Nelotanserin, a Novel Selective Human 5-Hydroxytryptamine2A Inverse Agonist for the Treatment of Insomnia

@article{AlShamma2010NelotanserinAN,
  title={Nelotanserin, a Novel Selective Human 5-Hydroxytryptamine2A Inverse Agonist for the Treatment of Insomnia},
  author={Hussien A. Al-Shamma and Christen M. Anderson and Emil Chuang and R{\'e}my Luthringer and Andrew J Grottick and Erin K Hauser and Michael E. Morgan and William R. Shanahan and Bradley R. Teegarden and William J. Thomsen and Dominic P. Behan},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2010},
  volume={332},
  pages={281 - 290}
}
5-Hydroxytryptamine (5-HT)2A receptor inverse agonists are promising therapeutic agents for the treatment of sleep maintenance insomnias. Among these agents is nelotanserin, a potent, selective 5-HT2A inverse agonist. Both radioligand binding and functional inositol phosphate accumulation assays suggest that nelotanserin has low nanomolar potency on the 5-HT2A receptor with at least 30- and 5000-fold selectivity compared with 5-HT2C and 5-HT2B receptors, respectively. Nelotanserin dosed orally… 

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