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Expert Opin Ther Pat. 2014 Jan;24(1):29-46. doi: 10.1517/13543776.2014.845168. Epub 2013 Oct 5.
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.
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.
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.
催产素是一种具有高度子宫收缩活性的九肽环状激素。催产素受体（Oxtr）在子宫和乳腺中表达最强，但也存在于大脑区域，表现出神经递质样活性。Oxtr 敲除小鼠在生育能力或性行为方面没有明显缺陷，但表现出异常的社交行为。所有这些都表明 Oxtr 可能成为治疗广泛疾病的重要治疗靶点。
本文将重点介绍 2002 年 1 月至 2013 年 5 月期间专利文献中发现和开发 Oxtr 激动剂和拮抗剂方面的重大进展。
在过去的十年中，累积的证据支持这样一种观点，即激活 Oxtr 可以对人类认知和社交行为产生积极影响。作者认为，新的激动剂和拮抗剂可能在治疗焦虑、自闭症或精神分裂症等疾病方面发挥重要作用。甚至，用于克服与分娩相关的功能障碍的较老的 Oxtr 激动剂和拮抗剂也可能对人类的社会行为产生重大影响。
