Inhibition of the HERG potassium channel by the tricyclic antidepressant doxepin

Biochemical Pharmacology

Volumn 74, Issue 3, 2007, Pages 425-437

  Duncan, R S ^a   McPate, M J ^a   Ridley, J M ^a   Gao, Z ^a   James, A F ^a   Leishman, D J ^b,c   Leaney, J L ^b   Witchel, H J ^a   Hancox, J C ^a  

^a SCHOOL OF MEDICAL SCIENCES   (United Kingdom)

^b PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

^c ELI LILLY AND COMPANY   (United States)

Author keywords

Antidepressant; Arrhythmia; Doxepin; HERG; IKr; Long QT syndrome; Potassium channel; QT interval; QT prolongation; Rapid delayed rectifier; Short QT syndrome; Torsade de pointes

Indexed keywords

DOXEPIN; POTASSIUM CHANNEL HERG; TRICYCLIC ANTIDEPRESSANT AGENT;

ANIMAL CELL; ARTICLE; CELL MEMBRANE DEPOLARIZATION; CONTROLLED STUDY; DRUG EFFECT; DRUG EFFICACY; DRUG POTENCY; EMBRYO; HEART ARRHYTHMIA; HUMAN; HUMAN CELL; MALE; MEMBRANE POTENTIAL; NONHUMAN; PATCH CLAMP; POINT MUTATION; PRIORITY JOURNAL; QT PROLONGATION; TEMPERATURE; WHOLE CELL;

EID: 34250749314     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bcp.2007.04.024     Document Type: Article

References (63)

1. Viskin S. Long QT syndromes and torsade de pointes. Lancet 354 (1999) 1625-1633
2. Haverkamp W., Breithardt G., Camm A.J., Janse M.J., Rosen M.R., Antzelevitch C., et al. The potential for QT prolongation and pro-arrhythmia by non-anti-arrhythmic drugs: clinical and regulatory implications report on a policy conference of the European Society of Cardiology. Cardiovasc Res 47 (2000) 219-233
3. Shah R.R. Drugs QT interval prolongation and ICH E14-the need to get it right. Drug Safety 28 (2005) 115-125
4. Witchel H.J., and Hancox J.C. Familial and acquired long QT syndrome and the cardiac rapid delayed rectifier potassium current. Clin Exp Pharmacol Physiol 27 (2000) 753-766
5. + channels: friend and foe. Trends Pharmacol Sci 22 (2001) 240-246
6. Kr potassium channel. Cell 81 (1995) 299-307
7. Trudeau M.C., Warmke J.W., Ganetzky B., and Robertson G.A. HERG a human inward rectifier in the voltage-gated potassium channel family. Science 269 (1995) 92-95
8. Mitcheson J.S., Chen J., Lin M., Culberson C., and Sanguinetti M.C. A structural basis for drug-induced long QT syndrome. Proc Natl Acad Sci USA 97 (2000) 12329-12333
9. Mitcheson J.S., and Perry M.D. Molecular determinants of high-affinity drug binding to HERG channels. Curr Opin Drug Discov Devel 6 (2003) 667-674
10. Lees-Miller J.P., Duan Y.J., Teng G.Q., and Duff H.J. Molecular determinant of high-affinity dofetilide binding to HERG1 expressed in Xenopus oocytes: Involvement of S6 sites. Mol Pharmacol 57 (2000) 367-374
11. Webster R., Leishman D., and Walker D. Towards a drug concentration effect relationship for QT prolongation and torsades de pointes. Curr Opin Drug Discov Devel 5 (2002) 116-126
12. TM) HT. J Pharmacol Toxicol Meth 54 (2006) 189-199
13. Redfern W.S., Carlsson L., Davis A.S., Lynch W.G., MacKenzie I., Palethorpe S., et al. Relationships between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: evidence for a provisional safety margin in drug development. Cardiovasc Res 58 (2003) 32-45
14. Pinder R.M., Brogden R.N., Speight T.M., Avery G.S., and Doxepin Up-To-Date. Review of its pharmacological properties and therapeutic efficacy with particular reference to depression. Drugs 13 (1977) 161-218
15. Dumovic P., Burrows G.D., Vohra J., Davies B., and Scoggins B.A. The effect of tricyclic antidepressant drugs on the heart. Arch Toxicol 35 (1976) 255-262
16. Luchins D.J. Review of clinical and animal studies comparing the cardiovascular effects of doxepin and other tricyclic antidepressants. Am J Psychiatry 140 (1983) 1006-1009
17. Roose S.P., Dalack G.W., Glassman A.H., Woodring S., Walsh B.T., and Giardina E.G. Is doxepin a safer tricyclic for the heart?. J Clin Psychiatry 52 (1991) 338-341
18. Baker B., Dorian P., Sandor P., Shapiro C., Schell C., Mitchell J., et al. Electrocardiographic effects of fluoxetine and doxepin in patients with major depressive disorder. J Clin Psychopharmacol 17 (1997) 15-21
19. Alter P., Tontsch D., and Grimm W. Doxepin-induced torsade de pointes tachycardia. Ann Intern Med 135 (2001) 384-385
20. Rademacher S., Dietz R., and Haverkamp W. QT prolongation and syncope with methadone, doxepin, and a beta-blocker. Ann Pharmacother 39 (2005) 1762-1763
21. Tie H., Walker B.D., Valenzuela S.M., Breit S.N., and Campbell T.J. The heart of psychotropic drug therapy. Lancet 355 (2000) 1825-11825
22. + channel by the antidepressant drug amitriptyline. Br J Pharmacol 129 (2000) 1474-1480
23. Teschemacher A.G., Seward E.P., Hancox J.C., and Witchel H.J. Inhibition of the current of heterologously expressed HERG potassium channels by imipramine and amitriptyline. Br J Pharmacol 128 (1999) 479-485
24. Zhou Z., Gong Q., Ye B., Fan Z., Makielski J.C., Robertson G.A., et al. Properties of HERG channels stably expressed in HEK 293 cells studied at physiological temperature. Biophys J 74 (1998) 230-241
25. Milnes J.T., Crociani O., Arcangeli A., Hancox J.C., and Witchel H.J. Blockade of HERG potassium currents by fluvoxamine: incomplete attenuation by S6 mutations at F656 or Y652. Br J Pharmacol 139 (2003) 887-898
26. + channels expressed in Xenopus oocytes reduces rectification by shifting the voltage dependence of inactivation. J Physiol 509 (1998) 129-137
27. Brugada R., Hong K., Dumaine R., Cordeiro J., Gaita F., Borggrefe M., et al. Sudden death associated with short-QT syndrome linked to mutations in HERG. Circulation 109 (2004) 30-35
28. + channel blockade by the antiarrhythmic agent dronedarone: resistance to mutations of the S6 residues Y652 and F656. Biochem Biophys Res Commun 325 (2004) 883-891
29. + channel: accessibility to F656 and Y652. Biochem Biophys Res Commun 341 (2006) 500-506
30. Hancox J.C., Levi A.J., Lee C.O., and Heap P. A method for isolating rabbit atrioventricular node myocytes which retain normal morphology and function. Am J Physiol 265 (1993) H755-H7666
31. Howarth F.C., Levi A.J., and Hancox J.C. Characteristics of the delayed rectifier K current compared in myocytes isolated from the atrioventricular node and ventricle of the rabbit heart. Pflugers Arch 431 (1996) 713-722
32. + channel. J Mol Cell Cardiol 40 (2006) 107-118
33. Kirsch G.E., Trepakova E.S., Brimecombe J.C., Sidach S.S., Erickson H.D., Kochan M.C., et al. Variability in the measurement of hERG potassium channel inhibition: effects of temperature and stimulus pattern. J Pharmacol Toxicol Meth 50 (2004) 93-101
34. + current and prolongation of the guinea-pig ventricular action potential by 4-aminopyridine. J Physiol 549 (2003) 667-672
35. + channel mutation in the 'short QT syndrome': mechanism of gain-in-function determined at 37 °C. Biochem Biophys Res Commun 334 (2005) 441-449
36. Milnes J.T., Dempsey C.E., Ridley J.M., Crociani O., Arcangeli A., Hancox J.C., et al. Preferential closed channel blockade of HERG potassium currents by chemically synthesised BeKm-1 scorpion toxin. FEBS Lett 547 (2003) 20-26
37. Kr inactivation by mutation N588K in KCNH2: a link to arrhythmogenesis in short QT syndrome. Cardiovasc Res 67 (2005) 498-509
38. Sanguinetti M.C., and Mitcheson J.S. Predicting drug-HERG channel interactions that cause acquired long QT syndrome. Trends Pharmacol Sci 26 (2005) 119-124
39. + channel. J Mol Cell Cardiol 36 (2004) 701-705
40. + channel blockade by the fluoroquinolone antibiotic moxifloxacin. Br J Pharmacol 147 (2006) 905-916
41. + channel by the antifungal drug ketoconazole depends on channel gating and involves the S6 residue F656. FEBS Lett 580 (2006) 1999-2005
42. Reilly J.G., Ayis S.A., Ferrier I.N., Jones S.J., and Thomas S.H.L. QTc-interval abnormalities and psychotropic drug therapy in psychiatric patients. Lancet 355 (2000) 1048-1052
43. Kiesecker C., Alter M., Kathofer S., Zitron E., Scholz E., Thomas P.D., et al. Atypical tetracyclic antidepressant maprotiline is an antagonist at cardiac hERG potassium channels. Naunyn-Schmiedebergs Arch Pharmacol 373 (2006) 212-220
44. Ferrer-Villada T., Navarro-Polanco R.A., Rodriguez-Menchaca A.A., Benavides-Haro D.E., and Sanchez-Chapula J.A. Inhibition of cardiac HERG potassium channels by antidepressant maprotiline. Eur J Pharmacol 531 (2006) 1-8
45. + channels. Circ Res 82 (1998) 386-395
46. Herzberg I.M., Trudeau M.C., and Robertson G.A. Transfer of rapid inactivation and sensitivity to the class III antiarrhythmic drug E-4031 from HERG to M-eag channels. J Physiol 511 (1998) 3-14
47. Yang B.F., Xu D.H., Xu C.Q., Li Z., Du Z.M., Wang H.Z., et al. Inactivation gating determines drug potency: a common mechanism for drug blockade of HERG channels. Acta Pharmacologica Sinica 25 (2004) 554-560
48. Chen J., Seebohm G., and Sanguinetti M.C. Position of aromatic residues in the S6 domain, not inactivation, dictates cisapride sensitivity of HERG and eag potassium channels. Proc Nat Acad Sci USA 99 (2002) 12461-12466
49. Witchel H.J., Pabbathi V.K., Hofmann G., Paul A.A., and Hancox J.C. Inhibitory actions of the selective serotonin re-uptake inhibitor citalopram on HERG and ventricular L-type calcium currents. FEBS Lett 512 (2002) 59-66
50. Snyders D.J., and Chaudhary A. High affinity open channel block by dofetilide of HERG expressed in a human cell line. Mol Pharmacol 49 (1996) 949-955
51. Sanguinetti M.C., and Tristan-Firouzi M. HERG potassium channels and cardiac arrhythmia. Nature 440 (2006) 463-469
52. o and C-type inactivation. FEBS Lett 417 (1997) 43-47
53. Mitcheson J.S., Chen J., and Sanguinetti M.C. Trapping of a Methanesulfonanilide by closure of the HERG potassium channel activation gate. J Gen Physiol 115 (2000) 229-240
54. Perry M., de Groot M.J., Helliwell R., Leishman D., Tristani-Firouzi M., Sanguinetti M.C., et al. Structural determinants of HERG channel block by clofilium and ibutilide. Mol Pharmacol 66 (2004) 240-249
55. Kr potassium channels with HERG and is associated with cardiac arrhythmia. Cell 97 (1999) 175-187
56. Weerapura M., Nattel S., Chartier D., Caballero R., and Hebert T.E. A comparison of currents carried by HERG, with and without coexpression of MiRP1, and the native rapid delayed rectifier current Is MiRP1 the missing link. J Physiol 540 (2002) 15-27
57. Marshall J.B., and Forker A.D. Cardiovascular effects of tricyclic antidepressant drugs: therapeutic usage, overdose, and management of complications. Am Heart J 103 (1982) 401-414
58. Elonen E., Linnoila M., Lukkari I., and Mattila M.J. Concentration of tricyclic antidepressants in plasma, heart and skeletal muscle after their intravenous infusion to anaesthetized rabbits. Acta Pharmacol Toxicol 37 (1975) 274-281 (Copenh)
59. Leucht S., Steimer W., Kreuz S., Abraham D., Orsulak P.J., and Kissling W. Doxepin plasma concentrations: is there really a therapeutic range?. J Clin Psychopharmacol 21 (2001) 432-439
60. Brugada R., Hong K., Cordeiro J.M., and Dumaine R. Short QT Syndrome. CMAJ 173 (2005) 1349-1354
61. Gaita F., Giustetto C., Bianchi F., Schimpf R., Haissaguerre M., Calo L., et al. Short QT syndrome: pharmacological treatment. J Am Coll Cardiol 43 (2004) 1494-1499
62. Wolpert C., Schimpf R., Giustetto C., Antzelevitch C., Cordeiro J., Dumaine R., et al. Further insights into the effect of quinidine in short QT syndrome caused by a mutation in HERG. J Cardiovasc Electrophysiol 16 (2005) 54-58
63. McPate M.J., Duncan R.S., Witchel H.J., and Hancox J.C. Disopyramide is an effective inhibitor of mutant HERG K+ channels involved in variant 1 short QT syndrome. J Mol Cell Cardiol 41 (2006) 563-566