Abstract
Advances in molecular biology are giving unprecedented insights into potassium (K)-channel structure and function. In parallel, the development of channel modulators and their investigation using electrophysiological techniques has revealed much, but posed many questions. What is the importance of the recently-discovered channel β-subunits? What is the nature of the so-called ATP-sensitive K-channel and how do K-channel openers exert tissue-protective actions? Can the K-channels in lymphocytes be exploited therapeutically? The purpose of this chapter is to give the reader an insight into this dynamic pharmacological field and to provide a stimulus for further discussion and experimentation. Correspondence to: Gillian Edwards, address as above.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
Similar content being viewed by others
References
Rudy B. Diversity and ubiquity of K+ channels. Neurosci. 1988; 25: 729–749.
Pongs O. Molecular biology of voltage-dependent potassium channels. Physiol. Rev. 1992; 72: S69–S88.
Gutman GA, Chandy KG. Nomenclature of mammalian voltage-dependent potassium channel genes. Neurosci. 1993; 5: 101–106.
Jan LY, Jan YN. Tracing the roots of ion channels. Cell 1992; 69: 715–718.
Jan LY, Jan YN. Structural elements involved in specific K+ channel functions. Ann. Rev. Physiol. 1992; 54: 537–555.
Pongs O. Structure-function studies of the pore of potassium channels. J. Membrane Biol. 1993; 136: 1–8.
MacKinnon R. Determination of the subunit stoichiometry of a voltage-activated potassium channel. Nature 1991; 350: 232–235.
Hoshi T, Zagotta WN, Aldrich RW. Two types of inactivation in Shaker K+ channels: effects of alterations in the carboxy-terminal region. Neuron 1991; 7: 547–556.
Rettig J, Heinemann S, Lorra C, Parcej DN, Dolly JO, Pongs O. Non-inactivating voltage-gated potassium channels are converted to A-type channels by association with a β-subunit. Nature 1994; 369: 289–294.
Grinstein S, Foskett JK. Ionic mechanisms of cell volume regulation in leukocytes. Ann. Rev. Physiol. 1990; 52: 599–614.
DeCoursey TE, Chandy KG, Gupta S, Cahalan MD. Voltage-gated K+ channels in human T lymphocytes: a role in mitogenesis? Nature 1984; 307: 465–468.
Matteson DR, Deutsch C. K channels in T lymphocytes: a patch clamp study using monoclonal antibody adhesion. Nature 1984; 307: 468–471.
Lewis RS, Cahalan MD. Subset-specific expression of potassium channels in developing murine T lymphocytes. Science 1988; 239: 771–775.
Deutsch C, Chen L-Q. Heterologous expression of specific K + channels in T lymphocytes: functional consequences for volume regulation. Proc. Natl. Acad. Sci. USA 1993; 90: 10036–10040.
Cahalan MD, Chandy KG, DeCoursey TE, Gupta S. A voltage-gated potassium channel in human T lymphocytes. J. Physiol. 1985; 358: 197–237.
Grissmer S, Dethlets B, Wasmuth JJ, Goldin AL, Gutman GA, Cahalan MD et al. Expression and chromosomal localization of a lymphocyte K + channel gene. Proc. Natl. Acad. Sci. USA 1990; 87: 9411–9415.
Garcia-Calvo M, Leonard RJ, Novick J, Stevens SP, Schmalhofer W, Kaczorowski GJ et al. Purification, characterization, and biosynthesis of margatoxin, a component of Centruroides margaritatus venom that selectively inhibits voltage-dependent potassium channels. J. Biol. Chem. 1993; 268: 18866–18874.
Leonard RJ, Garcia ML, Slaughter RS, Reuben JP. Selective blockers of voltage-gated K+ channels depolarize human T lymphocytes: mechanism of the antiproliferative effect of charybdotoxin. Proc. Natl. Acad. Sci. USA 1992; 89: 10094–10098.
Lin C, Boltz RC, Blake T, Nguyen M, Talento A, Fischer P et al. Voltage-gated potassium channels regulate calcium-dependent pathways involved in human T lymphocyte activation. J. Exp. Med. 1993; 177: 637–646.
Freedman BD, Price MA, Deutsch CJ. Evidence for voltage modulation of IL-2 production in mitogen-stimulated human peripheral blood lymphocytes. J. Immunol. 1992; 149: 3784–3794.
Edwards G, Weston AH. The pharmacology of ATP-sensitive potassium channels. Annu. Rev. Pharmacol. Toxicol. 1993; 33: 597–637.
Dunne MJ, Petersen OH. Intracellular ADP activates K+ channels that are inhibited by ATP in an insulin-secreting cell line. FEBS Lett. 1986; 208: 59–66.
Tung RT, Kurachi Y. On the mechanism of nucleotide diphosphate activation of the ATP-sensitive K+ channel in ventricular cell of guinea-pig. J. Physiol. 1991; 437: 239–256.
Terzic A, Findlay I, Hosoya Y, Kurachi Y. Dualistic behaviour of ATP-sensitive K+ channels toward intracellular nucleoside diphosphates. Neuron 1994; 12: 1049–1058.
Shen WK, Tung RT, Machulda MM, Kurachi Y. Essential role of nucleotide diphosphates in nicorandil-mediated activation of cardiac ATP-sensitive K+-channel — a comparison with pinacidil and lemakalim. Circ. Res. 1991; 69: 1152–1158.
Quast U, Bray KM, Andres H, Manley PW, Baumlin Y, Dosogne J. Binding of the K+ channel opener [H3] P1075 in rat isolated aorta — relationship to functional effects of openers and blockers. Mol. Pharmacol. 1993; 43: 474–481.
Hoffman FJ, Lenfers JB, Niemers E, Pleiss U, Scriabine A, Janis RA. High affinity binding of a potassium channel agonist to intact rat insulinoma cells. Biochem. Biophys. Res. Acta. 1993; 190: 551–558.
Edwards G, Ibbotson T, Weston AH. Levcromakalim may induce a voltage-independent K-current in rat portal veins by modifying the gating properties of the delayed rectifier. Br. J. Pharmacol. 1993; 110: 1037–1048.
Ashford MLJ, Bond CT, Blair TA, Adelman JP. Cloning and functional expression of a rat heart KATP channel. Nature 1994; 370: 456–459.
Arena JP, Kass RS. Enhancement of potassium-sensitive current in heart cells by pinacidil: Evidence for modulation of the ATP-sensitive potassium channel. Circ. Res. 1989; 65: 436–445.
Kubo Y, Baldwin TJ, Jan YN, Jan LY. Primary structure and functional expression of a mouse inward rectifier potassium channel. Nature 1993; 362: 127–133.
Tytgat J, Vereecke J, Carmeliet E. A possible structural link between voltage-gated and inward rectifier K+ channels. Biophys. J. 1994; 66: A425.
Parratt JR, Kane KA. KATP channels in ischemic preconditioning. Cardiovasc. Res. 1994; 28: 783–785.
Jennings RB, Murry CE, Reimer KA. Energy metabolism in preconditioned and control myocardium: effect of total ischemia. J. Mol. Cell Cardiol. 1991; 33: 1449–1458.
Tomai F, Crea F, Gaspardone A, Versaci F, De Paulis R, de Peppo AP et al. Blockade of ATP-sensitive potassium channels prevents myocardial preconditioning in man. Circulation 1994; 90: 700–705.
Gross GJ, Auchampach JA. Ischemic preconditioning during coronary angioplasty is prevented by glibenclamide, a selective ATP-sensitive K+ channel blocker. Circ. Res. 1992; 70: 223–233.
Escande D, Cavero I. Potassium channel openers in the heart. In: Escande D, Standen N, editors. K+ channels in cardiovascular medicine. Paris: Springer-Verlag, 1993: 225–244.
McPherson CD, Pierce GN, Cole WC. Ischemic cardioprotection by ATP-sensitive K+ channels involves high energy phosphate preservation. Am. J. Physiol. 1993; 34: H1809–H1818.
Djellas Y, Mestre M, Cavero I. Aprikalim protection against ischemic injury occurs with an accelerated decrease in action potential duration but not in myocardial contractility. Circulation 1993; 88: 1–632.
Auchampach JA, Maruyama M, Cavero I, Gross GJ. Pharmacological evidence for a role of ATP-dependent potassium channels in myocardial stunning. Circulation 1992; 86: 311–319.
Yao Z, Gross GJ. Effects of the KATP channel opener bimakalim on coronary blood flow, monophasic action potential duration, and infarct size in dogs. Circulation 1994; 89: 1769–1775.
Cavero I, Premmereur J. ATP-sensitive potassium channel openers are of potential benefit in ischemic heart disease. Cardiovasc. Res. 1994; 28: 32–33.
Taira N. Nicorandil as a hybrid between nitrates and potassium channel activators. Am. J. Cardiol. 1989; 63: 18J–24J.
Frampton J, Buckley MM, Fitton A. Nicorandil: a review of its pharmacology and therapeutic efficacy in angina pectoris. Drugs 1992; 44: 625–655.
Aizawa T, Ogasawara K, Nakamura F, Hirosaka A, Sakuma T, Nagashima K et al. Effect of nicorandil on coronary spasm. Am. J. Cardiol. 1989; 63: 75J–79J.
Lablanche J-M. Bauters C, Leroy F, Bertrand ME. Prevention of coronary spasm by nicorandil: comparison with nifedipine. J. Cardiovasc. Pharmacol. 1992; 20(Supplement 3): S82–S85.
Kishida H, Murao S. Effect of a new coronary vasodilator, nicorandil, on variant angina pectoris. Clin. Pharmacol. Ther. 1987; 42: 166–174.
Kinoshita M, Nisbikawa S, Sawamura M, Yamaguchi S, Mitsunami K, Itoh M et al. Comparative efficacy of high-dose versus low-dose nicorandil therapy for chronic stable angina pectoris. Am. J. Cardiol. 1986; 58: 733–738.
Thormann J, Schlepper M, Kramer W, Gottwik M, Kindler M. Effectiveness of nicorandil (SG-75), a new long-acting drug with nitroglycerin effects in patients with coronary artery disease: improved left ventricular function and regional wall motion and abolition of pacing-induced angina. J. Cardiovasc. Pharmacol. 1983; 5: 371–377.
Wagner G. Selected issues from an overview on nicorandil: tolerance, duration of action, and long-term efficacy. J. Cardiovasc. Pharmacol. 1992; 20(Supplement 3): S86–S92.
Friedel HA, Brogden RN. Pinacidil: A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in the treatment of hypertension. Drugs 1990; 39(6): 929–967.
Hamilton TC, Beerahee A, Moen JS, Price RK, Ramju JV, Clapham JC. Levcromakalim. Cardiovasc. Drugs Rev. 1993; 11: 199–222.
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 1995 Birkhäuser Verlag Basel/Switzerland
About this chapter
Cite this chapter
Edwards, G. et al. (1995). Aspects of Potassium Channel Modulation. In: Cuello, A.C., Collier, B. (eds) Pharmacological Sciences: Perspectives for Research and Therapy in the Late 1990s. Birkhäuser Basel. https://doi.org/10.1007/978-3-0348-7218-8_13
Download citation
DOI: https://doi.org/10.1007/978-3-0348-7218-8_13
Publisher Name: Birkhäuser Basel
Print ISBN: 978-3-0348-7220-1
Online ISBN: 978-3-0348-7218-8
eBook Packages: Springer Book Archive