FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2033258300> ?p ?o ?g. }

• W2033258300 endingPage "583" @default.
• W2033258300 startingPage "575" @default.
• W2033258300 abstract "Our goal was to synthesize with high specific activity R(-)-1-(2,5-Dimethoxy-4-[123I]iodophenyl)-2-aminopropane [R(-)[123I]DOI], an in vitro potent and selective 5-HT(2A/2C) serotonin agonist, and study in vivo its plasma pharmacokinetics and brain distribution in baboon by SPECT. The purpose was to evaluate this radiotracer as a potential tool in discerning the role of the agonist high affinity state of 5-HT(2) receptors in depression and other neurological disorders. The radiotracer was prepared by electrophilic radioiodination of the N-trifluoroacetyl precursor of R(-)-1-(2,5-Dimethoxyphenyl)-2-aminopropane [R(-)DMA-TFA] with high-purity sodium [123I]iodide in the presence of chloramine-T, followed by amino deprotection with KOH in isopropanol (labeling yield: 73%, radiochemical yield: 62%, radiochemical purity: 99%). In vivo studies in baboon showed high accumulation of radioactivity in thalamus, the frontoparietal cortex, temporal, occipital and the striatum regions, with slightly lower accumulation in the midbrain and cerebellum. Ketanserin did not displaced the radioactivity in any of these brain regions. Plasma metabolite analysis was performed using methanol protein precipitation, the methanol fractions contained from 68% to 92% of the mixture of a labeled metabolite and parent compound. The recovery coefficient of unmetabolized R(-)[123I]DOI was 68%. The percent parent compound present in the extracted fraction, measured by HPLC, decreased gradually with time from 99.8% to 0.3% still present after 4.7 hours post injection whereas the percentage of the only one detected metabolite increased conversely. Free fraction determination (f(1)), was 31 +/- 0.9% (n = 3). For comparison purposes, ex-vivo brain distribution, displacement and metabolite analysis was also carried out in rodents. Although R(-)[123I]DOI displayed good brain uptake and localized in serotonergic areas of the brain, its target to non target ratio and its insensitivity to ketanserin displacement suggest high nonspecific uptake, therefore non potentially useful as brain imaging radiotracer for visualization of the agonist high-affinity state of 5-HT(2A) receptors and for visualizing 5-HT(2C) receptors by SPECT." @default.
• W2033258300 created "2016-06-24" @default.
• W2033258300 creator A5037259368 @default.
• W2033258300 creator A5047401773 @default.
• W2033258300 creator A5053340431 @default.
• W2033258300 creator A5058205666 @default.
• W2033258300 creator A5084979953 @default.
• W2033258300 creator A5087635866 @default.
• W2033258300 date "2002-07-01" @default.
• W2033258300 modified "2023-09-27" @default.
• W2033258300 title "Pharmacokinetics and brain distribution in non human primate of R(-)[123I]DOI, A 5HT2A/2C serotonin agonist" @default.
• W2033258300 cites W1965303778 @default.
• W2033258300 cites W1972836962 @default.
• W2033258300 cites W1998939445 @default.
• W2033258300 cites W1999108044 @default.
• W2033258300 cites W2001522126 @default.
• W2033258300 cites W2009231298 @default.
• W2033258300 cites W2026612602 @default.
• W2033258300 cites W2028985501 @default.
• W2033258300 cites W2034005051 @default.
• W2033258300 cites W2035575808 @default.
• W2033258300 cites W2035878572 @default.
• W2033258300 cites W2043457240 @default.
• W2033258300 cites W2066190862 @default.
• W2033258300 cites W2070274847 @default.
• W2033258300 cites W2070290419 @default.
• W2033258300 cites W2080784754 @default.
• W2033258300 cites W2085549566 @default.
• W2033258300 cites W2087221664 @default.
• W2033258300 cites W2087542866 @default.
• W2033258300 cites W2131341449 @default.
• W2033258300 cites W2154371572 @default.
• W2033258300 doi "https://doi.org/10.1016/s0969-8051(02)00306-2" @default.
• W2033258300 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/12088728" @default.
• W2033258300 hasPublicationYear "2002" @default.
• W2033258300 type Work @default.
• W2033258300 sameAs 2033258300 @default.
• W2033258300 citedByCount "13" @default.
• W2033258300 countsByYear W20332583002017 @default.
• W2033258300 countsByYear W20332583002019 @default.
• W2033258300 countsByYear W20332583002021 @default.
• W2033258300 countsByYear W20332583002022 @default.
• W2033258300 crossrefType "journal-article" @default.
• W2033258300 hasAuthorship W2033258300A5037259368 @default.
• W2033258300 hasAuthorship W2033258300A5047401773 @default.
• W2033258300 hasAuthorship W2033258300A5053340431 @default.
• W2033258300 hasAuthorship W2033258300A5058205666 @default.
• W2033258300 hasAuthorship W2033258300A5084979953 @default.
• W2033258300 hasAuthorship W2033258300A5087635866 @default.
• W2033258300 hasConcept C112705442 @default.
• W2033258300 hasConcept C118552586 @default.
• W2033258300 hasConcept C134018914 @default.
• W2033258300 hasConcept C150903083 @default.
• W2033258300 hasConcept C170493617 @default.
• W2033258300 hasConcept C185592680 @default.
• W2033258300 hasConcept C207001950 @default.
• W2033258300 hasConcept C2775864247 @default.
• W2033258300 hasConcept C2777477808 @default.
• W2033258300 hasConcept C2777670902 @default.
• W2033258300 hasConcept C2777785214 @default.
• W2033258300 hasConcept C2778938600 @default.
• W2033258300 hasConcept C2779594886 @default.
• W2033258300 hasConcept C53910766 @default.
• W2033258300 hasConcept C55493867 @default.
• W2033258300 hasConcept C67847695 @default.
• W2033258300 hasConcept C71924100 @default.
• W2033258300 hasConcept C86803240 @default.
• W2033258300 hasConcept C98274493 @default.
• W2033258300 hasConceptScore W2033258300C112705442 @default.
• W2033258300 hasConceptScore W2033258300C118552586 @default.
• W2033258300 hasConceptScore W2033258300C134018914 @default.
• W2033258300 hasConceptScore W2033258300C150903083 @default.
• W2033258300 hasConceptScore W2033258300C170493617 @default.
• W2033258300 hasConceptScore W2033258300C185592680 @default.
• W2033258300 hasConceptScore W2033258300C207001950 @default.
• W2033258300 hasConceptScore W2033258300C2775864247 @default.
• W2033258300 hasConceptScore W2033258300C2777477808 @default.
• W2033258300 hasConceptScore W2033258300C2777670902 @default.
• W2033258300 hasConceptScore W2033258300C2777785214 @default.
• W2033258300 hasConceptScore W2033258300C2778938600 @default.
• W2033258300 hasConceptScore W2033258300C2779594886 @default.
• W2033258300 hasConceptScore W2033258300C53910766 @default.
• W2033258300 hasConceptScore W2033258300C55493867 @default.
• W2033258300 hasConceptScore W2033258300C67847695 @default.
• W2033258300 hasConceptScore W2033258300C71924100 @default.
• W2033258300 hasConceptScore W2033258300C86803240 @default.
• W2033258300 hasConceptScore W2033258300C98274493 @default.
• W2033258300 hasIssue "5" @default.
• W2033258300 hasLocation W20332583001 @default.
• W2033258300 hasLocation W20332583002 @default.
• W2033258300 hasOpenAccess W2033258300 @default.
• W2033258300 hasPrimaryLocation W20332583001 @default.
• W2033258300 hasRelatedWork W1492229869 @default.
• W2033258300 hasRelatedWork W1552728282 @default.
• W2033258300 hasRelatedWork W197521104 @default.
• W2033258300 hasRelatedWork W2001310902 @default.
• W2033258300 hasRelatedWork W2004556784 @default.
• W2033258300 hasRelatedWork W2056938528 @default.

• next