Application of ligand SAR, receptor modeling and receptor mutagenesis to the discovery and development of a new class of 5-HT(2A) ligands.

@article{Westkaemper2002ApplicationOL,
  title={Application of ligand SAR, receptor modeling and receptor mutagenesis to the discovery and development of a new class of 5-HT(2A) ligands.},
  author={Richard B. Westkaemper and Richard A Glennon},
  journal={Current topics in medicinal chemistry},
  year={2002},
  volume={2 6},
  pages={
          575-98
        }
}
The present review describes our approach to the development of a structurally unique class of 5-HT(2A) ligands. On the basis of an abbreviated graphics model of a 5-HT(2A) serotonin receptor, it was hypothesized that introduction of an additional aromatic ring might enhance the affinity of phenylethylamine (an agent that lacks significant affinity for the 5-HT(2A) receptors). Continued work with such structures, and the continual refinement of graphics receptor models, ultimately led to the… 

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