Molecular Interaction of Serotonin 5-HT2A Receptor Residues Phe339(6.51) and Phe340(6.52) with Superpotent N-Benzyl Phenethylamine Agonists

@article{Braden2006MolecularIO,
  title={Molecular Interaction of Serotonin 5-HT2A Receptor Residues Phe339(6.51) and Phe340(6.52) with Superpotent N-Benzyl Phenethylamine Agonists},
  author={Michael R. Braden and J. C. Parrish and John C. Naylor and D. Nichols},
  journal={Molecular Pharmacology},
  year={2006},
  volume={70},
  pages={1956 - 1964}
}
Experiments were conducted to examine the molecular basis for the high affinity and potency of a new class of 5-HT2A receptor agonists, N-benzyl phenethylamines. Competition binding assays at several serotonin receptors confirmed that an N-arylmethyl substitution was necessary for affinity increases up to 300-fold over simple N-alkyl homologs, as well as enhanced selectivity for 5-HT2A versus 5-HT2C and 5-HT1A receptors. PI hydrolysis functional assays confirmed that these N-benzyl… Expand
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