Oxytocin Antagonists

Oxytocin is a clinically proven inducer of labour in pregnant women. It works as a potent stimulant of uterine contractions via the interaction with OT receptors that are expressed in myometrial cells in the mammalian female uterus. These receptors in the uterus vastly increase in number during pregnancy. The agonist oxytocin, binds to the extracellular region and transmembrane domain of the receptor, which enables the intracellular part to couple to the G proteins and initiate a cascade of events liberating Ca2+ which causes contractions [2]. Oxytocin antagonists have been shown to inhibit uterine contractions and delay preterm delivery [6]. In the last decade, the intravenously administered peptidic oxytocin antagonist atosiban (Tractocileâ„¢) [7] has been established as an acute treatment of preterm labour and interest has increased in the search for orally bioavailable, selective, non-peptide antagonists. With the discovery that oxytocin has a wide spectrum of functions outside pregnancy [4,5], interest has also developed in oxytocin antagonists as a potential treatment of sexual dysfunction including premature ejaculation and the treatment or prevention of benign prostate hyperplasia. Oxytocin antagonists have been reviewed in 1997 [8], and recently covering the literature to the end of 2004 [9], while a general review of the condition of preterm labour and treatment options was published in 2003 [10]. This section will mainly focus on recent advances reported in late 2004 and 2005 towards the design and discovery of novel orally bioavailable non-peptide antagonists and the latest improvements in peptide antagonists.

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