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={R. Westkaemper and R. 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… Expand
35 Citations
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.
  • 56
Reformulating a Pharmacophore for 5-HT2A Serotonin Receptor Antagonists.
  • 5
...
1
2
3
4
...

References

SHOWING 1-10 OF 79 REFERENCES
Development of a receptor-interaction model for serotonin 5-HT2 receptor antagonists. Predicting selectivity with respect to dopamine D2 receptors.
  • 32
  • Highly Influential
Approaches to molecular modeling studies and specific application to serotonin ligands and receptors
  • 24
Ketanserin analogues: the effect of structural modification on 5-HT2 serotonin receptor binding.
  • 30
Molecular modeling of serotonin, ketanserin, ritanserin and their 5-HT2C receptor interactions.
  • 49
...
1
2
3
4
5
...