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

@article{Seggel1990ASS,
  title={A structure-affinity study of the binding of 4-substituted analogues of 1-(2,5-dimethoxyphenyl)-2-aminopropane at 5-HT2 serotonin receptors.},
  author={Mark R. Seggel and M Y Yousif and Robert A. Lyon and Milt Titeler and Bryan L. Roth and Eva A. Suba and Richard A Glennon},
  journal={Journal of medicinal chemistry},
  year={1990},
  volume={33 3},
  pages={
          1032-6
        }
}
With [3H]ketanserin as the radioligand, structure-affinity relationships (SAFIRs) for binding at central 5-HT2 serotonin receptors (rat frontal cortex) were examined for a series of 27 4-substituted 1-(2,5-dimethoxyphenyl)-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 agents for 5-HT2 receptors, 2,5… 

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