Inhibition by lifarizine of intracellular Ca2+ rises and glutamate exocytosis in depolarized rat cerebrocortical synaptosomes and cultured neurones

British Journal of Pharmacology

Volumn 118, Issue 1, 1996, Pages 162-166

  Budd, David C ^b   May, Gillian R ^a,c   Nicholls, David G ^b   McCormack, James G ^a,d  

^a HERIOT WATT UNIVERSITY   (United Kingdom)

^b UNIVERSITY OF DUNDEE   (United Kingdom)

^c UNIVERSITY OF EDINBURGH   (United Kingdom)

^d NOVO NORDISK A S   (Denmark)

Author keywords

Cultured neurones; Depolarization; Glutamate exocytosis; Intracellular Ca2+; Lifarizine; Synaptosomes

Indexed keywords

CALCIUM CHANNEL; CALCIUM CHANNEL BLOCKING AGENT; CALCIUM ION; FURA 2; GLUTAMATE DEHYDROGENASE; GLUTAMIC ACID; LIFARIZINE; POTASSIUM CHLORIDE; SODIUM CHANNEL;

ANIMAL CELL; ARTICLE; BRAIN CORTEX; CALCIUM CELL LEVEL; CONTROLLED STUDY; DEPOLARIZATION; DOSE RESPONSE; EXOCYTOSIS; MALE; NERVE CELL; NERVE CELL CULTURE; NEUROPROTECTION; NONHUMAN; PRIORITY JOURNAL; RAT; SYNAPTOSOME;

ANIMALS; CALCIUM; CELLS, CULTURED; CEREBRAL CORTEX; CYTOSOL; EXOCYTOSIS; GLUTAMIC ACID; IMIDAZOLES; MALE; NEURONS; NEUROPROTECTIVE AGENTS; PIPERAZINES; POTASSIUM CHLORIDE; RATS; RATS, WISTAR; SODIUM CHANNELS; SYNAPTOSOMES;

EID: 0029876306     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1476-5381.1996.tb15380.x     Document Type: Article

References (34)

1. ALPS, B.J. (1992). Drugs acting on calcium channels: potential treatment for ischaemic stroke. Br. J. Clin. Pharmacol., 34, 199-206.
2. ALPS, B.J., CALDER, C., HASS, W.K. & WILSON, A.D. (1988). Comparative protective effects of nicardipine, flunarizine, lidoflazine and nimodipine against ischaemic injury in the hippocampus of the Mongolian gerbil. Br. J. Pharmacol., 93, 877-883.
3. ALPS, B.J., CALDER, C., HASS, W.K. & WILSON, A.D. (1990). Cerebral protection with a novel calcium blocker in rats. Proc. XXth Intl. Congr. Med. (ISIM Satellite), Stockholm, Sweden.
4. BRADFORD, M.M. (1976). A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal. Biochem., 72, 248-254.
5. BROWN, C.M., CALDER, C., ALPS, B.J. & SPEDDING, M. (1993). The effect of lifarizine (RS-87476), a novel sodium and calcium channel modulator, on ischaemic dopamine depletion in the corpus striatum of the gerbil. Br. J. Pharmacol., 109, 175-177.
6. BROWN, C.M., RUSH, W.R. & COLQUHOUN, H.A. ( 1995a). Lifarizine: a blocker of inactivated voltage-dependent sodium channels and calcium channels with cerebral neuroprotective action. CNS Drug Rev., 1 (2), 149-167.
7. BROWN, C.M., SMALL, C., CALDER, C. & PATMORE, L. (1995b). Neuroprotective properties of lifarizine compared with those of other agents in a mouse model of focal ischaemia. Br. J. Pharmacol. ?tf=″Times-b″> 115, 1425-1432.
8. BUDD, D.C. & NICHOLLS, D.G. (1995). Protein kinase C-mediated suppression of the presynaptic adenosine A1 receptor by a facilitatory metabotrophic glutamate receptor. J. Neurochem., 65, 615-621.
9. CHOI, D.W. (1987). Ionic dependence of glutamate neurotoxicity in cortical cell culture. J. Neurosci., 7, 369-379.
10. CHOI, D.W. (1988). Calcium-mediated neurotoxicity: relationship to specific channel types and role in ischemic damage. Trends Neurosci., 11, 465-469.
11. COUSIN, M.A., NICHOLLS, D.G. & POCOCK, J.M. (1993). Flunarizine inhibits both calcium-dependent and -independent release of glutamate from synaptosomes and cultured neurones. Brain Res., 606, 227-236.
12. DUNKLEY, P.R., HEATH, J.W., HARRISON, S.M., JARVIE, P.E., GLENFIELD, P.J. & ROSTAS, J.A. (1988). A rapid Percoll gradient procedure for isolating synaptosomes from an S1 fraction: homogeneity and morphology of subcellular fractions. Brain Res., 441, 59-71.
13. FRASER, S AND SPEDDING, M. (1991). RS-87476, a novel neuroprotective agent, antagonises the effects of calcium channel activators in guinea-pig taenia. Br. J. Pharmacol., 104, 156P.
14. GILL, R., BRAZELL, C., WOODRUFF, G.N. & KEMP, J.A. (1991). The neuroprotective action of dizocilpine (MK-801) in the rat middle cerebral artery occlusion model of focal ischaemia. Br. J. Pharmacol., 103, 2030-2036.
15. GRAHAM, D., DARLES, G. & LANGER, S.Z. (1992). The neuroprotective properties of ifenprodil, a novel NMDA receptor antagonist, in neuronal cell culture toxicity studies. Eur. J. Pharmacol., 226, 373-376.
16. GRAHAM, S.H., CHEN, J., LAN, J., LEACH, M.J. & SIMON, R.P. (1994). Neuroprotective effects of a use-dependent blocker of voltage-dependent sodium channels, BW619C89, in rat middle cerebral artery occlusion. J. Pharmacol. Exp. Ther., 269, 854-859.
17. GRYNKIEWICZ, G., POENIE, M. & TSIEN, R.Y. (1985). A new generation of calcium indicators with greatly improved fluorescence properties. J. Biol. Chem., 260, 3440-3450.
18. 2+ concentration in isolated nerve terminals following metabolic inhibition: possible relevance to hypoglycaemia and anoxia. Neuroscience, 27, 175-182.
19. KUCHARCYZK, J., MINTROVITCH, J., MOSELEY, M.E., ASGARI, H.S., SEVICK, R.J., DERUGIN, N. & NORMAN, D. (1991). Ischemic brain damage: reduction by sodium-calcium ion channel modulator RS-87476. Radiology, 179, 221-227.
20. LEACH, M.J., SWAN, J.H., EISENTHAL, D., DOPSON, M. & NOBBS, M. (1993). BU619C89, a glutamate release inhibitor, protects against focal cerebral ischemic damage. Stroke, 24, 1063-1067.
21. 3H]-lifarizine, a high affinity probe for inactivated sodium channels. Br. J. Pharmacol., 115, 1103-1109.
22. MAY, G.R., ROWAND, W.S., MCCORMACK, J.G. & SHERIDAN, R.D. (1995). Neuroprotective profile of lifarizine (RS-87476-190) in rat cerebrocortical neurones in culture. Br. J. Pharmacol., 114, 1365-1370.
23. MCGIVERN, J.G., SHERIDAN, R.D. & PATMORE, L. (1995). Actions of the novel neuroprotective agent, lifarizine (RS-87476), on voltage-dependent sodium currents in the neuroblastoma cell line, N1E-115. Br. J. Pharmacol., 114, 1738-1744.
24. NICHOLLS, D.G. (1978). Calcium transport and proton electrochemical potential gradient in mitochondria from guinea-pig cerebral cortex and rat heart. Biochem. J., 170, 511-522.
25. NICHOLLS, D.G., SIHRA, T.S. & SANCHEZ-PRIETO, J. (1987). Calcium-dependent and -independent release of glutamate from synaptosomes monitored by continuous fluorometry. J. Neurochem., 49, 50-57.
26. PARK, C.K., NEHLS, D.G., GRAHAM, D.I., TEASDALE, G.M. & MCCULLOCH, J. (1988). The glutamate antagonist MK-801 reduces focal ischemic brain damage in the rat. Ann. Neurol., 24, 543-551.
27. 2+-mediated neuronal death in rat brain neuronal cultures by veratridine: protection by flunarizine. Mol. Pharmacol., 36, 525-531.
28. POCOCK, J.M., COUSIN, M.A. & NICHOLLS, D.G. (1993). The calcium channel coupled to the exocytosis of L-glutamate from cerebellar granule cells is inhibited by the spider toxin Aga-GI. Neuropharmacol., 32, 1185-1194.
29. PRENEN, G.H., GO, K.G., POSTEMA, F., ZUIDERVEEN, F. & KORF, J. (1988). Cerebral cation shifts in hypoxic-ischemic brain damage are prevented by the sodium channel blocker letrodotoxin. Exp. Neurol., 99, 118-132.
30. + entry through tetrodotoxin-sensitive channels. Biochem. J., 304, 353-357.
31. SHERIDAN, R.D., PATMORE, L. & SPEDDING, M. (1991). The novel neuroprotective agent, RS-87476, potently inhibits sodium currents in mouse neuroblastoma. Br. J. Pharmacol., 104, 25P.
32. SZATKOWSKI, M. & ATWELL, D. (1994). Triggering and execution of neuronal death in brain ischaemia: two phases of glutamate release by different mechanisms. Trends Neurosci., 17, 359-365.
33. WEISS, J.H., HARTLEY, D.M., KOH, J. & CHOI, D.W. (1990). The calcium channel blocker nifedipine attenuates slow excitatory amino acid neurotoxicity. Science, 247, 1474-1477.
34. YAMASAKI, Y., KOGURE, K., HARA, H., BAN, H. & AKAIKE, N. (1991). The possible involvement of tetrodotoxin-sensitive ion channels in ischemic neuronal damage in the rat hippocampus. Neurosci. Lett., 121, 251-254.