Differential phospholipase C activation by phenylalkylamine serotonin 5‐HT2A receptor agonists

@article{Parrish2005DifferentialPC,
  title={Differential phospholipase C activation by phenylalkylamine serotonin 5‐HT2A receptor agonists},
  author={Jason C. Parrish and Michael R. Braden and Emily Gundy and David E. Nichols},
  journal={Journal of Neurochemistry},
  year={2005},
  volume={95}
}
Experiments compared a series of phenethylamine hallucinogens with their phenylisopropylamine analogues for binding affinity and ability to stimulate serotonin 5‐HT2A receptor‐mediated hydrolysis of phosphatidyl inositol in cells expressing cloned rat and human 5‐HT2A receptors. The (±)phenylisopropylamine analogues had significantly higher intrinsic activities for 5‐HT2A receptor‐mediated hydrolysis of phosphatidyl inositol compared to their phenethylamine analogues. With respect to the… 
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TLDR
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TLDR
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TLDR
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TLDR
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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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TLDR
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Assessment of the Roles of Serines 5.43(239) and 5.46(242) for Binding and Potency of Agonist Ligands at the Human Serotonin 5-HT2A Receptor
TLDR
Using the ergoline lysergic acid diethylamide (LSD), and a series of substituted tryptamine and phenethylamine 5-HT2A receptor agonists, it is found that Ser5.43(239) is more critical for agonist binding and function than S5.46(242), which is consistent with the functional topography and utility of the in silico-activated homology model of the h5-HT 2A receptor.
Towards a biophysical understanding of hallucinogen action
Braden, Michael Robert. Ph.D., Purdue University, May, 2007. Towards a Biophysical Understanding of Hallucinogen Action. Major Professor: David E. Nichols. The serotonin 2A (5-HT2A) receptor is
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