Effects of local anesthetics and related drugs on endogenous glibenclamide-sensitive K+ channels in Xenopus oocytes.

Abstract:

: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.

journal_name

Eur J Pharmacol

authors

Yoneda I,Sakuta H,Okamoto K,Watanabe Y

doi

10.1016/0922-4106(93)90194-e

subject

Has Abstract

pub_date

1993-11-15 00:00:00

pages

267-72

issue

3

eissn

0014-2999

issn

1879-0712

journal_volume

247

pub_type

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