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Synthesis and in vi...
Synthesis and in vitro evaluation of 18F-β-carboline alkaloids as PET ligands
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- Blom, Elisabeth, 1979- (author)
- Uppsala universitet,Institutionen för biokemi och organisk kemi,Bengt Långström
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- Karimi, Farhad (author)
- Uppsala universitet,Institutionen för biokemi och organisk kemi
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- Eriksson, Olof (author)
- Uppsala universitet,Institutionen för onkologi, radiologi och klinisk immunologi
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Hall, Håkan (author)
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- Långström, Bengt (author)
- Uppsala universitet,Institutionen för biokemi och organisk kemi,Bengt Långström
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(creator_code:org_t)
- 2008
- 2008
- English.
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In: Journal of labelled compounds & radiopharmaceuticals. - : Wiley. - 0362-4803 .- 1099-1344. ; 51:6, s. 277-282
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- A one-step 18F-labelling strategy was used to prepare four 18F-labelled analogues of 7-methoxy-1-methyl-9H-β-carboline (harmine): 7-(2-[18F]fluoroethoxy)-1-methyl-9H-β-carboline (5), 7-(3-[18F]fluoro-propoxy)-1-methyl-9H-β-carboline (6), 7-[2-(2-[18F]fluoroethoxy)ethoxy]-1-methyl-9H-β-carboline (7), and 7-{2-[2-(2-[18F]fluoroethoxy)ethoxy]-ethoxy}-1-methyl-9H-β-carboline (8). These were synthesized as potential PET ligands for monoamine oxidase A. A solution of pure labelled compound in buffer was obtained in < 70 min from end of radionuclide production, with a decay-corrected yield of up to 23%. The average specific binding to MAO-A in rat brain, determined by autoradiography experiments, was highest for compounds 7 and 8 (89 ± 2 and 96 ± 1% respectively), which was obtained at < 1 nM radioligand concentration.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Andra medicinska och farmaceutiska grundvetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Other Basic Medicine (hsv//eng)
Keyword
- Harmine anologues
- nucleophilic 18F-fluorination
- one-step labelling
- b-carboline alkaloids
- MAO-A
- Chemistry
- Kemi
Publication and Content Type
- ref (subject category)
- art (subject category)
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