Haloperidol blocks BK channels by a "foot in the door" mechanism

Abstract

Large conductance Ca2+-activated K+ (BK) channels control a range of physiological functions, and gene mutations affecting BK channel function are linked to human neurological disease. We have recently found that the widely-used opioid agonist loperamide blocks BK channel current by binding preferentially in the open pore, while it apparently dissociates from the pore after channels have closed, consistent with the idea that BK channel gating does not occur by a “trap door” mechanism (Vouga et al.