced uptake of [18F] in cerebellum (mainly beta(2)) by 30%. Specific binding (tissue minus medulla values) in various brain regions corresponded with those observed for [18F]-fluorocarazolol (r(2)=0.95) and with in vitro beta-adrenoceptor densities (r(2)=0.76). Autoradiography using phosphor images of (S)-[18F]-fluoroethylcarazolol in rat brain showed the characteristic binding pattern of beta-antagonists, while propranolol treatment resulted in low and homogenous uptake. Regional tissue minus medulla values corresponded with in vitro beta-adrenoceptor densities (r(2)=0.77). We conclude that (S)-[18F]-fluoroethylcarazolol is a high affinity ligand that binds specifically to cerebral beta-adrenoceptors in vivo and may be of use for beta-adrenoceptor imaging in the brain with PET." @default.
• W2168278440 created "2016-06-24" @default.
• W2168278440 creator A5033663616 @default.
• W2168278440 creator A5042954317 @default.
• W2168278440 creator A5047870715 @default.
• W2168278440 creator A5067569222 @default.
• W2168278440 creator A5074439765 @default.
• W2168278440 date "2002-07-01" @default.
• W2168278440 modified "2023-09-25" @default.
• W2168278440 title "Synthesis and evaluation of (S)-[18F]-fluoroethylcarazolol for in vivo β-adrenoceptor imaging in the brain" @default.
• W2168278440 cites W1551098834 @default.
• W2168278440 cites W1970342596 @default.
• W2168278440 cites W1975514703 @default.
• W2168278440 cites W1977861565 @default.
• W2168278440 cites W1979557679 @default.
• W2168278440 cites W1980380868 @default.
• W2168278440 cites W1981097071 @default.
• W2168278440 cites W1987014128 @default.
• W2168278440 cites W1993449966 @default.
• W2168278440 cites W1999709032 @default.
• W2168278440 cites W2009648433 @default.
• W2168278440 cites W2020697786 @default.
• W2168278440 cites W2023029107 @default.
• W2168278440 cites W2025285868 @default.
• W2168278440 cites W2031400678 @default.
• W2168278440 cites W2040995606 @default.
• W2168278440 cites W2045964369 @default.
• W2168278440 cites W2062092019 @default.
• W2168278440 cites W2062631337 @default.
• W2168278440 cites W2066237947 @default.
• W2168278440 cites W2074631079 @default.
• W2168278440 cites W2078081646 @default.
• W2168278440 cites W2078627063 @default.
• W2168278440 cites W2082204063 @default.
• W2168278440 cites W2088180214 @default.
• W2168278440 cites W2091468456 @default.
• W2168278440 cites W2092589305 @default.
• W2168278440 cites W2094380189 @default.
• W2168278440 cites W2101034455 @default.
• W2168278440 cites W2103864607 @default.
• W2168278440 cites W2108178755 @default.
• W2168278440 cites W2127136273 @default.
• W2168278440 cites W2133209973 @default.
• W2168278440 cites W4243171138 @default.
• W2168278440 cites W968361956 @default.
• W2168278440 doi "https://doi.org/10.1016/s0197-0186(01)00140-1" @default.
• W2168278440 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/11918968" @default.
• W2168278440 hasPublicationYear "2002" @default.
• W2168278440 type Work @default.
• W2168278440 sameAs 2168278440 @default.
• W2168278440 citedByCount "9" @default.
• W2168278440 countsByYear W21682784402014 @default.
• W2168278440 countsByYear W21682784402020 @default.
• W2168278440 crossrefType "journal-article" @default.
• W2168278440 hasAuthorship W2168278440A5033663616 @default.
• W2168278440 hasAuthorship W2168278440A5042954317 @default.
• W2168278440 hasAuthorship W2168278440A5047870715 @default.
• W2168278440 hasAuthorship W2168278440A5067569222 @default.
• W2168278440 hasAuthorship W2168278440A5074439765 @default.
• W2168278440 hasConcept C116569031 @default.
• W2168278440 hasConcept C126322002 @default.
• W2168278440 hasConcept C134018914 @default.
• W2168278440 hasConcept C150903083 @default.
• W2168278440 hasConcept C170493617 @default.
• W2168278440 hasConcept C17291353 @default.
• W2168278440 hasConcept C185592680 @default.
• W2168278440 hasConcept C199360897 @default.
• W2168278440 hasConcept C202751555 @default.
• W2168278440 hasConcept C207001950 @default.
• W2168278440 hasConcept C2776174256 @default.
• W2168278440 hasConcept C2778151854 @default.
• W2168278440 hasConcept C2778499207 @default.
• W2168278440 hasConcept C40465926 @default.
• W2168278440 hasConcept C41008148 @default.
• W2168278440 hasConcept C55493867 @default.
• W2168278440 hasConcept C71924100 @default.
• W2168278440 hasConcept C86803240 @default.
• W2168278440 hasConcept C98274493 @default.
• W2168278440 hasConceptScore W2168278440C116569031 @default.
• W2168278440 hasConceptScore W2168278440C126322002 @default.
• W2168278440 hasConceptScore W2168278440C134018914 @default.
• W2168278440 hasConceptScore W2168278440C150903083 @default.
• W2168278440 hasConceptScore W2168278440C170493617 @default.
• W2168278440 hasConceptScore W2168278440C17291353 @default.
• W2168278440 hasConceptScore W2168278440C185592680 @default.
• W2168278440 hasConceptScore W2168278440C199360897 @default.
• W2168278440 hasConceptScore W2168278440C202751555 @default.
• W2168278440 hasConceptScore W2168278440C207001950 @default.
• W2168278440 hasConceptScore W2168278440C2776174256 @default.
• W2168278440 hasConceptScore W2168278440C2778151854 @default.
• W2168278440 hasConceptScore W2168278440C2778499207 @default.
• W2168278440 hasConceptScore W2168278440C40465926 @default.
• W2168278440 hasConceptScore W2168278440C41008148 @default.
• W2168278440 hasConceptScore W2168278440C55493867 @default.
• W2168278440 hasConceptScore W2168278440C71924100 @default.
• W2168278440 hasConceptScore W2168278440C86803240 @default.
• W2168278440 hasConceptScore W2168278440C98274493 @default.
• W2168278440 hasIssue "1" @default.

• next