CIM0216

CIM0216, a synthetic TRPM3 ligand, acts as a potent and selective agonist of TRPM3. CIM0216 exhibits selectivity for TRPM3 over TRPM1, TRPM2 and TRPM4-8. CIM0216 acts in a TRPM3-dependent manner to induce pain and evoke neuropeptide release from sensory nerve terminals in vitro. CIM0216 is a powerful tool for studies of the physiological functions of TRPM3, and can be used for neurogenic inflammation research^[1]. In Vitro: CIM0216 elicits a dose-dependent Ca²⁺ response [pEC₅₀=0.77±0.1 µM] in HEK-TRPM3 cells, which is not observed in nontransfected HEK293 cells. CIM0216 induces a robust increase in intracellular Ca²⁺ concentration (1,145±26 nM) in single-cell FURA2-ratiometric Ca²⁺ imaging in HEK-TRPM3 cells. These responses are not observed in nontransfected HEK cells or in the absence of extracellular Ca^2+[1].
CIM0216 (10 µM) has no stimulating/blocking effect on TRPM1, TRPM4, TRPM6, or TRPM7 currents; however, a small blocking effect of CIM0216 is observed after activation of TRPM2 (16.6% block) and TRPM5 (33.5% block). CIM0216 also has no detectable effect on human TRPV1 and TRPM8 channel activation^[1].