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Wiley, British Journal of Pharmacology, 8(137), p. 1269-1279, 2002

DOI: 10.1038/sj.bjp.0704978

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Effects of levobupivacaine, ropivacaine and bupivacaine on HERG channels: stereoselective bupivacaine block

This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

Levobupivacaine and ropivacaine are the pure S(−) enantiomers of N-butyl- and N-propyl-2′,6′-pipecoloxylidide, developed as less cardiotoxic alternatives to bupivacaine. In the present study, we have analysed the effects of levobupivacaine, ropivacaine and bupivacaine on HERG channels stably expressed in CHO cells.The three drugs blocked HERG channels in a concentration-, time- and state-dependent manner. Block measured at the end of 5 s pulses to −10 mV induced by 20 μM bupivacaine (52.7±2.0%, n=15) and ropivacaine (55.5±2.7%, n=13) was similar (P>0.05) and both lower than that induced by levobupivacaine (67.5±4.2%, n=11) (P