Recent animal studies have resulted in newer central nervous system (CNS)-acting agents for the treatment of sexual dysfunction in men and women. CNS stimulation and control of sexual function primarily originates in the hypothalamus, medial preoptic area, and paraventricular nucleus. Neurotransmitters responsible for sexual function, such as serotonin, dopamine, and oxytocin, can be manipulated pharmacologically. Early clinical trials and use of apomorphine have shown limited success and acceptance among patients, especially after the introduction of agents with improved efficacy and tolerability such as phosphodiesterase type 5 inhibitors. Newer CNS-acting agents such as bremelanotide show significant promise in bringing to clinical practice a group of centrally acting agents to supplement the treatment of erectile dysfunction. CNS-acting agents also show promise in treating female sexual dysfunction. Further, development of selective dopamine receptor agonists, melatonin agonists, and other CNS stimulatory or inhibitory agents may lead to improved treatment of sexual dysfunction in men and women.