Clotrimazole (FB 5097), an imidazole derivative with a broad spectrum of antimycotic activity, inhibits biosynthesis of the sterol ergostol.

Intradermal injection of Clotrimazole in mice stimulates capsaicin-sensitive and mustard oil-sensitive trigeminal neurons, inducing nocifensive behavior and thermal hyperalgesia. In TRPV1 knockout mice, Clotrimazole-induced pain behavior is inhibited by the TRPV1 antagonist BCTC [1,2,3,4-tetrahydro-6-trichloromethyl-pyrimidine-2-one].

In the CRI-G1 whole-cell of a rat insulinoma cell line, Clotrimazole antagonizes ADP-ribose-activated and single-channel currents. Clotrimazole effectively and rapidly inhibits parasite growth across five different strains of the malignant malaria protozoan. In HEK-293 cells expressing recombinant human TRPM2, Clotrimazole inhibits ADP-ribose-activated currents. At 2 mM concentration, Clotrimazole completely suppresses parasite replication, resulting in the destruction of host cells. Furthermore, Clotrimazole at concentrations ranging from 3 mM to 30 mM entirely inhibits TRPM2-mediated currents.