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Interestingly, this role has expanded in recent years and has positioned these neuropeptides as therapeutic targets for various neuropsychiatric diseases such as autism, addiction, schizophrenia, depression, and anxiety disorders. Due to the chemical-physical characteristics of these neuropeptides including short half-life, poor blood-brain barrier penetration, promiscuity for AVP and OT receptors (AVP-R, OT-R), novel ligands have been developed in recent decades. This review summarizes the role of OT and AVP in neuropsychiatric conditions, as well as the findings of different OT-R and AVP-R agonists and antagonists, used both at the preclinical and clinical level. Furthermore, we discuss their possible therapeutic potential for central nervous system (CNS) disorders.<\/jats:p>","DOI":"10.3390\/ijms222112077","type":"journal-article","created":{"date-parts":[[2021,11,8]],"date-time":"2021-11-08T08:05:16Z","timestamp":1636358716000},"page":"12077","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":35,"title":["Role of Oxytocin and Vasopressin in Neuropsychiatric Disorders: Therapeutic Potential of Agonists and Antagonists"],"prefix":"10.3390","volume":"22","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-2227-1023","authenticated-orcid":false,"given":"Valeska","family":"Cid-Jofr\u00e9","sequence":"first","affiliation":[{"name":"Centro de Investigaci\u00f3n Biom\u00e9dica y Aplicada (CIBAP), Escuela de Medicina, Facultad de Ciencias M\u00e9dicas, Universidad de Santiago de Chile (USACH), Santiago 9170022, Chile"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5954-0675","authenticated-orcid":false,"given":"Macarena","family":"Moreno","sequence":"additional","affiliation":[{"name":"Centro de Investigaci\u00f3n Biom\u00e9dica y Aplicada (CIBAP), Escuela de Medicina, Facultad de Ciencias M\u00e9dicas, Universidad de Santiago de Chile (USACH), Santiago 9170022, Chile"},{"name":"Facultad de Ciencias Sociales, Escuela de Psicolog\u00eda, Universidad Bernardo OHiggins, Santiago 8370993, Chile"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2376-990X","authenticated-orcid":false,"given":"Miguel","family":"Reyes-Parada","sequence":"additional","affiliation":[{"name":"Centro de Investigaci\u00f3n Biom\u00e9dica y Aplicada (CIBAP), Escuela de Medicina, Facultad de Ciencias M\u00e9dicas, Universidad de Santiago de Chile (USACH), Santiago 9170022, Chile"},{"name":"Facultad de Ciencias de la Salud, Universidad Aut\u00f3noma de Chile, Providencia 7500912, Chile"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5439-7547","authenticated-orcid":false,"given":"Georgina M.","family":"Renard","sequence":"additional","affiliation":[{"name":"Centro de Investigaci\u00f3n Biom\u00e9dica y Aplicada (CIBAP), Escuela de Medicina, Facultad de Ciencias M\u00e9dicas, Universidad de Santiago de Chile (USACH), Santiago 9170022, Chile"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2021,11,8]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"e00472","DOI":"10.1002\/prp2.472","article-title":"Depressive Disorders: Treatment Failures and Poor Prognosis over the Last 50 Years","volume":"7","author":"Blackburn","year":"2019","journal-title":"Pharmacol. 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