A basic understanding of the mediators and related mechanisms involved in the genital physiology of the female sexual response, and, in particular, the physiology of arousal, is paramount for the clinical practitioner whose medical knowledge and practice pertain to female sexual dysfunction. Familiarity with established and evolving scientific principles relating to female genital physiology offers insight into functional aspects as well as disturbances of function relating to the female sexual response. Improved knowledge with regard to the central and peripheral nervous system components of female genital responses, chemical mediators, including endocrine factors determining the female sexual response, and other cellular and subcellular mechanisms should advance pharmacologic management for female sexual arousal disorder.