Benzocaine enhances and inhibits the K+ current through a human cardiac cloned channel (Kv1.5)

Cardiovascular Research

Volumn 42, Issue 2, 1999, Pages 510-520

  Delpón, Eva ^a   Caballero, Ricardo ^a   Valenzuela, Carmen ^a   Longobardo, Mónica ^a   Snyders, Dirk ^b   Tamargo, Juan ^a  

^a UNIVERSIDAD COMPLUTENSE DE MADRID   (Spain)

^b Laboratory for Molecular Biophysics   (Belgium)

Author keywords

Benzocaine; Drug channel interactions; K+ channels; Local anesthetic; Mouse

Indexed keywords

BENZOCAINE; DEXAMETHASONE; DIMETHYL SULFOXIDE; POTASSIUM; POTASSIUM CHANNEL;

ALLOSTERISM; ANIMAL CELL; ARTICLE; CHANNEL GATING; CONTROLLED STUDY; DRUG BINDING SITE; DRUG EFFECT; MOLECULAR CLONING; MOUSE; NONHUMAN; PATCH CLAMP; POTASSIUM CELL LEVEL; POTASSIUM CONDUCTANCE; POTASSIUM CURRENT; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN ISOLATION;

ANALYSIS OF VARIANCE; ANESTHETICS, LOCAL; BENZOCAINE; BIOLOGICAL TRANSPORT, ACTIVE; CLONING, MOLECULAR; HUMANS; ION CHANNEL GATING; ION TRANSPORT; KV1.5 POTASSIUM CHANNEL; MYOCARDIUM; PATCH-CLAMP TECHNIQUES; POTASSIUM; POTASSIUM CHANNELS; POTASSIUM CHANNELS, VOLTAGE-GATED; PROTEIN BINDING; TIME FACTORS;

EID: 0032977686     PISSN: 00086363     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0008-6363(99)00043-7     Document Type: Article

References (25)

1. Hille B. Local anesthetics: hydrophilic and hydrophobic pathways for the drug receptor reaction. J Gen Physiol. 69:1977;497-515.
2. Valenzuela C., Delpón E., Tamkun M.M., Tamargo J., Snyders D.J. Stereoselective block of a human cardiac potassium channel (Kv1.5) by bupivacaine enantiomers. Biophys J. 69:1995;418-427.
3. Valenzuela C., Delpón E., Franqueza L., et al. Effects of ropivacaine on a potassium channel (hKv1.5) cloned from human ventricle. Anesthesiology. 86:1997;718-728.
4. Longobardo M., Delpón E., Caballero R., Tamargo J., Valenzuela C. Structural determinants of potency and stereoselective block of hKv1.5 channels induced by local anesthetics. Mol Pharmacol. 54:1998;162-169.
5. + current similar to Kv1.5 cloned channel currents. Circ Res. 73:1993;1061-1076.
6. Armstrong C.M. Interaction of tetraethylammonium ion derivatives with the potassium channels of giant axons. J Gen Physiol. 58:1971;413-437.
7. Snyders D.J., Yeola S.W. Determinants of antiarrhythmic drug action: electrostatic and hydrophobic components of block of the human cardiac hKv1.5 channel. Circ Res. 77:1995;575-583.
8. + channel. Role of S6 in antiarrhythmic drug binding. Circ Res. 78:1996;1105-1114.
9. Franqueza L., Longobardo M., Vicente J., et al. Molecular determinants of stereoselective bupivacaine block of hKv1.5 channels. Circ Res. 81:1997;1053-1064.
10. Snyders D., Tamkun M.M., Bennett P.B. A rapidly activating and slowly inactivating potassium channel cloned from human heart. J Gen Physiol. 101:1993;513-543.
11. + channels: state-dependent interactions. J Gen Physiol. 103:1994;501-518.
12. Hoshi T., Zagotta W.N., Aldrich R.W. Biophysical and molecular mechanisms of Shaker potassium channel inactivation. Science. 250:1990;533-538.
13. + channels. Proc Natl Acad Sci USA. 88:1991;5092-5095.
14. López-Barneo J., Hoshi T., Heinemann S.H., Aldrich R.W. Effects of external cations and mutations in the pore region on C-type inactivation of Shaker potassium channels. Recept Channels. 1:1993;61-71.
15. + channels. Circ Res. 82:1998;739-750.
16. + channels. Proc Natl Acad Sci USA. 93:1996;13357-13361.
17. Rich T.C., Snyders D.J. Evidence for multiple open and inactivated states of the hKv1.5 delayed rectifier. Biophys J. 75:1998;183-195.
18. + channel deactivation. J Gen Physiol. 110:1997;87-100.
19. Zhang X., Anderson J.W., Fedida D. Characterization of nifedipine block of the human heart delayed rectifier, hKv1.5. J Pharmacol Exp Ther. 281:1997;1247-1256.
20. Delpón E., Valenzuela C., Gay P., et al. Block of human cardiac Kv1.5 channels by loratadine: voltage-, time- and use-dependent block at concentrations above therapeutic levels. J Cardiovasc Pharmacol. 35:1997;341-350.
21. + current by almokalant in rabbit ventricular myocytes. Circ Res. 73:1993;857-868.
22. Tseng G.-N., Zhu B., Ling S., Yao J.-A. Quinidine enhances and suppresses Kv1.2 from outside and inside the cell, respectively. J Pharmacol Exp Ther. 279:1996;844-855.
23. +]: a tale of two inactivation mechanisms. Neuron. 15:1995;951-960.
24. + at the potassium channel selectivity filter. Biophys J. 74:1998;1840-1849.
25. + channel. Biophys J. 74:1998;1808-1820.