Investigation of pyrazolo-sulfonamides as putative small molecule oxytocin receptor agonists

Timothy A. Katte, Tristan A. Reekie, Eryn L. Werry, William T. Jorgensen, Rochelle Boyd, Erick C. N. Wong, Damien W. Gulliver, Mark Connor, Michael Kassiou*

*Corresponding author for this work

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

The neuropeptide oxytocin has been implicated in multiple central nervous system functions in mammalian species. Increased levels have been reported to improve trust, alleviate symptoms related to autism and social phobias, and reduce social anxiety. Hoffman-La Roche published a patent claiming to have found potent small molecule oxytocin receptor agonists, smaller than the first non-peptide oxytocin agonist reported, WAY 267,464. We selected two of the more potent compounds from the patent and, in addition, created WAY 267,464 hybrid structures and determined their oxytocin and vasopressin receptor activity. Human embryonic kidney and Chinese hamster ovary cells were used for the expression of oxytocin or vasopressin 1a receptors and activity assessed via IP1 accumulation assays and calcium FLIPR assays. The results concluded that the reported compounds in the patent and the hybrid structures have no activity at the oxytocin or vasopressin 1a receptors.

Original languageEnglish
Pages (from-to)330-333
Number of pages4
JournalEuropean Journal of Medicinal Chemistry
Volume136
DOIs
Publication statusPublished - 18 Aug 2017

Keywords

  • Oxytocin agonists
  • Small molecule
  • Sulfonamide

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    Katte, T. A., Reekie, T. A., Werry, E. L., Jorgensen, W. T., Boyd, R., Wong, E. C. N., ... Kassiou, M. (2017). Investigation of pyrazolo-sulfonamides as putative small molecule oxytocin receptor agonists. European Journal of Medicinal Chemistry, 136, 330-333. https://doi.org/10.1016/j.ejmech.2017.05.013