Research ResourcePharmacology

Subtle modifications to oxytocin produce ligands that retain potency and improved selectivity across species

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Science Signaling  05 Dec 2017:
Vol. 10, Issue 508, eaan3398
DOI: 10.1126/scisignal.aan3398

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  • Therapeutic drugs for post partum hemorrhage
    • Jorge Alberto Castañón González, Researcher, Hospital Juárez de México
    • Other Contributors:
      • Carlos Polanco, Postdoctoral Researcher, Universidad Nacional Autónoma de México

    Uterotonic drugs are widely used as prophylactic and therapeutic drugs for post partum hemorrhage, in particular uterine atony, which is the leading cause of direct maternal death worldwide. Although they are widely used, oxytocin loses potency in hot climates if not refrigerated, and the synthetic oxytocin analogue carbetocin, despite its safety profile, frequently causes reports of chest tightness, palpitations, and breathing discomfort after its administration. Also, severe bronchospasm and bradycardia have been reported after carbetocin administration, which suggests activity in cardiac conduction and muscle cells, as well as in bronchial smooth muscle (1-3). The timely article by Muttenthalen M, et al. (4), in which they identified a selective and more stable oxytocin receptor (OTR) agonist, [Se-Se]-oxytocin-OH, with improved selectivity for OTR definitively opens a much needed therapeutic window for potential clinical applications as a new uterotonic drug without activity in human cardiocites.

    Sincerely yours, Jorge Alberto Castañón González M.D., Ph.D., Candidate (*,a), Carlos Polanco, Ph.D., D.Sc. (b)

    (a) Hospital Juaréz de México, México City, México.

    (b) Universidad Nacional Autónoma de México, México City, México.

    Jorge Alberto Castañón González is a researcher at the Department of Critical Care in the Hospital Juárez...

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    Competing Interests: None declared.

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