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Título

Effect of bupivacaine and a novel local anesthetic IQB-9302, on human cardiac K+ channels

AutorGonzález, Teresa CSIC ORCID; Longobardo, Mónica; Caballero, Ricardo; Delpón, Eva; Tamargo, Juan; Valenzuela, Carmen CSIC ORCID CVN
Fecha de publicación2001
EditorAmerican Society for Pharmacology and Experimental Therapeutics
CitaciónJournal of Pharmacology and Experimental Therapeutics 296(2): 573-583 (2001)
ResumenWe have studied and compared the effects of bupivacaine with those induced by a new local anesthetic, IQB-9302, on human cardiac K+ channels hKv1.5, Kv2.1, Kv4.3, and HERG. Both drugs have a close chemical structure, only differing in their N-substituent (n-butyl and cyclopropylmethyl, for bupivacaine and IQB-9302, respectively). Both drugs blocked Kv2.1, Kv4.3, and HERG channels similarly. Bupivacaine inhibited these channels by 48.6 ± 3.4, 45.4 ± 12.4, and 43.1 ± 9.1%, respectively, and IQB-9302 by 48.1 ± 3.3, 36.1 ± 3.7, and 50.3 ± 6.6%, respectively. However, bupivacaine was 2.5 times more potent than IQB-9302 to block hKv1.5 channels (EC50 = 8.9 ± 1.4 versus 21.5 ± 4.7 μM). Both drugs induced a time- and voltage-dependent block of hKv1.5 and Kv2.1 channels. Block of Kv4.3 channels induced by either drug was time- and voltage-dependent at membrane potentials coinciding with the activation of the channels. IQB-9302 produced an instantaneous block of Kv4.3 and hKv1.5 channels at the beginning of the depolarizing pulse that can be interpreted as a drug interaction with a nonconducting state. Bupivacaine and IQB-9302 induced a similar degree of block of HERG channels and induced a steep voltage-dependent decrease of the relative current. These results suggest that 1) bupivacaine and IQB-9302 block the open state of hKv1.5, Kv2.1, Kv4.3, and HERG channels; and 2) small differences at the N-substituent of these drugs do not affect the drug-induced block of Kv2.1, Kv4.3, or HERG, but specifically modify block of hKv1.5 channels.
URIhttp://hdl.handle.net/10261/79921
Identificadoresissn: 0022-3565
e-issn: 1521-0103
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