Oxytocin Agonists

Although not strictly within the scope of this review, it is interesting to note that Ferring has recently reported on the properties of a non-peptidic series of oxytocin agonists. The authors envisage that the compounds may be of value in providing an oral alternative to the current practice of intravenously administered oxytocin for the induction of labour and may also have a role in the treatment of male erectile dysfunction, presumably based on the part oxytocin is believed to play in the regulation of male and female sexual activity. Selectivity for oxytocin over vasopressin V2 has been a problem with this series, but success was obtained with compound (59), which has an oxytocin agonist EC50 of 33 nM and a 25-fold selectivity versus vasopressin V2 [118, 119]. Related compounds from this series have been claimed in a recent patent and are reported to be oxytocin agonists and vasopressin V1a antagonists [120, 121].

(58) OPC-31260

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