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Abstract
Background: Oxytocin is produced primarily in hypothalamic neurons and is secreted from the posterior pituitary gland into the circulation in response to stimuli such as suckling, parturition, or stress. Oxytocin functions as an essential component in milk ejection and is among the most potent uterotonic substances known. The oxytocin receptor system supports physiological processes associated with reproduction at several levels. Objective: To characterize and evaluate oxytocin receptor ligands for therapeutic applications. Methods: Analysis of oxytocin analogs and nonpeptide oxytocin receptor ligands, and major applications of these substances. Results/conclusion: Oxytocin receptor ligands, peptides, and nonpeptide molecules, with high specificity over the related vasopressin receptors, are currently available. These ligands are expected to show therapeutic utility for a vast range of applications, e.g., increasing lactation, improving in vitro inseminations, and inducing cardiomyogenesis; and also acting against preterm labor, breast cancer, an over-reactive immune system, osteoporosis, and autism-related disorders.