The well-known side effects of antimuscarinic drugs have focused interest on other modalities of treatment of the overactive bladder. To effectively control bladder activity, identification of suitable targets for pharmacologic intervention is necessary. Such targets may be found in the central nervous system (CNS) or peripherally. Several CNS transmitters may modulate voiding, but few drugs with a defined CNS site of action have been developed for treatment of voiding disorders. Drugs affecting gamma-aminobutyric acid, opioid, serotonin, noradrenaline, dopamine, or glutamatergic receptors and mechanisms are known to influence micturition, and potentially such drugs could be developed for clinical use. However, a selective action on the lower urinary tract may be difficult to obtain.