Vasopressin (AVP) and oxytocin (OT) were the first biologically active peptides to be synthesized. They are two chemically very similar neurohypophyseal neuropeptides which could be involved in mood disorders. Neuropeptides, short-chain amino-acid neurotransmitters and neuromodulators, are attractive therapeutic targets for mood disorders. AVP seems to play an important role in the pathophysiology of major depression. There are both clinical and laboratory evidences suggest a role for OT as an endogenous antidepressant/anxiolytic hormone. OT release is also an important aspect of pharmacological action of SSRIs. In addition to AVP and OT, their receptors are growing off interest for psychiatric research. Vasopressin receptor antagonist might represent potential agents for the treatment of depression. A selective, nonpeptide AVP V1b receptor antagonist, SSR149415, has been characterized and is endowed with anxiolytic- and antidepressant-like properties. For the treatment of depression, Vasopressin antagonist and the related patents are also discussed in this article.