Novel oxytocin receptor agonists and antagonists: a patent review (2002 – 2013)

Introduction: Oxytocin is a nine amino acid cyclic peptide hormone with a high degree of uterotonic activity. The oxytocin receptor (Oxtr) is most strongly expressed in the uterus and mammary gland, but can also be found in regions of the brain, showing a neurotransmitter-like activity. The Oxtr knockout mice have no obvious defects in fertility or sexual behavior, but display aberrant social behavior. All of these suggest that Oxtr may become an important therapeutic target for the treatment of a wide range of conditions.<p></p> Areas covered: This article will highlight the significant progress that has been made in the discovery and development of Oxtr agonists and antagonists in the patent literature between January 2002 and May 2013.<p></p> Expert opinion: In the past decade, cumulative evidence supports the idea that activation of the Oxtr can have a positive effect upon human cognition and social behavior. The authors suggest that new agonists and antagonists may play an important role in the treatment of disorders such as anxiety, autism or schizophrenia. It may even be that older Oxtr agonists and antagonists, which were used to overcome labor-related dysfunction, may also have a significant impact on human social behavior.<p>