Structural determinants for high 5-HT 2A receptor affinity of spiro [9, 10-dihydroanthracene]-9, 3′-pyrrolidine (SpAMDA)

…, BL Roth, RA Glennon, RB Westkaemper

Index: Peddi, Srinivas; Roth, Bryan L.; Glennon, Richard A.; Westkaemper, Richard B. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 9 p. 2279 - 2283

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Citation Number: 15

Abstract

The synthesis and 5-HT2A receptor affinities of ring altered derivatives of spiro [9, 10- dihydroanthracene]-9, 3′-pyrrolidine (4), a structurally unique tetracyclic 5-HT2A receptor antagonist, are described. The characteristics of the parent compound prove to be necessary for optimal 5-HT2A receptor affinity. However, expansion of the size of the pyrrolidine and central rings produce compounds with reasonably high 5-HT2A receptor ...