The search for an effective aphrodisiac has been a perennial pursuit of most societies throughout history. In the past decade, attention has focused increasingly on the prosexual effects of oral pharmacological agents with central neurotransmitter actions. The role of various dopaminergic, adrenergic, and serotonergic agents, in particular, has been intensively investigated in both human and animal studies. Some of these drugs have been considered for their potential role in the treatment of sexual dysfunction, while others have contributed to our understanding of basic neurophysiological processes in sexual arousal. This review provides a critical evaluation of current laboratory and clinical research on the "new aphrodisiacs," including studies in both patient populations and normal volunteers. Several conceptual and methodological problems are addressed, such as the definition and measurement of sexual response, the need to separate specific and nonspecific drug effects on sexual response, and the lack of studies in women. Although no single drug has proven to be clinically safe and reliably effective for human use, several promising candidates have been identified. Overall, research on prosexual drugs has contributed significantly to our understanding of basic mechanisms in sexual response, as well as providing new treatment options for common sexual disorders.