NS11021 is a potent and specific activator of large-conductance Ca2+-activated potassium channels (BKCa/KCa1.1).
NS11021 activates KCa1.1 in a concentration-dependent manner by parallelshifting the channel activation curves to more negative potentials at >0.3 uM.
NS11021 increased the open probability of the channel by altering gating kinetics without affecting the single-channel conductance.
NS11021 influenced neither a number of cloned Kv channels nor endogenous Na(+) and Ca(2+) channels (L- and T-type) in guinea pig cardiac myocytes.
NS11021 displayed better specificity and a 10 times higher potency compared with the most broadly applied KCa1.1 opener, NS1619.
NS11021 leads to relaxation of both intracavernous arteries and corpus cavernosum strips primarily through opening of BK(Ca) channels.
