Molecular cloning and functional characterization of a unique mammalian cardiac Nav channel isoform with low sensitivity to the synthetic inactivation inhibitor (-)-(S)-6-amino-α-[(4-diphenylmethyl-1-piperazinyl)-methyl] -9H-purine-9-ethanol (SDZ 211-939)

Journal of Pharmacology and Experimental Therapeutics

Volumn 303, Issue 1, 2002, Pages 89-98

  Denac, Helena ^a   Mevissen, Meike ^b   J p kühn, Frank ^a   Kühn, Cornelia ^b   T guionaud, Christophe ^a   Scholtysik, Günter ^a   Greeff, Nikolaus G ^a  

^a UNIVERSITY OF BERN   (Switzerland)

^b UNIVERSITY OF ZURICH   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

4 [3 (4 BENZHYDRYL 1 PIPERAZINYL) 2 HYDROXYPROPOXY] 1H INDOLE 2 CARBONITRILE; 6 AMINO ALPHA [(4 DIPHENYLMETHYL 1 PIPERAZINYL)METHYL] 9H PURINE 9 ETHANOL; AMINO ACID; ISOPROTEIN; SDZ 211939; SEA ANEMONE TOXIN; SODIUM CHANNEL; SODIUM CHANNEL AFFECTING AGENT; SODIUM CHANNEL STIMULATING AGENT; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; ANIMAL CELL; ARTICLE; BINDING AFFINITY; CATTLE; CHANNEL GATING; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG MECHANISM; DRUG PROTEIN BINDING; DRUG SENSITIVITY; ELECTROPHYSIOLOGY; HEART; HUMAN; MOLECULAR CLONING; NONHUMAN; NUCLEOTIDE SEQUENCE; OOCYTE; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; SEQUENCE HOMOLOGY; SPECIES COMPARISON; XENOPUS LAEVIS;

AMINO ACID SEQUENCE; ANIMALS; BASE SEQUENCE; BRAIN; CATTLE; CLONING, MOLECULAR; DNA PRIMERS; HEART; MEMBRANE POTENTIALS; MOLECULAR SEQUENCE DATA; PIPERAZINES; PROTEIN ISOFORMS; PROTEIN SUBUNITS; PURINES; RATS; RATS, WISTAR; SEQUENCE ALIGNMENT; SEQUENCE HOMOLOGY, AMINO ACID; SODIUM CHANNEL BLOCKERS; SODIUM CHANNELS;

EID: 0036785464     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.303.1.89     Document Type: Article

References (41)

1. Akopian AN, Sivilotti L, and Wood JN (1996) A tetrodotoxin-resistant voltage-gated sodium channel expressed by sensory neurons. Nature (Lond) 379:257-262.
2. Benzinger GR, Tonkovich GS, and Hanck DA (1999) Augmentation of recovery from inactivation by site-3 Na channel toxins. A single-channel and whole-cell study of persistent currents. J Gen Physiol 113:333-346.
3. Bezanilla F and Armstrong CM (1975) Kinetic properties and inactivation of the gating currents of sodium channels in squid axon. Phil Trans R Soc Lond B Biol Sci 270:449-458.
4. Catterall WA (1980) Neurotoxins that act on voltage-sensitive sodium channels in excitable membranes. Annu Rev Pharmacol Toxicol 20:15-43.
5. + channel fast inactivation. Neuron 22:73-87.
6. Chahine M, George AL, Zhou M, Ji S, Sun W, Barchi RL, and Horn R (1994) Sodium channel mutations in paramyotonia congenita uncouple inactivation from activation. Neuron 12:281-294.
7. Chen J, Ikeda SR, Lang W, Isales CM, and Wei X (1997) Molecular cloning of a putative tetrodotoxin-resistant sodium channel from dog nodose ganglion neurons. Gene 202:7-14.
8. Chen LQ, Santarelli V, Horn R, and Kallen RG (1996) A unique role for the S4 segment of domain 4 in the inactivation of sodium channels. J Gen Physiol 108:549-556.
9. Denac H, Mevissen M, and Scholtysik G (2000) Structure, function and pharmacology of voltage gated sodium channels. Naunyn-Schmiedeberg's Arch Pharmacol 362:453-479.
10. Fozzard HA and Lipkind GM (1996) The guanidinium toxin binding site on the sodium channel. Jpn Heart J 37:683-692.
11. Fozzard HA and Hanck DA (1996) Structure and function of voltage-dependent sodium channels: comparison of brain II and cardiac isoforms. Physiol Rev 76:887-926.
12. Frohman MA, Dush MK, and Martin GR (1988) Rapid production of full-length cDNAs from rare transcripts: amplification using a single gene-specific oligonucleotide primer. Proc Natl Acad Sci USA 85:8998-9002.
13. Gellens ME, George AL, Chen LQ, Chahine M, Horn R, Barchi RL, and Kallen RG (1992) Primary structure and functional expression of the human cardiac tetrodo-toxin-insensitive voltage-dependent sodium channel. Proc Natl Acad Sci USA 89:554-558.
14. Gerard JL, Berdeaux A, and Giudicelli JF (1989) Cardiac and hemodynamic profile of the new cardiotonic agent, DPI 201-106, in the conscious dog. Eur J Pharmacol 165:39-49.
15. Goldin AL (2001) Resurgence of sodium channel research. Annu Rev Physiol 63:871-894.
16. Greeff NG and Forster IC (1991) The quantal gating charge of sodium channel inactivation. Eur Biophys J 20:165-176.
17. Greeff NG and Kühn FJ (2000) Variable ratio of permeability to gating charge of rBIIA sodium channels and sodium influx in Xenopus laevis oocytes. Biophys J 79:2434-2453.
18. Kallen RG, Sheng ZH, Yang J, Chen L, Rogart RB, and Barchi RL (1990) Primary structure and expression of a sodium channel characteristic of denervated and immature rat skeletal muscle. Neuron 4:233-242.
19. Kontis KJ and Goldin AL (1997) Sodium channel inactivation is altered by substitution of voltage sensor positive charges. J Gen Physiol 110:403-413.
20. Kozak M (1986) Point mutations define a sequence flanking the AUG initiator codon that modulates translation by eukaryotic ribosomes. Cell 44:283-292.
21. Krafte DS, Davison K, Dugrenier N, Estep K, Josef K, Barchi RL, Kallen RG, Silver PJ, and Ezrin AM (1994) Pharmacological modulation of human cardiac Na channels. Eur J Pharmacol 266:245-254.
22. Kühn FJ and Greeff NG (1999) Movement of voltage sensor S4 in domain 4 is tightly coupled to sodium channel fast inactivation and gating charge immobilization. J Gen Physiol 114:167-183.
23. Mevissen M, Denac H, Schaad A, Portier CJ, and Scholtysik G (2001) Identification of a cardiac sodium channel insensitive to synthetic modulators. J Cardiovasc Pharmacol Ther 6:201-212.
24. Morgan K, Stevens EB, Shah B, Cox PJ, Dixon AK, Lee K, Pinnock RD, Hughes J, Richardson PJ, Mizuguchi K, and Jackson AP (2000) β3: an additional auxiliary subunit of the voltage-sensitive sodium channel that modulates channel gating with distinct kinetics. Proc Natl Acad Sci USA 97:2308-2313.
25. Murphy BJ, Rogers J, Perdichizzi AP, Colvin AA, and Catterall WA (1996) cAMP-dependent phosphorylation of two sites in the α subunit of the cardiac sodium channel. J Biol Chem 15:28837-28843.
26. Narahashi T, Moore JW, and Shapiro BI (1969) Condylactis toxin: interaction with nerve membrane ionic conductances. Science (Wash DC) 163:680-681.
27. Portier CJ, Tritscher A, Kohn M, Sewal C, Clark G, Edler L, Hoel D, and Lucier G (1993) Ligand/receptor binding for 2,3,7,8-TCDD: implications for risk assessment. Fundam Appl Toxicol 20:48-56.
28. + channel isoform. Proc Natl Acad Sci USA 86:8170-8174.
29. Romey G, Abita JP, Schweitz H, Wunderer G, and Lazdunski M (1976) Sea anemone toxin: a tool to study molecular mechanisms of nerve conduction and excitation-secretion coupling. Proc Natl Acad Sci USA 73:4055-4059.
30. - channels as sites of action of the cardioactive agent DPI 201-106 with agonist and antagonist enantiomers. Proc Natl Acad Sci USA 84:896-900.
31. Salzmann R, Scholtysik G, Clark B, and Berthold R (1986) Cardiovascular actions of DPI 201-106, a novel cardiotonic agent. J Cardiovasc Pharmacol 8:1035-1043.
32. Sato C, Ueno Y, Asai K, Takahashi K, Sato M, Engel A, and Fujiyoshi Y (2001) The voltage-sensitive sodium channel is a bell-shaped molecule with several cavities. Nature (Lond) 409:1047-1051.
33. - channel activation as a positive inotropic principle. J Cardiovasc Pharm 14:S24-S29.
34. Scholtysik G, Salzmann R, Berthold R, Herzig JW, Quast U, and Markstein R (1985) DPI 201-106, a novel cardioactive agent. Combination of cAMP-independent positive inotropic, negative chronotropic, action potential prolonging and coronary dilatory properties. Naunyn-Schmiedeberg's Arch Pharmacol 329:316-325.
35. Scholtysik G, Salzmann R, Quast U, Berthold R, Ott H, Schaad A, and Wettwer E (1993) SDZ 211-939, a new cardiotonic Na+ current activator. Naunyn-Schmiedeberg's Arch Pharmacol 347:345.
36. Sheets MF, Kyle JW, and Hanck DA (2000) The role of the putative inactivation lid in sodium channel gating current immobilization. J Gen Physiol 115:609-620.
37. Sheng ZH, Zhang H, Barchi RL, and Kallen RG (1994) Molecular cloning and functional analysis of the promoter of rat skeletal muscle voltage-sensitive sodium channel subtype 2 (rSkM2): evidence for muscle-specific nuclear protein binding to the core promoter. DNA Cell Biol 13:9-23.
38. Shih TM, Smith RD, Toro L, and Goldin AL (1998) High level expression and detection of ion channels in Xenopus oocytes. Methods Enzymol 293:529-556.
39. Wald A (1943) Tests of statistical hypothesis concerning several parameters when the number of observations is large. Trans Am Math Soc 54:426-482.
40. + channel. Circulation 99:3165-3171.
41. --channel inactivation. Proc Natl Acad Sci USA 89:10910-10914.