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XB-ART-21992
Eur J Pharmacol 1993 Nov 15;2473:267-72. doi: 10.1016/0922-4106(93)90194-e.
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Effects of local anesthetics and related drugs on endogenous glibenclamide-sensitive K+ channels in Xenopus oocytes.

Yoneda I , Sakuta H , Okamoto K , Watanabe Y .


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Effects of local anesthetics and structurally related drugs on the glibenclamide-sensitive K+ currents evoked by Y-26763 (a K+ channel opener) were investigated in native Xenopus oocytes. The K+ current induced by Y-26763 (100 microM) was reversibly suppressed by all six local anesthetics tested in a concentration-dependent manner with the rank order of potencies (IC50 in microM): bupivacaine (67) > dibucaine (136) > tetracaine (845) > lidocaine (1710) = mepivacaine (1945) > procaine (3112). (+)-Propranolol and mexiletine also suppressed Y-26763-induced K+ currents with IC50 values of 115 microM and 789 microM, respectively. These results suggest that a suppressive action on glibenclamide-sensitive K+ channels is the common property of local anesthetics.

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