Benzofuran bioisosteres of hallucinogenic tryptamines

Z Tomaszewski, MP Johnson, X Huang…

Index: Tomaszewski, Zbigniew; Johnson, Michael P.; Huang, Xuemei; Nichols, David E. Journal of Medicinal Chemistry, 1992 , vol. 35, # 11 p. 2061 - 2064

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Citation Number: 41

Abstract

2-(N, N-di-n-propylamino) tetralin ([3H]-8-OH-DPAT), respectively. At the 5-HT2 receptor, the benzofurans had slightly decreased affinities, approximately one-third and one-sixth those of the indoles, for the primary amines and the tertiary amines, respectively. The benzofurans also had lower affinity at the 5-HTM receptor, but decreased only about 20-30% from that of the indole isosteres. Thus, the 5-HTM receptor is less discriminating with respect to ...