Besides its use in the brewing industry, hop cones appear as a powerful source of biologically active compounds, already checked for their putative anticancer, antimicrobial, and other bioactivities. Conversely, hop use in pest control remains to date under-investigated. Therefore, the biological activity of hop essential oil (EO) and its main constituents was investigated here againstSitophilus granarius. Adult contact toxicity was found 24 h after treatment with hop EO (LD50/LD(90)13.30/40.23 mu g/adult), and its three most abundant components, alpha-humulene, beta-myrcene, and beta-caryophyllene (LD50/LD(90)41.87/73.51, 75.91/126.05, and 138.51/241.27 mu g/adult, respectively); negligible variations at 48 h, except for alpha-humulene (LD50/LD(90)26.83/49.49 mu g/adult), were found. The fumigant toxicity of the EO and terpenes was also checked: in the absence of wheat grains, beta-myrcene showed the highest inhalation toxicity (LC50/LC(90)72.78/116.92 mg/L air), whereas alpha-humulene, beta-caryophyllene, and the EO induced similar values (LC50/LC(90)about 130/200 mg/L air); with the exception for EO, the wheat presence increased (30-50%) LC50/LC(90)values. Moreover, EO and terpenes were perceived by insect antennae and elicited repellent activity. Only beta-caryophyllene showed an anticholinesterase effect, this suggesting that different mechanisms of action should be responsible for hop EO toxicity. Therefore, hop EO appears suitable for developing control means against this pest.