The amiodarone derivative 2-methyl-3-(3,5-diiodo-4-carboxymethoxybenzyl)benzofuran (KB130015) opens large-conductance Ca2+-activated K+ channels and relaxes vascular smooth muscle

European Journal of Pharmacology

Volumn 555, Issue 2-3, 2007, Pages 185-193

  Gessner, Guido ^a   Heller, Regine ^a   Hoshi, Toshinori ^b   Heinemann, Stefan H ^a  

^a FRIEDRICH SCHILLER UNIVERSITY JENA   (Germany)

^b UNIVERSITY OF PENNSYLVANIA   (United States)

Author keywords

BKCa channel; K+ channel opener; KB130015; Patch clamp; Smooth muscle

Indexed keywords

1 (2 HYDROXY 5 TRIFLUOROMETHYLPHENYL) 5 TRIFLUOROMETHYL 2(3H) BENZIMIDAZOLONE; 2 METHYL 3 (3,5 DIIODO 4 CARBOXYMETHOXYBENZYL)BENZOFURAN; AMIODARONE; CALCIUM ION; KB 130015; LARGE CONDUCTANCE CALCIUM ACTIVATED POTASSIUM CHANNEL; POTASSIUM CHANNEL STIMULATING AGENT; TETRAMETHYLAMMONIUM; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ANTIARRHYTHMIC ACTIVITY; ARTICLE; CALCIUM CELL LEVEL; CELL STRAIN HEK293; CONTROLLED STUDY; DRUG MECHANISM; HUMAN; HUMAN CELL; NONHUMAN; PATCH CLAMP; PRIORITY JOURNAL; PULMONARY ARTERY; SWINE; VASCULAR ENDOTHELIUM; VASCULAR SMOOTH MUSCLE; VASODILATATION;

AMIODARONE; ANIMALS; BENZOFURANS; CALCIUM; CELL LINE, TUMOR; HUMANS; LARGE-CONDUCTANCE CALCIUM-ACTIVATED POTASSIUM CHANNELS; MUSCLE RELAXATION; MUSCLE, SMOOTH, VASCULAR; MYOCYTES, SMOOTH MUSCLE; PULMONARY ARTERY; SWINE; VASODILATION;

EID: 33845987008     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2006.10.053     Document Type: Article

References (33)

1. 2+] in ventricular myocytes. J. Pharmacol. Exp. Ther. 316 (2006) 162-168
2. Brandts B., Borchard R., Macianskiene R., Gendviliene V., Dirkmann D., VanBracht M., Prull M., Meine M., Wickenbrock I., Mubagwa K., and Trappe H.J. Inhibition of G protein-coupled and ATP-sensitive potassium currents by 2-methyl-3-(3,5-diiodo-4-carboxymethoxybenzyl)benzofuran (KB130015), an amiodarone derivate. J. Pharmacol. Exp. Ther. 308 (2004) 134-142
3. Brenner R., Peréz G.J., Bonev A.D., Eckman D.E., Kosek J.C., Wiler S.W., Patterson A.J., Nelson M.T., and Aldrich R.W. Vasoregulation by the β1 subunit of the calcium-activated potassium channel. Nature 407 (2000) 870-876
4. Carlsson B., Singh B.N., Temciuc M., Nilsson S., Li Y.-L., Mellin C., and Malm J. Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone. J. Med. Chem. 45 (2002) 623-630
5. 2+-activated potassium channel (pSlo) of the cockroach Periplaneta americana: structure, localization in neurons and electrophysiology. Eur. J. Neurosci. 17 (2003) 1197-1212
6. Dick G.M., Rossow C.F., Smirnov S., Horowitz B., and Sanders K.M. Tamoxifen activates smooth muscle BK channels through the regulatory β1 subunit. J. Biol. Chem. 276 (2001) 34594-34599
7. Dick G.M., Hunter C., and Sanders K.M. Ethylbromide tamoxifen, a membrane-impermeant antiestrogen, activates smooth muscle calcium-activated large-conductance potassium channels from the extracellular side. Mol. Pharmacol. 61 (2002) 1105-1113
8. Dworetzky S.I., Boissard C.G., Lum-Ragan J.T., McKay M.C., Post-Munson D.J., Trojnacki J.T., Chang C.-P., and Gribkoff V.K. Phenotypic alteration of a human BK (hSlo) channel by hSloβ subunit coexpression: changes in blocker sensitivity, activation/relaxation and inactivation kinetics, and protein kinase A modulation. J. Neurosci. 16 (1996) 4543-4550
9. Fernández-Fernández J.M., Tomás M., Vázquez E., Orio P., Latorre R., Senti M., Marrugat J., and Valverde M.A. Gain-of-function mutation in the KCNMB1 potassium channel subunit is associated with low prevalence of diastolic hypertension. J. Clin. Invest. 113 (2004) 1032-1039
10. Ca channels activating at resting potential without calcium in LNCaP prostate cancer cells. J. Membr. Biol. 208 (2006) 229-240
11. Giangiacomo K.M., Kamassah A., Harris G., and McManus O.B. Mechanism of maxi-K channel activation by dehydrosoyasaponin-I. J. Gen. Physiol. 112 (1998) 485-501
12. Glusa E., and Adam C. Endothelium-dependent relaxation induced by cathepsin G in porcine pulmonary arteries. Br. J. Pharmacol. 133 (2001) 422-428
13. Gribkoff V.K., Starret Jr. J.E., Dworetzky S.I., Hewawasam P., Boisard C.G., Cook D.A., Frantz S.W., Heman K., Hibbard J.R., Huston K., Johnson G., Krishnan B.S., Kinney G.G., Lombardo L.A., Meanwell N.A., Molinoff P.B., Myers R.A., Moon S.L., Ortiz A., Pajor L., Pieschl R.L., Post-Munson D.J., Signor L.J., Srinivas N., Taber M.T., Thalody G., Trojnacki J.T., Wiener H., Yeleswaram K., and Yeola S.W. Targeting acute ischemic stroke with a calcium-sensitive opener of maxi-K potassium channels. Nat. Med. 7 (2001) 471-477
14. Grossman M., Dobrev D., and Kirch W. Amiodarone causes endothelium-dependent vasodilation in human hand veins in vivo. Clin. Pharmacol. Ther. 64 (1998) 302-311
15. 2+ binding and channel opening in large conductance (BK) potassium channel. J. Gen. Physiol. 120 (2002) 267-305
16. + channel α-subunits. Mol. Pharmacol. 62 (2002) 836-846
17. Kaczorowski G.J., Knaus H.-G., Leonard R.J., McManus O.B., and Garcia M.L. High-conductance calcium-activated potassium channels: structure, pharmacology, and function. J. Bioenerg. Biomembranes 28 (1996) 255-267
18. Kiehn J., Thomas D., Karle C.A., Schols W., and Kubler W. Inhibitory effects of the class III antiarrhythmic drug amiodarone on cloned HERG potassium channels. Naunyn-Schmiedeberg's Arch. Pharmacol. 359 (1999) 212-219
19. Kodama I., Makiya K., and Toyama J. Amiodarone: ionic and cellular mechanisms of action of the most promising class III agent. Am. J. Cardiol. 84 (1999) 20-28
20. Kowey P.R., Marinchak R.A., Rials S.J., and Filart R.A. Intravenous amiodarone. J. Am. Coll. Cardiol. 29 (1997) 1190-1198
21. Lu R., Alioua A., Kumar Y., Eghbali M., Stefani E., and Toro L. MaxiK channel partners: physiological impact. J. Physiol. 570 (2006) 65-72
22. McManus O.B., Harris G.H., Giangiacomo K.M., Feigenbaum P., Reuben J.P., Addy M.E., Burka J.F., Kaczorowski G.J., and Garcia M.L. An activator of calcium-dependent potassium channels isolated from a medicinal herb. Biochemistry 32 (1993) 6128-6133
23. McManus O.B., Helms L.M.H., Pallanck L., Ganetzky B., Swanson R., and Leonard R.J. Functional role of the β subunit of high conductance calcium-activated potassium channels. Neuron 14 (1995) 645-650
24. Mubagwa K., Macianskiene R., Viappiani S., Gendviliene V., Carlsson B., and Brandts B. KB130015, a new amiodarone derivative with multiple effects on cardiac ion channels. Cardiovasc. Drug Rev. 21 (2003) 216-235
25. + channels by novel benzimidazolone. Eur. J. Pharmacol. 251 (1994) 53-59
26. Orio P., Rojas P., Ferreira G., and Latorre R. New disguises for an old channel: MaxiK channel β-subunits. News Physiol. Sci. 17 (2002) 156-161
27. + channels in human pulmonary artery smooth muscle cells. Am. J. Physiol., Lung Cell. Mol. Physiol. 287 (2004) L226-L238
28. + channel isoforms from human brain. Neuron 13 (1994) 1315-1330
29. Weiger T.M., Hermann A., and Levitan I.B. Modulation of calcium-activated potassium channels. J. Comp. Physiol., A Sens. Neural Behav. Physiol. 188 (2002) 79-87
30. Xie J., and McCobb D.P. Control of alternative splicing of potassium channels by stress hormones. Science 280 (1998) 443-446
31. Zakharov S.I., Morrow J.P., Liu G., Yang L., and Marx S.O. Activation of the BK (slo1) potassium channel by mallotoxin. J. Biol. Chem. 280 (2005) 30882-30887
32. Ca channels. Am. J. Physiol., Heart. Circ. Physiol. 280 (2001) H2430-H2440
33. + channels. Biochem. Biophys. Res. Commun. 342 (2006) 1389-1395