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Synthesis of [ 3 H]‐labelled trans 4‐hydroxycrotonic acid (T‐HCA), an endogenous substance interfering with 4‐hydroxybutyrate (GHB)
Author(s) -
Schmitt Martine,
Bourguig JeanJacques,
Wermuth CamilleGeorges,
Schott Dominique,
Rousseau Bernard,
Beaucourt JeanPierre
Publication year - 1989
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580270105
Subject(s) - chemistry , enzyme , metabolism , endogeny , specific activity , stereochemistry , chemical synthesis , biochemistry , in vitro
Trans 4‐hydroxycrotonic acid (T‐HCA) has been identified in central nervous system of mammalians as a naturally occuring substance, which may compete with 4‐hydroxybutyric acid (GHB) for specific biological targets, such as high affinity binding sites, uptake systems and metabolism enzymes. T‐HCA has been tritiated at the 2,3 positions, using a multi‐step synthesis and a one‐pot reaction for the three last critical steps. Thus, T‐HCA‐[2,3‐ 3 H] was obtained with a specific radioactivity of 45 Ci/mmole (1.66 TBq/mmole) and a radiochemical purity of 97%.