Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols.

@article{Pglion2002ImprovementIT,
  title={Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols.},
  author={J L P{\'e}glion and Bertrand Goument and Nicole Despaux and Val{\'e}rie Charlot and H{\'e}l{\`e}ne Giraud and Christian Nisole and Adrian Newman-Tancredi and Anne Dekeyne and Marc L Bertrand and Patrick Genissel and Mark John Millan},
  journal={Journal of medicinal chemistry},
  year={2002},
  volume={45 1},
  pages={165-76}
}
S 15535 (1) displays a distinctive profile of agonist and antagonist (weak partial agonist) activity at pre- and postsynaptic 5-HT(1A) receptors, respectively. It has proven to be active in several models predictive of anxiolytic, antidepressant, and procognitive properties. In an attempt to increase its selectivity and metabolic stability, and guided by the results of human metabolic studies, we prepared a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols. Irrespective of the nature… CONTINUE READING