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Nashar PE, Whitfield AA, Mikusek J, et al. The Current Status of Drug Discovery for the Oxytocin Receptor. Methods Mol Biol. 2022;2384:153-174doi: 10.1007/978-1-0716-1759-5_10.
Nashar, P. E., Whitfield, A. A., Mikusek, J., & Reekie, T. A. (2022). The Current Status of Drug Discovery for the Oxytocin Receptor. Methods in molecular biology (Clifton, N.J.), 2384153-174. https://doi.org/10.1007/978-1-0716-1759-5_10
Nashar, Philippe E, et al. "The Current Status of Drug Discovery for the Oxytocin Receptor." Methods in molecular biology (Clifton, N.J.) vol. 2384 (2022): 153-174. doi: https://doi.org/10.1007/978-1-0716-1759-5_10
Nashar PE, Whitfield AA, Mikusek J, Reekie TA. The Current Status of Drug Discovery for the Oxytocin Receptor. Methods Mol Biol. 2022;2384:153-174. doi: 10.1007/978-1-0716-1759-5_10. PMID: 34550574.
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Methods Mol Biol. 2022;2384:153-174. doi: 10.1007/978-1-0716-1759-5_10.

The Current Status of Drug Discovery for the Oxytocin Receptor.

Methods in molecular biology (Clifton, N.J.)

Philippe E Nashar, Aidan A Whitfield, Jiri Mikusek, Tristan A Reekie

Affiliations

  1. Research School of Chemistry, Australian National University, Canberra, ACT, Australia.
  2. Research School of Chemistry, Australian National University, Canberra, ACT, Australia. [email protected].

PMID: 34550574 DOI: 10.1007/978-1-0716-1759-5_10

Abstract

The oxytocin receptor plays a significant role in peripheral regulation of parturition and lactation. Given this important role, multiple drug discovery programs have been conducted to develop agonists and antagonists for peripheral activity. The role of the oxytocin receptor in the central nervous system is also significant, promoting social interaction, trust, and empathy in humans. As such, molecules that can access the central nervous system and target the oxytocin receptor are of significant interest. Due to the role of the oxytocin receptor in regulating social function and psychological well-being, agonists of this receptor have considerable promise for the treatment of numerous neuropsychiatric conditions. The poor pharmacokinetic properties and blood-brain barrier penetration of peptide-based molecules means nonpeptide compounds have more commonly been the focus for central nervous system activity. This chapter aims to summarize the current standing of peptide and nonpeptide drug discovery for antagonists and agonists of the oxytocin receptor and focusses on centrally active nonpeptidic agonists.

© 2022. Springer Science+Business Media, LLC, part of Springer Nature.

Keywords: Agonist; Antagonist; Oxytocin; Oxytocin receptor; Peptide; Small molecule; Vasopressin

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