Stereoselective inhibition of the hERG1 potassium channel

Frontiers in Pharmacology

Volumn 1 NOV, Issue , 2010, Pages

  Grilo, Liliana Sintra ^a,b   Carrupt, Pierre Alain ^a   Abriel, Hugues ^b  

^a UNIVERSITY OF GENEVA   (Switzerland)

^b UNIVERSITY OF BERN   (Switzerland)

Author keywords

Cardiotoxicity; Enantiomer; hERG1 channel; Long QT syndrome; Methadone; Stereoselectivity

Indexed keywords

EID: 84865972249     PISSN: None     EISSN: 16639812     Source Type: Journal    
DOI: 10.3389/fphar.2010.00137     Document Type: Article

References (97)

1. Abernethy, D. R., Wesche, D. L., Barbey, J. T., Ohrt, C., Mohanty, S., Pezzullo, J. C., and Schuster, B. G. (2001). Stereoselective halofantrine disposition and effect: concentration-related QTc prolongation. Br. J. Clin. Pharmacol. 51, 231-237.
2. Abriel, H., Schlapfer, J., Keller, D. I., Gavillet, B., Buclin, T., Biollaz, J., Stoller, R., and Kappenberger, L. (2004). Molecular and clinical determinants of drug-induced long QT syndrome: an iatrogenic channelopathy. Swiss. Med. Wkly. 134, 685-694.
3. Ansermot, N., Albayrak, O., Schlapfer, J., Crettol, S., Croquette-Krokar, M., Bourquin, M., Deglon, J. J., Faouzi, M., Scherbaum, N., and Eap, C. B. (2010). Substitution of (R,S)-methadone by (R)-methadone: Impact on QTc interval. Arch. Intern. Med. 170, 529-536.
4. Bell, I. M., Gallicchio, S. N., Abrams, M., Beese, L. S., Beshore, D. C., Bhimnathwala, H., Bogusky, M. J., Buser, C. A., Culberson, J. C., Davide, J., Ellis-Hutchings, M., Fernandes, C., Gibbs, J. B., Graham, S. L., Hamilton, K. A., Hartman, G. D., Heimbrook, D. C., Homnick, C. F., Huber, H. E., Huff, J. R., Kassahun, K., Koblan, K. S., Kohl, N. E., Lobell, R. B., Lynch, J. J. Jr., Robinson, R., Rodrigues, A. D., Taylor, J. S., Walsh, E. S., Williams, T. M., and Zartman, C. B. (2002). 3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency. J. Med. Chem. 45, 2388-2409.
5. Brown, A. M. (2004). Drugs, hERG and sudden death. Cell Calcium 35, 543-547.
6. Busse, D., Templin, S., Mikus, G., Schwab, M., Hofmann, U., Eichelbaum, M., and Kivisto, K. T. (2006). Cardiovascular effects of (R)- and (S)-verapamil and racemic verapamil in humans: a placebo-controlled study. Eur. J. Clin. Pharmacol. 62, 613-619.
7. Cahill, S. A., and Gross, G. J. (2004). Propafenone and its metabolites preferentially inhibit IKr in rabbit ventricular myocytes. J. Pharmacol. Exp. Ther. 308, 59-65.
8. Caner, H., Groner, E., Levy, L., and Agranat, I. (2004). Trends in the development of chiral drugs. Drug Discov. Today 9, 105-110.
9. Crettol, S., Deglon, J. J., Besson, J., Croquette-Krokkar, M., Gothuey, I., Hammig, R., Monnat, M., Huttemann, H., Baumann, P., and Eap, C. B. (2005). Methadone enantiomer plasma levels, CYP2B6, CYP2C19, and CYP2C9 genotypes, and response to treatment. Clin. Pharmacol. Ther. 78, 593-604.
10. Crettol, S., Deglon, J. J., Besson, J., Croquette-Krokar, M., Hammig, R., Gothuey, I., Monnat, M., and Eap, C. B. (2006). ABCB1 and cytochrome P450 genotypes and phenotypes: influence on methadone plasma levels and response to treatment. Clin. Pharmacol. Ther. 80, 668-681.
11. De Ponti, F., Poluzzi, E., Montanaro, N., and Ferguson, J. (2000). QTc and psychotropic drugs. Lancet 356, 75-76.
12. Deamer, R. L., Wilson, D. R., Clark, D. S., and Prichard, J. G. (2001). Torsades de pointes associated with high dose levomethadyl acetate (ORLAAM). J. Addict. Dis. 20, 7-14.
13. Dukes, I. D., and Williams, E. M. V. (1984). The Multiple-Modes of Action of Propafenone. Eur. Heart J. 5, 115-125.
14. Eap, C. B., Buclin, T., and Baumann, P. (2002). Interindividual variability of the clinical pharmacokinetics of methadone: implications for the treatment of opioid dependence. Clin. Pharmacokinet. 41, 1153-1193.
15. Eap, C. B., Crettol, S., Rougier, J. S., Schläpfer, J., Sintra Grilo, L., Déglon, J. J., Besson, J., Croquette-Krokar, M., Carrupt, P. A., and Abriel, H. (2007). Stereoselective block of hERG channel by (S)-methadone and QT interval prolongation in CYP2B6 slow metabolizers. Clin. Pharmacol. Ther. 81, 719-728.
16. Ehret, G. B., Voide, C., Gex-Fabry, M., Chabert, J., Shah, D., Broers, B., Piguet, V., Musset, T., Gaspoz, J. M., Perrier, A., Dayer, P., and Desmeules, J. A. (2006). Drug-induced long QT syndrome in injection drug users receiving methadone: high frequency in hospitalized patients and risk factors. Arch. Intern. Med. 166, 1280-1287.
17. Eichelbaum, M., Reetz, K. P., Schmidt, E. K., and Zekorn, C. (1986). The genetic polymorphism of sparteine metabolism. Xenobiotica 16, 465-481.
18. Escande, D., Mestre, M., Cavero, I., Brugada, J., and Kirchhof, C. (1992). RP 58866 and its active enantiomer RP 62719 (terikalant): blockers of the inward rectifier K + current acting as pure class III antiarrhythmic agents. J. Cardiovasc. Pharmacol. 20 (Suppl. 2), S106-S113.
19. Ferrari, A., Coccia, C. P., Bertolini, A., and Sternieri, E. (2004). Methadone - metabolism, pharmacokinetics and interactions. Pharmacol. Res. 50, 551-559.
20. Fjordside, L., Jeppesen, U., Eap, C. B., Powell, K., Baumann, P., and Brosen, K. (1999). The stereoselective metabolism of fluoxetine in poor and extensive metabolizers of sparteine. Pharmacogenetics 9, 55-60.
21. Gaertner, J., Voltz, R., and Ostgathe, C. (2008). Methadone: a closer look at the controversy. J. Pain Symptom. Manage. 36, e4-e7.
22. Gonzalez, T., Arias, C., Caballero, R., Moreno, I., Delpon, E., Tamargo, J., and Valenzuela, C. (2002). Effects of levobupivacaine, ropivacaine and bupivacaine on HERG channels: stereoselective bupivacaine block. Brit. J. Pharmacol. 137, 1269-1279.
23. Hartigan-Go, K., Bateman, D. N., Daly, A. K., and Thomas, S. H. L. (1996). Stereoselective cardiotoxic effects of terodiline. Clin. Pharmacol. Ther. 60, 89-98.
24. Hii, J. T., Wyse, D. G., Gillis, A. M., Cohen, J. M., and Mitchell, L. B. (1991). Propafenone-induced torsade de pointes: cross-reactivity with quinidine. Pacing Clin. Electrophysiol. 14, 1568-1570.
25. Hirose, K., Yamaguchi, H., Oshima, Y., Choraku, M., Hirono, A., Takamori, N., and Tamura, K. (2008). Severe respiratory failure and torsades de pointes induced by disopyramide in a patient with myasthenia gravis. Intern. Med. 47, 1703-1708.
26. ICH S7B. (2005). International Conference on Harmonisation; guidance on S7B nonclinical evaluation of the potential for delayed ventricular repolarization (QT interval prolongation) by human pharmaceuticals. Fed. Regist. 70, 61133-61134.
27. Ingelman-Sundberg, M. (2001). Pharmacogenetics: an opportunity for a safer and more efficient pharmacotherapy. J. Intern. Med. 250, 186-200.
28. Jamieson, C., Moir, E. M., Rankovic, Z., and Wishart, G. (2006). Medicinal chemistry of hERG optimizations: highlights and hang-ups. J. Med. Chem. 49, 5029-5046.
29. Jones, S. E., Ogura, T., Shuba, L. M., and McDonald, T. F. (1998). Inhibition of the rapid component of the delayed-rectifier K+ current by therapeutic concentrations of the antispasmodic agent terodiline. Br. J. Pharmacol. 125, 1138-1143.
30. Jurkiewicz, N. K., Wang, J., Fermini, B., Sanguinetti, M. C., and Salata, J. J. (1996). Mechanism of action potential prolongation by RP 58866 and its active enantiomer, terikalant. Block of the rapidly activating delayed rectifier K+ current, IKr. Circulation 94, 2938-2946.
31. Kanai, Y., Tateyama, S., Nakamura, T., Kasaba, T., and Takasaki, M. (1999). Effects of levobupivacaine, bupivacaine, and ropivacaine on tail-flick response and motor function in rats following epidural or intrathecal administration. Reg. Anesth. Pain Med. 24, 444-452.
32. Karbwang, J., Davis, T. M., Looareesuwan, S., Molunto, P., Bunnag, D., and White, N. J. (1993). A comparison of the pharmacokinetic and pharmacodynamic properties of quinine and quinidine in healthy Thai males. Br. J. Clin. Pharmacol. 35, 265-271.
33. Katchman, A. N., McGroary, K. A., Kilborn, M. J., Kornick, C. A., Manfredi, P. L., Woosley, R. L., and Ebert, S. N. (2002). Influence of opioid agonists on cardiac human ether-a-go-go-related gene K(+) currents. J. Pharmacol. Exp. Ther. 303, 688-694.
34. Kimura, Y., Takayanagi, K., Sakai, Y., Satoh, T., Fujito, T., Inoue, T., Hayashi, T., Morooka, S., and Takabatake, Y. (1994). Torsades de pointes in paced patients with sick sinus syndrome after disopyramide administration. Jpn. Heart J. 35, 153-161.
35. Kroemer, H. K., Fromm, M. F., Buhl, K., Terefe, H., Blaschke, G., and Eichelbaum, M. (1994). An enantiomer-enantiomer interaction of (S)-and (R)-propafenone modifies the effect of racemic drug therapy. Circulation 89, 2396-2400.
36. Kroemer, H. K., Funck-Brentano, C., Silberstein, D. J., Wood, A. J., Eichelbaum, M., Woosley, R. L., and Roden, D. M. (1989). Stereoselective disposition and pharmacologic activity of propafenone enantiomers. Circulation 79, 1068-1076.
37. Labro, A. J., Raes, A. L., Bellens, I., Ottschytsch, N., and Snyders, D. J. (2003). Gating of shaker-type channels requires the flexibility of S6 caused by prolines. J. Biol. Chem. 278, 50724-50731.
38. Lee-Son, S., Wang, G. K., Concus, A., Crill, E., and Strichartz, G. (1992). Stereoselective inhibition of neuronal sodium channels by local anesthetics. Evidence for two sites of action? Anesthesiology 77, 324-335.
39. Lin, C. R., Somberg, T., Molnar, J., and Somberg, J. (2009). The effects of chiral isolates of methadone on the cardiac potassium channel IKr. Cardiology 113, 59-65.
40. Mannhold, R., Kubinyi, H., and Folkers, G. (2006). Chirality in Drug Research. Weinheim: Wiley-VCH. Marban, E. (2002). Cardiac channelopathies. Nature 415, 213-218.
41. Margolis, J. M., O'Donnell, J. P., Mankowski, D. C., Ekins, S., and Obach, R. S. (2000). (R)-, (S)-, and racemic fluoxetine N-demethylation by human cytochrome P450 enzymes. Drug Metab. Dispos. 28, 1187-1191.
42. Martin, R. L., Su, Z., Limberis, J. T., Palmatier, J. D., Cowart, M. D., Cox, B. F., and Gintant, G. A. (2006). In vitro preclinical cardiac assessment of tolterodine and terodiline: multiple factors predict the clinical experience. J. Cardiovasc. Pharmacol. 48, 199-206.
43. Mattick, R. P., Breen, C., Kimber, J., and Davoli, M. (2009). Methadone maintenance therapy versus no opioid replacement therapy for opioid dependence. Cochrane Database Syst. Rev. CD002209.
44. Mbai, M., Rajamani, S., and January, C. T. (2002). The anti-malarial drug halofantrine and its metabolite N-desbutylhalofantrine block HERG potassium channels. Cardiovasc. Res. 55, 799-805.
45. Mergenthaler, J., Haverkamp, W., Huttenhofer, A., Skryabin, B. V., Musshoff, U., Borggrefe, M., Speckmann, E. J., Breithardt, G., and Madeja, M. (2001). Blocking effects of the antiarrhythmic drug propafenone on the HERG potassium channel. Naunyn Schmiedebergs Arch. Pharmacol. 363, 472-480.
46. Michalets, E. L., and Williams, C. R. (2000). Drug interactions with cisapride: clinical implications. Clin. Pharmacokinet. 39, 49-75.
47. Miller, S. (2006). Scientific and Regulatory Aspects of Quality Control for Chiral Drugs. Chirality International Symposium, Busan, South Korea; www.fda.gov/downloads/AboutFDA/CentersOffices/CDER/ucm103532.pdf.
48. Mitcheson, J. S., Chen, J., Lin, M., Culberson, C., and Sanguinetti, M. C. (2000a). A structural basis for drug-induced long QT syndrome. Proc. Natl. Acad. Sci. U.S.A. 97, 12329-12333.
49. Mitcheson, J. S., Chen, J., and Sanguinetti, M. C. (2000b). Trapping of a methanesulfonanilide by closure of the HERG potassium channel activation gate. J. Gen. Physiol. 115, 229-239.
50. Mohammad, S., Zhou, Z. F., Gong, Q. M., and January, C. T. (1997). Blockage of the HERG human cardiac K + channel by the gastrointestinal prokinetic agent cisapride. Am. J. Physio. Heart Circ. Physiol. 273, H2534-H2538.
51. Monserrat, J. M., and Bianchini, A. (2001). Anticholinesterase effect of eserine (physostigmine) in fish and crustacean species. Braz. Arch. Biol. Techn. 44, 63-68.
52. Newcombe, D. A. L. (2006). An Examination of the Pharmacodynamics and Pharmacokinetics of Levo-alpha-actelymethadol (LAAM), Compared to Methadone, in Opioid Maintenance Patients. Ph.D. Thesis. University of Adelaide, Australia.
53. Niewinski, P., Orzechowska-Juzwenko, K., Hurkacz, M., Rzemislawska, Z., Jazwinska-Tarnawska, E., Milejski, P., and Forkasiewicz, Z. (2002). CYP2D6 extensive, intermediate, and poor phenotypes and genotypes in a Polish population. Eur. J. Clin. Pharmacol. 58, 533-535.
54. Paavonen, K. J., Chapman, H., Laitinen, P. J., Fodstad, H., Piippo, K., Swan, H., Toivonen, L., Viitasalo, M., Kontula, K., and Pasternack, M. (2003). Functional characterization of the common amino acid 897 polymorphism of the cardiac potassium channel KCNH2 (HERG). Cardiovasc. Res. 59, 603-611.
55. Paul, A. A., Witchel, H. J., and Hancox, J. C. (2002). Inhibition of the current of heterologously expressed HERG potassium channels by flecainide and comparison with quinidine, propafenone and lignocaine. Br. J. Pharmacol. 136, 717-729.
56. Paul, A. A., Witchel, H. J., and Hancox, J. C. (2001). Inhibition of HERG potassium channel current by the class 1a antiarrhythmic agent disopyramide. Biochem. Biophys. Res. Commun. 280, 1243-1250.
57. Paulussen, A. D., Gilissen, R. A., Armstrong, M., Doevendans, P. A., Verhasselt, P., Smeets, H. J., Schulze-Bahr, E., Haverkamp, W., Breithardt, G., Cohen, N., and Aerssens, J. (2004). Genetic variations of KCNQ1, KCNH2, SCN5A, KCNE1, and KCNE2 in drug-induced long QT syndrome patients. J. Mol. Med. 82, 182-188.
58. Perry, M., de Groot, M. J., Helliwell, R., Leishman, D., Tristani-Firouzi, M., Sanguinetti, M. C., and Mitcheson, J. (2004). Structural determinants of HERG channel block by clofilium and ibutilide. Mol. Pharmacol. 66, 240-249.
59. Popp, B. D., Hutchinson, D. S., Evans, B. A., and Summers, R. J. (2004). Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors. Eur. J. Pharmacol. 484, 323-331.
60. Rajamani, S., Eckhardt, L. L., Valdivia, C. R., Klemens, C. A., Gillman, B. M., Anderson, C. L., Holzem, K. M., Delisle, B. P., Anson, B. D., Makielski, J. C., and January, C. T. (2006). Drug-induced long QT syndrome: hERG K + channel block and disruption of protein trafficking by fluoxetine and norfluoxetine. Br. J. Pharmacol. 149, 481-489.
61. Roden, D. M. (2004). Drug-induced prolongation of the QT interval. N. Engl. J. Med. 350, 1013-1022.
62. Roden, D. M. (2006). Long QT syndrome: reduced repolarization reserve and the genetic link. J. Intern. Med. 259, 59-69.
63. Roden, D. M., and Viswanathan, P. C. (2005). Genetics of acquired long QT syndrome. J. Clin. Invest. 115, 2025-2032.
64. Roden, D. M., Woosley, R. L., and Primm, R. K. (1986). Incidence and clinical features of the quinidine-associated long QT syndrome: implications for patient care. Am. Heart J. 111, 1088-1093.
65. Rosengarten, M., and Brooks, R. (1987). Torsade de pointes ventricular tachycardia in a hypothyroid patient treated with propafenone. Can. J. Cardiol. 3, 234-239.
66. Roy, M. L., Dumaine, R., and Brown, A. M. (1996). HERG, a primary human ventricular target of the nonsedating antihistamine terfenadine. Circulation 94, 817-823.
67. Sanchez-Chapula, J. A., Ferrer, T., Navarro-Polanco, R. A., and Sanguinetti, M. C. (2003). Voltage-dependent profile of human ether-a-go-go-related gene channel block is influenced by a single residue in the S6 transmembrane domain. Mol. Pharmacol. 63, 1051-1058.
68. Sandler, G., Clayton, G. A., and Thornicroft, S. G. (1968). Clinical evaluation of verapamil in angina pectoris. Br. Med. J. 3, 224-227.
69. Shah, R. R. (2002). The significance of QT interval in drug development. Br. J. Clin. Pharmacol. 54, 188-202.
70. Shimazawa, R., Nagai, N., Toyoshima, S., and Okuda, H. (2008). Present state of new chiral drug development and review in Japan. J. Health Sci. 54, 23-29.
71. Siebrands, C. C., Schmitt, N., and Friederich, P. (2005). Local anesthetic interaction with human ether-a-go-go-related gene (HERG) channels. Anesthesiology 103, 102-112.
72. Smith, S. W. (2009). Chiral toxicology: it's the same thing...only different. Toxicol. Sci. 110, 4-30.
73. Snyders, D. J., and Chaudhary, A. (1996). High affinity open channel block by dofetilide of HERG expressed in a human cell line. Mol. Pharmacol. 49, 949-955.
74. Snyders, D. J., Knoth, K. M., Roberds, S. L., and Tamkun, M. M. (1991). Time-, voltage-, and state-dependent block by quinidine of a cloned human cardiac potassium channel. Mol. Pharmacol. 41, 322-330.
75. Spector, P. S., Curran, M. E., Keating, M. T., and Sanguinetti, M. C. (1996). Class III antiarrhythmic drugs block HERG, a human cardiac delayed rectifier K + channel. Open-channel block by methanesulfonanilides. Circ. Res. 78, 499-503.
76. Stansfeld, P. J., Gedeck, P., Gosling, M., Cox, B., Mitcheson, J. S., and Sutcliffe, M. J. (2007). Drug block of the hERG potassium channel: insight from modeling. Proteins 68, 568-580.
77. Sticherling, C., Schaer, B. A., Ammann, P., Maeder, M., and Osswald, S. (2005). Methadone-induced torsade de pointes tachycardias. Swiss Med. Wkly 135, 282-285.
78. Sun, Z., Milos, P. M., Thompson, J. F., Lloyd, D. B., Mank-Seymour, A., Richmond, J., Cordes, J. S., and Zhou, J. (2004). Role of a KCNH2 polymorphism (R1047 L) in dofetilide-induced Torsades de Pointes. J. Mol. Cell Cardiol. 37, 1031-1039.
79. Thomas, D., Gut, B., Wendt-Nordahl, G., and Kiehn, J. (2002). The antidepressant drug fluoxetine is an inhibitor of human ether-a-go-go-related gene (HERG) potassium channels. J. Pharmacol. Exp. Ther. 300, 543-548.
80. Thomas, D., Wu, K., Kathöfer, S., Katus, H. A., Schoels, W., Kiehn, J., and Karle, C. A. (2003). The antipsychotic drug chlorpromazine inhibits HERG potassium channels. Brit. J. Pharmacol. 139, 567-574.
81. Tierney, M. G., Uhthoff, T. L., Kravcik, S., and Wielgosz, A. T. (1997). Potential cisapride-erythromycin interaction. Can. J. Clin. Pharmacol. 4, 82-84.
82. Triggle, D. J. (1996). Ion channels as pharmacologic receptors: the chirality of drug interactions. Chirality 8, 35-38.
83. Tucker, G. T. (2000). Chiral switches. The Lancet 355, 1085-1087.
84. Valenzuela, C., Delpon, E., Tamkun, M. M., Tamargo, J., and Snyders, D. J. (1995a). Stereoselective block of a human cardiac potassium channel (Kv1.5) by bupivacaine enantiomers. Biophys. J. 69, 418-427.
85. Valenzuela, C., Snyders, D. J., Bennett, P. B., Tamargo, J., and Hondeghem, L. M. (1995b). Stereoselective block of cardiac sodium channels by bupivacaine in guinea pig ventricular myocytes. Circulation 92, 3014-3024.
86. Valko, K., Du, C. M., Bevan, C., Reynolds, D. P., and Abraham, M. H. (2001). Rapid method for the estimation of octanol/water partition coefficient (log Poct) from gradient RP-HPLC retention and a hydrogen bond acidity term (Σα2H). Curr. Med. Chem. 8, 1137-1146.
87. Vanhoutte, F., Vereecke, J., Carmeliet, E., and Verbeke, N. (1991). Effects of the enantiomers of disopyramide and its major metabolite on the electrophysiological characteristics of the guinea-pig papillary muscle. Naunyn-Schmiedberg's Arch. Pharmacol. 344, 662-673.
88. Waldegger, S., Niemeyer, G., Mörike, K., Wagner, C. A., Suessbrich, H., Busch, A. E., Lang, F., and Eichelbaum, M. (1999). Effect of verapamil enantiomers and metabolites on cardiac K + channels expressed in xenopus oocytes. Cell. Physiol. Biochem. 9, 81-89.
89. Walker, B. D., Valenzuela, S. M., Singleton, C. B., Tie, H., Bursill, J. A., Wyse, K. R., Qiu, M. R., Breit, S. N., and Campbell, T. J. (1999). Inhibition of HERG channels stably expressed in a mammalian cell line by the antianginal agent perhexiline maleate. Br. J. Pharmacol. 127, 243-251.
90. Wesche, D. L., Schuster, B. G., Wang, W.-X., and Woosley, R. L. (2000). Mechanism of cardiotoxicity of halofantrine. Clin. Pharmacol. Ther. 521-529.
91. White, N. J. (2007). Cardiotoxicity of antimalarial drugs. Lancet Infect. Dis. 7, 549-558.
92. Wilcock, A., and Beattie, J. M. (2009). Prolonged QT interval and methadone: implications for palliative care. Curr. Opin. Support Palliat. Care 3, 252-257.
93. Witchel, H. J., Dempsey, C. E., Sessions, R. B., Perry, M., Milnes, J. T., Hancox, J. C., and Mitcheson, J. S. (2004). The low-potency, voltage-dependent HERG blocker propafenone - molecular determinants and drug trapping. Mol. Pharmacol. 66, 1201-1212.
94. Yang, I. C. H., Scherz, M. W., Bahinski, A., Bennett, P. B., and Murray, K. T. (2000). Stereoselective interactions of the enantiomers of chromanol 293B with human voltage-gated potassium channels1. J. Pharmacol. Exp. Ther. 294, 955-962.
95. Yang, P., Kanki, H., Drolet, B., Yang, T., Wei, J., Viswanathan, P. C., Hohnloser, S. H., Shimizu, W., Schwartz, P. J., Stanton, M., Murray, K. T., Norris, K., George, A. L. Jr., and Roden, D. M. (2002). Allelic variants in long-QT disease genes in patients with drug-associated torsades de pointes. Circulation 105, 1943-1948.
96. Yang, T., Snyders, D. J., and Roden, D. M. (1997). Rapid inactivation determines the rectification and [K +]o dependence of the rapid component of the delayed rectifier K + current in cardiac cells. Circ. Res. 80, 782-789.
97. Zhang, S., Rajamani, S., Chen, Y., Gong, Q., Rong, Y., Zhou, Z., Ruoho, A., and January, C. T. (2001). Cocaine blocks HERG, but not KvLQT1 + minK, potassium channels. Mol. Pharmacol. 59, 1069-1076.