Conformationally Restricted Butyrophenones with Mixed Dopaminergic (D2) and Serotoninergic (5-HT2A) Affinities. Synthesis of 5-Aminoethyl and 6-Aminomethyl-4- …

CF MASAGUER, I Casariego, E Ravina

Index: Masaguer, Christian F.; Casariego, Isabel; Ravina, Enrique Chemical and Pharmaceutical Bulletin, 1999 , vol. 47, # 5 p. 621 - 632

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Citation Number: 13

Abstract

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 ...