Central nervous system processes are fundamental to sexual function. Considerable progress has been made in our understanding of the neuroanatomical and neuropharmacological bases for erection. Based largely on rat models, there is adequate understanding presently of the general anatomical areas of the brain that relate to sexual function, including the medial amygdala, medial preoptic area, paraventricular nucleus, the periaqueductal gray, ventral tegmentum and others. There is also a burgeoning body of evidence implicating nitric oxide, dopamine, serotonin and oxytocin as critical central neurotransmitters involved in various aspects of sexual function. The role of dopamine, in particular, appears fundamental in the mediation of erectile responses in both animals and man. Additionally, clinical research with apomorphine, a D1/D2 agonist, has shown significant promise in improving erections in men with a wide range of erectile difficulties. Finally, a new classification matrix has been proposed for existing treatments for erectile dysfunction based upon the putative site and mechanism of action. Implications for the further development of neuropharmacological agents in this area are discussed.