Abstract
In the present report, we investigated the potential involvement of imidazoline I 1 and I 2 binding sites in the inhibition of the Ca 2+-activated K + channel (Gardos channel) by clotrimazole in human red cells. Ca 2+-activated 86Rb influx was inhibited by clotrimazole and efaroxan but not by the imidazoline binding site ligands clonidine, moxonidine, cirazoline and idazoxan (100 μM). Binding studies with [ 3H]idazoxan and [ 3H] p-aminoclonidine did not reveal the expression of I 1 and I 2 binding sites in erythrocytes. These data indicate that the effects of clotrimazole and efaroxan on the erythrocyte Ca 2+-activated K + channel may be mediated by a ‘non-I 1/non-I 2’ binding site.
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