메뉴 건너뛰기




Volumn 32, Issue 12, 2005, Pages 1088-1096

The neuroprotective agent sipatrigine blocks multiple cardiac ion channels and causes triangulation of the ventricular action potential

Author keywords

BW 619C89; Fast sodium current; Guinea pig cardiac myocytes; Inward rectifier; L type calcium current; Potassium current; Pro arrhythmia; Rapidly activating delayed rectifier; Slowly activating delayed rectifier; Ventricular myocytes

Indexed keywords

CALCIUM CHANNEL L TYPE; CHROMANOL 293B; DOFETILIDE; INWARDLY RECTIFYING POTASSIUM CHANNEL; NEUROPROTECTIVE AGENT; SIPATRIGINE; SODIUM CHANNEL; CALCIUM CHANNEL BLOCKING AGENT; ION CHANNEL; PIPERAZINE DERIVATIVE; POTASSIUM CHANNEL BLOCKING AGENT; PYRIMIDINE DERIVATIVE; SODIUM CHANNEL BLOCKING AGENT;

EID: 33644968894     PISSN: 03051870     EISSN: 14401681     Source Type: Journal    
DOI: 10.1111/j.1440-1681.2005.04312.x     Document Type: Article
Times cited : (4)

References (43)
  • 1
    • 0033847175 scopus 로고    scopus 로고
    • 19C89) is a neuroprotective agent and a sodium channel and calcium channel inhibitor
    • Sipatrigine (BW 6
    • Hainsworth AH Stefani A Calabresi P Smith TW Leach MJ. Sipatrigine (BW 6 19C89) is a neuroprotective agent and a sodium channel and calcium channel inhibitor. CNS Drug Rev. 2000 6 : 111 34.
    • (2000) CNS Drug Rev. , vol.6 , pp. 111-34
    • Hainsworth, A.H.1    Stefani, A.2    Calabresi, P.3    Smith, T.W.4    Leach, M.J.5
  • 3
    • 0029551409 scopus 로고
    • Evaluation of the novel neuroprotective agent BW619C89 in the middle cerebral artery occlusion model of focal ischemia in the spontaneously hypertensive rat and normotensive Fischer 344 rat
    • Swan JH Leach MJ. Evaluation of the novel neuroprotective agent BW619C89 in the middle cerebral artery occlusion model of focal ischemia in the spontaneously hypertensive rat and normotensive Fischer 344 rat. Ann. N.Y. Acad. Sci. 1995 765 : 39 46.
    • (1995) Ann. N.Y. Acad. Sci. , vol.765 , pp. 39-46
    • Swan, J.H.1    Leach, M.J.2
  • 4
    • 0031037335 scopus 로고    scopus 로고
    • Neuroprotective effects of the glutamate release inhibitor 619C89 in temporary middle cerebral artery occlusion
    • Kawaguchi K Graham SH. Neuroprotective effects of the glutamate release inhibitor 619C89 in temporary middle cerebral artery occlusion. Brain Res. 1997 749 : 131 4.
    • (1997) Brain Res. , vol.749 , pp. 131-4
    • Kawaguchi, K.1    Graham, S.H.2
  • 5
    • 13544263591 scopus 로고    scopus 로고
    • Effects of the antiepileptic drugs lamotrigine, topiramate and gabapentin on hERG potassium currents
    • Danielsson BR Lansdell K Patmore L Tomson T. Effects of the antiepileptic drugs lamotrigine, topiramate and gabapentin on hERG potassium currents. Epilepsy Res. 2005 63 : 17 25.
    • (2005) Epilepsy Res. , vol.63 , pp. 17-25
    • Danielsson, B.R.1    Lansdell, K.2    Patmore, L.3    Tomson, T.4
  • 6
    • 0035032246 scopus 로고    scopus 로고
    • 2+ exchange current recorded from guinea-pig ventricular myocytes
    • 2+ exchange current recorded from guinea-pig ventricular myocytes. Cell Calcium 2001 29 : 347 58.
    • (2001) Cell Calcium , vol.29 , pp. 347-58
    • Zhang, Y.-H.1    Hinde, A.K.2    Hancox, J.C.3
  • 7
    • 2342624602 scopus 로고    scopus 로고
    • Gender-related differences in ventricular myocyte repolarization in the guinea pig
    • James AF Arberry LA Hancox JC. Gender-related differences in ventricular myocyte repolarization in the guinea pig. Basic Res. Cardiol. 2004 99 : 183 92.
    • (2004) Basic Res. Cardiol. , vol.99 , pp. 183-92
    • James, A.F.1    Arberry, L.A.2    Hancox, J.C.3
  • 9
    • 0033846750 scopus 로고    scopus 로고
    • 198 on action potentials and ionic currents from guinea-pig isolated ventricular myocytes
    • Effects of BDF 9
    • Yuill KH Convery MK Dooley PC Doggrell SA Hancox JC. Effects of BDF 9 198 on action potentials and ionic currents from guinea-pig isolated ventricular myocytes. Br. J. Pharmacol. 2000 130 : 1753 66.
    • (2000) Br. J. Pharmacol. , vol.130 , pp. 1753-66
    • Yuill, K.H.1    Convery, M.K.2    Dooley, P.C.3    Doggrell, S.A.4    Hancox, J.C.5
  • 10
    • 33745202980 scopus 로고
    • inventors. The Wellcome Foundation Ltd, assignee. Pharmacologically active CNS compounds. European Patent no. 0372934A2, application no. 89312723.3. December
    • Miller A Nobbs M Hyde R Leach M, inventors. The Wellcome Foundation Ltd, assignee. Pharmacologically active CNS compounds. European Patent no. 0372934A2, application no. 89312723.3. December 1989.
    • (1989)
    • Miller, A.1    Nobbs, M.2    Hyde, R.3    Leach, M.4
  • 11
    • 0025351245 scopus 로고
    • + current: Differential sensitivity to block by class III antiarrhythmic agents
    • + current: Differential sensitivity to block by class III antiarrhythmic agents. J. Gen. Physiol. 1990 96 : 194 214.
    • (1990) J. Gen. Physiol. , vol.96 , pp. 194-214
    • Sanguinetti, M.C.1    Jurkiewicz, N.K.2
  • 12
    • 0006722698 scopus 로고
    • Two types of calcium channels in guinea pig ventricular myocytes
    • Mitra R Morad M. Two types of calcium channels in guinea pig ventricular myocytes. Proc. Natl Acad. Sci. USA 1986 83 : 5340 4.
    • (1986) Proc. Natl Acad. Sci. USA , vol.83 , pp. 5340-4
    • Mitra, R.1    Morad, M.2
  • 13
    • 0029781813 scopus 로고    scopus 로고
    • Ks in guinea-pig isolated ventricular myocytes
    • Ks in guinea-pig isolated ventricular myocytes. Exp. Physiol. 1996 81 : 605 21.
    • (1996) Exp. Physiol. , vol.81 , pp. 605-21
    • Heath, B.M.1    Terrar, D.A.2
  • 14
    • 0034141614 scopus 로고    scopus 로고
    • Kr, through a reduction in C-type inactivation in guinea-pig ventricular myocytes
    • Kr, through a reduction in C-type inactivation in guinea-pig ventricular myocytes. J Physiol. 2000 522 : 391 402.
    • (2000) J Physiol. , vol.522 , pp. 391-402
    • Heath, B.M.1    Terrar, D.A.2
  • 15
    • 0021286989 scopus 로고
    • Voltage-dependent inactivation of inward-rectifying single-channel currents in the guinea-pig heart cell membrane
    • Sakmann B Trube G. Voltage-dependent inactivation of inward-rectifying single-channel currents in the guinea-pig heart cell membrane. J. Physiol. 1984 347 : 659 83.
    • (1984) J. Physiol. , vol.347 , pp. 659-83
    • Sakmann, B.1    Trube, G.2
  • 16
    • 0021330206 scopus 로고
    • A comparison of calcium currents in rat and guinea pig single ventricular cells
    • Josephson IR Sanchez-Chapula J Brown AM. A comparison of calcium currents in rat and guinea pig single ventricular cells. Circ. Res. 1984 54 : 144 56.
    • (1984) Circ. Res. , vol.54 , pp. 144-56
    • Josephson, I.R.1    Sanchez-Chapula, J.2    Brown, A.M.3
  • 17
    • 0035901578 scopus 로고    scopus 로고
    • Instability and triangulation of the action potential predict serious proarrhythmia, but action potential prolongation is antiarrhythmic
    • Hondeghem LM Carlsson L Duker G. Instability and triangulation of the action potential predict serious proarrhythmia, but action potential prolongation is antiarrhythmic. Circulation 2001 103 : 2004 13.
    • (2001) Circulation , vol.103 , pp. 2004-13
    • Hondeghem, L.M.1    Carlsson, L.2    Duker, G.3
  • 19
    • 0033545725 scopus 로고    scopus 로고
    • Ks heterogeneity on action potential duration and its rate dependence: A simulation study
    • Ks heterogeneity on action potential duration and its rate dependence: A simulation study. Circulation 1999 99 : 2466 74.
    • (1999) Circulation , vol.99 , pp. 2466-74
    • Viswanathan, P.C.1    Shaw, R.M.2    Rudy, Y.3
  • 20
    • 0032735979 scopus 로고    scopus 로고
    • An investigation of the role played by the E-4031-sensitive (rapid delayed rectifier) potassium current in isolated rabbit atrioventricular nodal and ventricular myocytes
    • Mitcheson JS Hancox JC. An investigation of the role played by the E-4031-sensitive (rapid delayed rectifier) potassium current in isolated rabbit atrioventricular nodal and ventricular myocytes. Pflügers Arch. 1999 438 : 843 50.
    • (1999) Pflügers Arch. , vol.438 , pp. 843-50
    • Mitcheson, J.S.1    Hancox, J.C.2
  • 21
    • 0032401951 scopus 로고    scopus 로고
    • Control of L-type calcium current during the action potential of guinea-pig ventricular myocytes
    • Linz KW Meyer R. Control of L-type calcium current during the action potential of guinea-pig ventricular myocytes. J. Physiol. 1998 513 : 425 42.
    • (1998) J. Physiol. , vol.513 , pp. 425-42
    • Linz, K.W.1    Meyer, R.2
  • 22
    • 17344391838 scopus 로고    scopus 로고
    • Electrophysiology of sipatrigine: A lamotrigine derivative exhibiting neuroprotective effects
    • Calabresi P Stefani A Marfia GA et al. Electrophysiology of sipatrigine: A lamotrigine derivative exhibiting neuroprotective effects. Exp. Neurol. 2000 162 : 171 9.
    • (2000) Exp. Neurol. , vol.162 , pp. 171-9
    • Calabresi, P.1    Stefani, A.2    Marfia, G.A.3
  • 24
    • 0037373028 scopus 로고    scopus 로고
    • Differential interactions of lamotrigine and related drugs with transmembrane segment IVS6 of voltage-gated sodium channels
    • Liu G Yarov-Yarovoy V Nobbs M Clare JJ Scheuer T Catterall WA. Differential interactions of lamotrigine and related drugs with transmembrane segment IVS6 of voltage-gated sodium channels. Neuropharmacology 2003 44 : 413 22.
    • (2003) Neuropharmacology , vol.44 , pp. 413-22
    • Liu, G.1    Yarov-Yarovoy, V.2    Nobbs, M.3    Clare, J.J.4    Scheuer, T.5    Catterall, W.A.6
  • 27
    • 0031788811 scopus 로고    scopus 로고
    • On the inhibition of voltage activated calcium currents in rat cortical neurones by the neuroprotective agent 619C89
    • Stefani A Hainsworth A Spadoni F Bernardi G. On the inhibition of voltage activated calcium currents in rat cortical neurones by the neuroprotective agent 619C89. Br. J. Pharmacol. 1998 125 : 1058 64.
    • (1998) Br. J. Pharmacol. , vol.125 , pp. 1058-64
    • Stefani, A.1    Hainsworth, A.2    Spadoni, F.3    Bernardi, G.4
  • 31
    • 0142091429 scopus 로고    scopus 로고
    • Molecular determinants of high-affinity drug binding to HERG channels
    • Mitcheson JS Perry MD. Molecular determinants of high-affinity drug binding to HERG channels. Curr. Opin. Drug Discov. Dev. 2003 6 : 667 74.
    • (2003) Curr. Opin. Drug Discov. Dev. , vol.6 , pp. 667-74
    • Mitcheson, J.S.1    Perry, M.D.2
  • 32
    • 0035010434 scopus 로고    scopus 로고
    • Effects of extracellular pH on the interaction of sipatrigine and lamotrigine with high-voltage-activated (HVA) calcium channels in dissociated neurones of rat cortex
    • Hainsworth AH Spadoni F Lavaroni F Bernardi G Stefani A. Effects of extracellular pH on the interaction of sipatrigine and lamotrigine with high-voltage-activated (HVA) calcium channels in dissociated neurones of rat cortex. Neuropharmacology 2001 40 : 784 91.
    • (2001) Neuropharmacology , vol.40 , pp. 784-91
    • Hainsworth, A.H.1    Spadoni, F.2    Lavaroni, F.3    Bernardi, G.4    Stefani, A.5
  • 33
    • 0009737358 scopus 로고    scopus 로고
    • 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
    • Haverkamp W Breithardt G Camm AJ 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. 2000 47 : 219 33.
    • (2000) Cardiovasc. Res. , vol.47 , pp. 219-33
    • Haverkamp, W.1    Breithardt, G.2    Camm, A.J.3
  • 34
    • 0344492207 scopus 로고    scopus 로고
    • 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
    • Redfern WS Carlsson L Davis AS 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. 2003 58 : 32 45.
    • (2003) Cardiovasc. Res. , vol.58 , pp. 32-45
    • Redfern, W.S.1    Carlsson, L.2    Davis, A.S.3
  • 35
    • 0035033092 scopus 로고    scopus 로고
    • Phase 2 prolongation, in the absence of instability and triangulation, antagonizes class III proarrhythmia
    • Hondeghem LM Dujardin K De Clerck F. Phase 2 prolongation, in the absence of instability and triangulation, antagonizes class III proarrhythmia. Cardiovasc. Res. 2001 50 : 345 53.
    • (2001) Cardiovasc. Res. , vol.50 , pp. 345-53
    • Hondeghem, L.M.1    Dujardin, K.2    De Clerck, F.3
  • 36
    • 4344633215 scopus 로고    scopus 로고
    • Comparison of the in vitro electrophysiologic and proarrhythmic effects of amiodarone and sotalol in a rabbit model of acute atrioventricular block
    • Milberg P Ramtin S Monnig G et al. Comparison of the in vitro electrophysiologic and proarrhythmic effects of amiodarone and sotalol in a rabbit model of acute atrioventricular block. J. Cardiovasc. Pharmacol. 2004 44 : 278 86.
    • (2004) J. Cardiovasc. Pharmacol. , vol.44 , pp. 278-86
    • Milberg, P.1    Ramtin, S.2    Monnig, G.3
  • 38
    • 0029552523 scopus 로고
    • The tolerability, pharmacokinetics and pharmacodynamics of increasing intravenous doses of 619C89, a novel compound for the acute treatment of stroke, in healthy volunteers
    • Mercer AJ Lamb RJ Hussein Z Hobbiger S Posner J. The tolerability, pharmacokinetics and pharmacodynamics of increasing intravenous doses of 619C89, a novel compound for the acute treatment of stroke, in healthy volunteers. Ann. N.Y. Acad. Sci. 1995 765 : 324 6.
    • (1995) Ann. N.Y. Acad. Sci. , vol.765 , pp. 324-6
    • Mercer, A.J.1    Lamb, R.J.2    Hussein, Z.3    Hobbiger, S.4    Posner, J.5
  • 39
    • 0029887359 scopus 로고    scopus 로고
    • Pharmacokinetics of 619C89, a novel neuronal sodium channel inhibitor, in acute stroke patients after loading and discrete maintenance infusions
    • Hussein Z Fraser IJ Lees KR et al. Pharmacokinetics of 619C89, a novel neuronal sodium channel inhibitor, in acute stroke patients after loading and discrete maintenance infusions. Br. J. Clin. Pharmacol. 1996 41 : 505 11.
    • (1996) Br. J. Clin. Pharmacol. , vol.41 , pp. 505-11
    • Hussein, Z.1    Fraser, I.J.2    Lees, K.R.3
  • 41
    • 0033777534 scopus 로고    scopus 로고
    • Phase II clinical trial of sipatrigine (619C89) by continuous infusion in acute stroke
    • Muir KW Holzapfel L Lees KR. Phase II clinical trial of sipatrigine (619C89) by continuous infusion in acute stroke. Cerebrovasc. Dis. 2000 10 : 431 6.
    • (2000) Cerebrovasc. Dis. , vol.10 , pp. 431-6
    • Muir, K.W.1    Holzapfel, L.2    Lees, K.R.3
  • 42
    • 0031913533 scopus 로고    scopus 로고
    • Combined potassium and calcium channel antagonistic activities as a basis for neutral frequency dependent increase in action potential duration. Comparison between BRL-32872 and azimilide
    • Bril A Forest M-C Cheval B Faivre J-F. Combined potassium and calcium channel antagonistic activities as a basis for neutral frequency dependent increase in action potential duration. Comparison between BRL-32872 and azimilide. Cardiovasc. Res. 1998 37 : 130 40.
    • (1998) Cardiovasc. Res. , vol.37 , pp. 130-40
    • Bril, A.1    Forest, M.-C.2    Cheval, B.3    Faivre, J.-F.4
  • 43
    • 0032745315 scopus 로고    scopus 로고
    • Amiodarone: Ionic and cellular mechanisms of action of the most promising class III agent
    • Kodama I Kamiya K Toyama J. Amiodarone: Ionic and cellular mechanisms of action of the most promising class III agent. Am. J. Cardiol. 1999 84 : R20 8.
    • (1999) Am. J. Cardiol. , vol.84
    • Kodama, I.1    Kamiya, K.2    Toyama, J.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.