Conformationally Restricted Butyrophenones with Mixed Dopaminergic (D_2) and Serotoninergic (5-HT_<2A>) Affinities. Synthesis of 5-Aminoethyl- and 6-Aminomethyl-4-oxotetrahydroindoles as Potential Atypical

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概要

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• We describe the synthesis of 5-aminoethyl- and 6-aminomethyl-4-oxotetrahydroindoles as butyrophenone derivatives in the indole series, as potential atypical antipsychotics. The affinities of these compounds for serotonin (5-HT_<2A>) and dopamine (D_2) receptors were evaluated in vitro. The ratios of pK_i's for 5-HT_<2A>/D_2 receptors may be useful for rapid screening of new compounds and assessing potential induction of extrapyramidal symptoms; ratio values ≥1.12 (Meltzer's ratio) are predictive of an atypical antipsychotic profile. Compounds 26e (QF 0408B) and 26f (QF 0409B) showed high affinity for both D_2 and 5-HT_<2A> receptors, and their MEltzer's ratios were 1.32 and 1.17 respectively, while haloperidol showed a ratio of 0.93.

• 公益社団法人日本薬学会の論文
• 1999-05-15

著者

• Ravina Enrique

  Dpto. Quimica Organica Laboratorio De Quimica Farmaceutica Facultad De Farmacia Universidad De Santi

• MASAGUER Chiristian

  Dpto. Quimica Organica, Laboratorio de Quimica Farmaceutica, Facultad de Farmacia, Universidad de Sa

• CASARIEGO Isabel

  Dpto. Quimica Organica, Laboratorio de Quimica Farmaceutica, Facultad de Farmacia, Universidad de Sa

• Casariego Isabel

  Dpto. Quimica Organica Laboratorio De Quimica Farmaceutica Facultad De Farmacia Universidad De Santi

• Masaguer Chiristian

  Dpto. Quimica Organica Laboratorio De Quimica Farmaceutica Facultad De Farmacia Universidad De Santi

• Masaguer Christian

  Dpto. Quimica Organica, Laboratorio de Quimica Farmaceutica, Facultad de Farmacia, Universidad de Santiago

関連論文

• Conformationally Restricted Butyrophenones with Mixed Dopaminergic (D_2) and Serotoninergic (5-HT_) Affinities. Synthesis of 5-Aminoethyl- and 6-Aminomethyl-4-oxotetrahydroindoles as Potential Atypical

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