Recently, catnip, Nepeta cataria L. (Lamiaceae), essential oil has been formulated and marketed as an alternative repellent for protection against biting arthropods by several vendors. We isolated the major active components of catnip oil, E,Z- and Z,E-nepetalactone, and quantitatively measured their antibiting efficacy compared with the repellents N,N-diethyl-3-methylbenzamide (deet) and chiral (1S,2′S)-2-methylpiperidinyl-3-cyclohexene-1-carboxamide (SS220) against the yellowfever mosquito, Aedes aegypti (L.), by using an in vitro assay and human volunteers at 24 nmol compound/cm² (cloth or skin). Of all compounds tested in an in vitro assay, SS220 ranked as the most effective, whereas catnip oil and the nepetalactone compounds did not differ significantly from each other or from deet. However, in human volunteer bioassays, neither E,Z and Z,E-nepetalactone nor racemic nepetalactone deterred mosquito biting as effectively as SS220 or deet. All compounds differed significantly from the control. We conclude that catnip oil and nepetalactone isomers are significantly less effective than deet or SS220 in deterring the biting of Ae. aegypti.