Presented herein are compounds that inhibit T-type Ca2+ channel activity in a cell when the cell membrane potential is about −90 mV. Preferred compounds inhibit T-type Ca2+ channel activity with an IC50 of 10 μM or less at a membrane potential of about −90 mV. Preferred compounds show selectivity for inhibiting T-type Ca2+ channel activity at about −90 mV, relative to inhibition of T-type Ca2+ channel activity at about −30 mV to −60 mV, of 10:1 or less. Also provided are methods for identifying compounds that inhibit T-type Ca2+ channel activity in a cell when the cell membrane potential is about −90 mV, and compounds identified by such methods.
