About: New Synthesis and Tritium Labeling of a Selective Ligand for Studying High-Affinity gamma-Hydroxybutyrate (GHB) Binding Sites     Goto   Sponge   NotDistinct   Permalink

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  • 3-Hydroxycyclopent-1-enecarboxylic acid (HOCPCA, 1) is a potent ligand for the high-affinity GHB binding sites in the CNS. An improved synthesis of 1 together with a very efficient synthesis of [H-3]-1 is described. The radiosynthesis employs in situ generated lithium trimethoxyborotritide. Screening of 1 against different CNS targets establishes a high selectivity, and we demonstrate in vivo brain penetration. In vitro characterization of [H-3]-1 binding shows high specificity to the high-affinity GHB binding sites.
  • 3-Hydroxycyclopent-1-enecarboxylic acid (HOCPCA, 1) is a potent ligand for the high-affinity GHB binding sites in the CNS. An improved synthesis of 1 together with a very efficient synthesis of [H-3]-1 is described. The radiosynthesis employs in situ generated lithium trimethoxyborotritide. Screening of 1 against different CNS targets establishes a high selectivity, and we demonstrate in vivo brain penetration. In vitro characterization of [H-3]-1 binding shows high specificity to the high-affinity GHB binding sites. (en)
Title
  • New Synthesis and Tritium Labeling of a Selective Ligand for Studying High-Affinity gamma-Hydroxybutyrate (GHB) Binding Sites
  • New Synthesis and Tritium Labeling of a Selective Ligand for Studying High-Affinity gamma-Hydroxybutyrate (GHB) Binding Sites (en)
skos:prefLabel
  • New Synthesis and Tritium Labeling of a Selective Ligand for Studying High-Affinity gamma-Hydroxybutyrate (GHB) Binding Sites
  • New Synthesis and Tritium Labeling of a Selective Ligand for Studying High-Affinity gamma-Hydroxybutyrate (GHB) Binding Sites (en)
skos:notation
  • RIV/61388963:_____/13:00421055!RIV14-AV0-61388963
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  • I
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  • 20
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  • 91693
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  • RIV/61388963:_____/13:00421055
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  • rat-brain; acid; oxidation (en)
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  • US - Spojené státy americké
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  • [C8F977BE6C26]
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  • Journal of Medicinal Chemistry
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  • 56
http://linked.open...iv/tvurceVysledku
  • Marek, Aleš
  • Bay, T.
  • Bundgaard, C.
  • Clausen, R. P.
  • Frolund, B.
  • Kehler, J.
  • Pedersen, M. H. F.
  • Vogensen, S. B.
  • Wellendorph, P.
http://linked.open...ain/vavai/riv/wos
  • 000326259900041
issn
  • 0022-2623
number of pages
http://bibframe.org/vocab/doi
  • 10.1021/jm4011719
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