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Synthesis and receptor binding of 5??amino [3H] 2methyl??3??isothiazolol ([3H] thiomuscimol), a specific GABAa agonist photoaffinity label

…, SD Hurt, P Krogsgaard??Larsen

文献索引:Frolund; Ebert; Lawrence; Hurt; Krogsgaard-Larsen Journal of Labelled Compounds and Radiopharmaceuticals, 1995 , vol. 36, # 9 p. 877 - 889

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被引用次数: 6

摘要

Abstract The synthesis of tritium labelled thiomuscimol (5-amino [3 H] 2 methyl-3- isothiazolol)(7c), a specific and high-affinity agonist photoaffinity label for GABA A receptors, is described. The synthesis of 7c is based on a procedure for the preparation of 5-amino [2 H] 2 methyl-3-isothiazolol (7b). Methyl 3-ethoxyisothiazole-5-carboxylate (3), synthesized from 3-hydroxyisothiazole-5-carboxamide (1) via the corresponding methyl ester (2), was ...