Key result
Mallotoxin (rottlerin) potently activates the BK channel, shifting the conductance/voltage relationship by >100 mV and acting as a beta1 subunit mimetic.
Population
Heterologous expression system and human vascular smooth muscle cells expressing BK (SLO1) potassium channels
Design
Preclinical
Authors
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Animal data preclude clinical use; hypothesis-generating for BK-targeted excitability therapies in cardiovascular research.
Mallotoxin acts as a potent activator of the BK potassium channel, shifting its activation to a more hyperpolarized membrane potential, suggesting a novel mechanism for regulating membrane excitability.
Zakharov et al. (2005) studied this question. Mallotoxin (rottlerin) was evaluated on Activation of the large conductance voltage and Ca2+-activated K+ channel (BK). Mallotoxin (rottlerin) potently activates the BK channel, shifting the conductance/voltage relationship by >100 mV and acting as a beta1 subunit mimetic.
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