Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists andTrp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonistsas well as methods for identifying and characterizing novel small-molecule Trp-p8modulators and methods for decreasing viability and/or inhibiting growth ofTrp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx,methods for stimulating apoptosis and/or necrosis, and related methods forthe treatment of diseases, including cancers such as lung, breast, colon, and/orprostate cancers as well as other diseases, such as benign prostatic hyperplasia, thatare associated with Trp-p8 expression.