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

A more selective oxytocin receptor agonist

Oxytocin is clinically used to induce labor, and there is interest in using this peptide to treat social disorders. However, oxytocin triggers adverse cardiovascular side effects because it activates the vasopressin receptor and the oxytocin receptor. Muttenthaler et al. generated ligands based on oxytocin with subtle modifications, yielding a lead compound that was more selective for the oxytocin receptor than for the vasopressin receptors. It reduced social fear in mice and induced contractile activity in human myometrial strips without affecting cultured cardiomyocytes. Given the cross-talk between oxytocin, vasopressin, and their receptors, this compound will also be helpful in identifying effects that are solely mediated by the oxytocin receptor.

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