Vasopressin and oxytocin are primarily synthesized in the magnocellular supraoptic and paraventricular nuclei of the hypothalamus and transported to the posterior pituitary. In the human, an extensive accessory magnocellular neuroendocrine system is present with contact to the posterior pituitary and blood vessels in the hypothalamus itself. Vasopressin and oxytocin are involved in social and behavioral functions. However, only few neocortical areas are targeted by vasopressinergic and oxytocinergic nerve fibers, which mostly project to limbic areas in the forebrain, where also their receptors are located. Vasopressinergic/oxytocinergic perikarya in the forebrain project to the brain stem and spinal cord targeting nuclei and areas involved in autonomic functions. Parvocellular neurons containing vasopressin are located in the suprachiasmatic nucleus and synchronize the activity of the pacemaker in this nucleus. From the suprachiasmatic nucleus fibers project to the parvocellular part of the paraventricular nucleus, where preautonomic neurons project to the intermediolateral nucleus in the thoracic spinal cord, from where the superior cervical ganglion is reached whose noradrenergic fibers terminate in the pineal gland to stimulate melatonin secretion at night. The pineal gland is also innervated by vasopressin- and oxytocin-containing fibers reaching the gland via the “central innervation” in the pineal stalk, which might be involve in an annual regulation of melatonin secretion.