Synthesis and pharmacology of the enantiomers of the potential atypical antipsychotic agents 5-OMe-BPAT and 5-OMe-(2, 6-di-OMe)-BPAT

EJ Homan, S Copinga, L Unelius, DM Jackson…

Index: Homan, Evert J.; Copinga, Swier; Unelius, Lena; Jackson, David M.; Wikstroem, Hkan V.; Grol, Cor J. Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 7 p. 1263 - 1271

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Citation Number: 10

Abstract

The optically pure enantiomers of the potential atypical antipsychotic agents 5-methoxy-2-[N- (2-benzamidoethyl)-Nn-propylamino] tetralin (5-OMe-BPAT, 5) and 5-methoxy-2-{N-[2-(2, 6- dimethoxy) benzamidoethyl]-Nn-propylamino} tetralin [5-OMe-(2, 6-di-OMe)-BPAT, 6] were synthesized and evaluated for their in vitro binding affinities at α1-, α2-, and β-adrenergic, muscarinic, dopamine D1, D2A, and D3, and serotonin 5-HT1A and 5-HT2 receptors. In ...