C-(4,5,6-trimethoxyindan-1-yl)methanamine: a mescaline analogue designed using a homology model of the 5-HT2A receptor.

@article{Mclean2006C456trimethoxyindan1ylmethanamineAM,
  title={C-(4,5,6-trimethoxyindan-1-yl)methanamine: a mescaline analogue designed using a homology model of the 5-HT2A receptor.},
  author={Thomas H. Mclean and James J. Chambers and Jason Charles Parrish and Michael R. Braden and Danuta Marona-Lewicka and Deborah Marie Kurrasch-Orbaugh and David E. Nichols},
  journal={Journal of medicinal chemistry},
  year={2006},
  volume={49 14},
  pages={
          4269-74
        }
}
A conformationally restricted analogue of mescaline, C-(4,5,6-trimethoxyindan-1-yl)-methanamine, was designed using a 5-HT(2A) receptor homology model. The compound possessed 3-fold higher affinity and potency than and efficacy equal to that of mescaline at the 5-HT(2A) receptor. The new analogue substituted fully for LSD in drug discrimination studies and was 5-fold more potent than mescaline. Resolution of this analogue into its enantiomers corroborated the docking experiments, showing the R… CONTINUE READING
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