Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, 5-HT2B and 5-HT2C receptors

@article{Nelson1999ComparisonsOH,
  title={Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, 5-HT2B and 5-HT2C receptors},
  author={David L. G. Nelson and Virginia L. Lucaites and D Bradley Wainscott and Richard A Glennon},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={1999},
  volume={359},
  pages={1-6}
}
Since the classical hallucinogens were initially reported to produce their behavioral effects via a 5-HT2 agonist mechanism (i.e., the 5-HT2 hypothesis of hallucinogen action), 5-HT2 receptors have been demonstrated to represent a family of receptors that consists of three distinct subpopulations: 5-HT2A, 5-HT2B, and 5-HT2C receptors. Today, there is greater support for 5-HT2A than for 5-HT2C receptor involvement in the behavioral effects evoked by these agents. However, with the recent… 
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The results indicate the importance of defining the selectivity of pharmacological tools, which may have been over-estimated in the past, and highlights the need to find more selective agonists to investigate 5-HT2 receptor pharmacology.
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Receptor Interaction Profiles of 4-Alkoxy-Substituted 2,5-Dimethoxyphenethylamines and Related Amphetamines
TLDR
4-alkyloxy-substituted 2,5-dimethoxyamphetamines and Phenethylamines share some trends with the many other phenethylamine pharmacophore containing compounds, such as when increasing the size of the 4- substituent and increasing the lipophilicity, the affinities at the 5-HT2A/C subtype also increase, and only weak 5- HT2A or C subtype selectivities were achieved.
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