A structure-affinity study of the binding of 4-substituted analogs of 1-(2, 5-dimethoxyphenyl)-2-aminopropane at 5-HT2 serotonin receptors

…, M Titeler, BL Roth, EA Suba, RA Glennon

Index: Seggel; Yousif; Lyon; Titeler; Roth; Suba; Glennon Journal of Medicinal Chemistry, 1990 , vol. 33, # 3 p. 1032 - 1036

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Citation Number: 53

Abstract

With [SH] ketanserin as the radioligand, structureaffinity relationships (SAFIRs) for binding at central 5HTz serotonin receptors (rat frontal cortex) were examined for a series of 27 4- substituted 1-(2, 5dimethoxypheny1)-2-aminopropane derivatives (2, 5-DMAs). The affinity (Ki values) ranged over a span of several orders of magnitude. It appears that the lipophilic character of the 4-position substituent plays a major role in determining the affinity of these ...