Identification and preclinical testing of novel antiepileptic compounds

Epilepsia

Volumn 38, Issue SUPPL. 9, 1997, Pages

  Meldrum, Brian S ^a  

^a KING'S COLLEGE LONDON   (United Kingdom)

Author keywords

Antiepileptic drugs; Drug screening; Epileptogenesis; GABA; Glutamate; Ion channels; Neurotransmitters; Receptors; Transporters

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; ANTICONVULSIVE AGENT; BENZODIAZEPINE DERIVATIVE; FELBAMATE; ION CHANNEL; LORECLEZOLE; NATURAL PRODUCT; PENTETRAZOLE; PHENYTOIN;

ABSENCE; CONFERENCE PAPER; DRUG MECHANISM; DRUG SCREENING; EPILEPSY; GENE DELETION; GENE TARGETING; HUMAN; HUMAN CELL; HUMAN TISSUE; MOLECULAR CLONING; NERVE CELL EXCITABILITY; PRIORITY JOURNAL;

EID: 0030664670     PISSN: 00139580     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1528-1157.1997.tb05204.x     Document Type: Conference Paper

References (97)

1. Krall RL, Penry JK, White BG, Kupferberg HJ, Swinyard EA. Antiepileptic drug development: II. Anticonvulsant drug screening. Epilepsia 1978;19:404-28.
2. Cereghino JJ, Kupferberg HJ. Preclinical testing. In: French JA, Dichter MA, Leppik IE, eds. New antiepileptic drug development: preclinical and clinical aspects. Amsterdam: Elsevier, 1993;19-30.
3. Löscher W, Schmidt D. Strategies in antiepileptic drug development: is rational drug design superior to random screening and structural variation. Epilepsy Res 1994;17:95-134.
4. Rogawski MA. Epilepsy. In: Pullan L, Patel J, eds. Neurotherapeutics: emerging strategies. Totowa, NJ: Humana Press, 1996: 193.
5. Meldrum BS. Current strategies for designing and identifying new antiepileptic drugs. In: Engel J Jr, Pedley TA, eds. Epilepsy: a comprehensive textbook. Philadelphia: Lippincott-Raven Publishers 1997:1405-16.
6. + channels expressed in a mammalian cell line by local anaesthetic, antiarrhythmic and anticonvulsant drugs. Mol Pharmacol 1991;40:756-65.
7. Macdonald RL, Meldrum BS. Principles of antiepileptic drug action. In: Levy RH, Mattson RH, Meldrum BS, eds. Antiepileptic drugs. 4th ed. New York: Raven Press, 1995:61-78.
8. + channels by local anaesthetics. Science 1994;265:1724-8.
9. + channels as targets for neuroprotective drugs. Trends Pharmacol Sci 1995;16:309-16.
10. Balser JR, Nuss HB, Chaimvimonvat N, Perez-Garcia MT, Marban E, Tomaselli GF. External pore residue mediates slow inactivation in U1 rat skeletal muscle sodium channels. J Physiol 1996;494: 431-42.
11. ++ channel currents in rat cerebellar granule neurons. J Neurosci 1995;15:2995-3012.
12. Caterall WA. Structure and function of voltage-gated ion channels. Annu Rev Biochem 1995;64:493-531.
13. ++ channel diversity. Annu Rev Neurosci 1994;17:399-418.
14. Caterall WA. Cellular and molecular biology of voltage-gated sodium channels. Physiol Rev 1992;72:15-48.
15. Cousin MA, Nicholls DG, Pocock JM. Flunarizine inhibits both calcium-dependent and -independent release of glutamate from synaptosomes and cultured neurones. Brain Res 1993;606:227-36.
16. 2+ channels as drug targets for the treatment of epilepsy or ischemic stroke. Neuropharmacology 1997;36.
17. + currents in neurones: types, physiological roles and modulation. Trends Neurol Sci 1996;19:150-4.
18. + channel openers decrease seizures in genetically epileptic rats. Eur J Pharmacol 1989;167:181-3.
19. Weston AH, Edwards G. Recent progress in potassium channel opener pharmacology. Biochem Pharmacol 1992;43:47-54.
20. Beck H, Blumke I, Kral T, et al. Properties of a delayed rectifier potassium current in dentate granule cells isolated from the hippocampus of patients with chronic temporal lobe epilepsy. Epilepsia 1996;37:892-901.
21. + uptake in glia prevents long-term depression maintenance and causes epileptiform activity. J Neurosci 1997;17: 2813-24.
22. Patil N, Cox DR, Bhat D, Faham M, Myers RM, Peterson AS. A potassium channel mutation in weaver mice implicates membrane excitability in granule cell differentiation. Nature Genet 1995;11: 126-9.
23. A and glycine receptors by chlormethiazole. Eur J Pharmacol 1992;210:239-46.
24. A receptor complex. Brain Res 1993;615:170-4.
25. Kokate TG, Svennson BE, Rogawski MA. Anticonvulsant activity of neurosteroids: correlation with gamma-aminobutyric acid-evoked chloride current potentiation. J Pharmacol Exp Ther 1994; 270:1223-9.
26. A) receptor. J Pharmacol Exp Ther 1996;277:1784-92.
27. A receptor beta-subunit. Neuron 1994;12: 775-82.
28. 2 subtypes of cloned γ-aminobutyric acid type A receptors. Mol Pharmacol 1993;44:866-70.
29. McKernan RM, Wafford K, Quirk K, et al. The pharmacology of the benzodiazepine site of the GABA-A receptor is dependent on the type of gamma-subunit present. J Recept Res 1995;15:173-83.
30. A receptor subtypes. Psychopharmacol Ser 1993;11:50-61.
31. Sieghart W. Structure and pharmacology of gamma-aminobutyric acidA receptor subtypes. Pharmacol Rev 1995;47:181-234.
32. A receptor subunit mRNAs in the rat brain. I. Telencephalon, diencephalon, mesencephalon. J Neurosci 1992;12:1040-62.
33. A receptor subunit mRNAs in 13 cell lines. J Neurosci 1994;14:5417-28.
34. A/ benzodiazepine receptor exclusively localized in the limbic system. Neuroreport 1996;8:117-22.
35. Tretter V, Ehya N, Fuchs K, Sieghart W. Stoichiometry and assembly of a recombinant GABAA receptor subtype. J Neurosci 1997;17:2728-37.
36. Hollmann M, Heinemann S. Cloned glutamate receptors. Annu Rev Neurosci 1994;17:31-108.
37. Hess SD, Daggett LP, Crona J, et al. Cloning and functional characterization of human heteromeric N-methyl-D-aspartate receptors. J Pharmacol Exp Ther 1996;278:808-16.
38. Ilyin VI, Whittemore ER, Guastella J, Weber E, Woodward RM. Subtype-selective inhibition of N-methyl-D-aspartate receptors by haloperidol. Mol Pharmacol 1996;50:1541-50.
39. Chapman AG, Meldrum BS. Non-competitive N-methyl-D-aspartate antagonists protect against sound-induced seizures in DBA/2 mice. Eur J Pharmacol 1989;166:201-11.
40. Meldrum BS, Chapman AG. Competitive NMDA antagonists as drugs. In: Watkins JC, Collingridge GL, eds. The NMDA receptor. Oxford: IRL Press, 1994:455.
41. 2+ permeability of AMPA receptors in principal neurons and interneurons in rat CNS. Neuron 1995;15:193-204.
42. Lomeli H, Mosbacher J, Melcher T, et al. Control of kinetic properties of AMPA receptor channels by nuclear RNA editing. Science 1994;266:1709-13.
43. Chapman AG, Smith SE, Meldrum BS. The anticonvulsant effect of the non-NMDA antagonists, NBQX and GYKI 52466, in mice. Epilepsy Res 1991;9:92-6.
44. Brusa R, Zimmermann F, Koh DS, et al. Early-onset epilepsy and postnatal lethality associated with an editing-deficient GluR-B allele in mice. Science 1995;270:1677-80.
45. Bleakman D, Schoepp DD, Ballyk B, et al. Pharmacological discrimination of GluR5 and GluR6 kainate receptor subtypes by (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydroisoquinoline-3 carboxylic acid. J Pharmacol Exp Ther 1996;49: 581-5.
46. Pin J-P, Duvoisin R. The metabotropic glutamate receptors: structure and functions. Neuropharmacology 1995;34:1-26.
47. Tizzano JP, Griffey KI, Schoepp DD. Induction or protection of limbic seizures in mice by mGlu subtype selective agonists. Neuropharmacology 1995;34:1063-7.
48. Thomsen C, Klitgaard H, Sheardown M, et al. (S)-4-carboxy-3-hydroxphenylglycine, an antagonist of metabotropic glutamate receptor (mGluR)1a and an agonist of mGluR2, protects against audiogenic seizures in DBA/2 mice. J Neurochem 1994;62: 2492-5.
49. Ghauri M, Chapman AG, Meldrum BS. Convulsant and anticonvulsant actions of agonists and antagonists of group II mGluRs. Neuroreport 1996;7:1469-74.
50. Tang E, Yip PK, Chapman AG, Jane DE, Watkins JC, Meldrum BS. Prolonged anticonvulsant action of glutamate metabotropic agonists in inferior colliculus of genetically epilepsy-prone rats. Eur J Pharmacol 1997;327:109-15.
51. Borden LA, Dhar TGM, Smith KE, Weinshank RL, Branchek TA, Gluchowski C. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol Mol Pharmacol 1994;269:219-24.
52. Mengel H. Tiagabine. Epilepsia 1994;35(suppl 5):S81-4.
53. Suzdak PD, Jansen JA. A review of the preclinical pharmacology of tiagabine: a potent and selective anticonvulsant GABA uptake inhibitor. Epilepsia 1995;36:612-26.
54. Dalby NO, Thomsen C, Fink-Jensen A, et al. Anticonvulsant properties of two GABA uptake inhibitors NNC 05-2045 and NNC 05-2090 not acting preferentially on GAT1. Epilepsy Res 1997;28:51-62.
55. Scanziani M, Salin PA, Vogt KE, Malenka RC, Nicoll RA. Use-dependent increases in glutamate concentration activate presynaptic metabotropic glutamate receptors. Nature 1997;385:630-4.
56. Millan MH, Chapman AG, Meldrum BS. Extracellular amino acid levels in hippocampus during pilocarpine-induced seizures. Epilepsy Res 1993;14:139-48.
57. Hausser M, Roth A. Dendritic and somatic glutamate receptor channels in rat cerebellar Purkinje cells. J Physiol 1997;501:77-95.
58. Amara SG, Kuhar MJ. Neurotransmitter transporters: recent progress. Annu Rev Neurosci 1993;16:73-93.
59. + exchangers in rat central nervous system. Neuroscience 1997;79: 591-603.
60. Lippert B, Metcalf BW, Jung MJ, Casara P. 4-amino-hex-5-enoic acid, a selective catalytic inhibitor of 4-aminobutyric acid aminotransferase in mammalian brain. Eur J Biochem 1977;74:441-5.
61. A receptors. Science 1995;269:977-81.
62. Meldrum BS, Horton RW. Neuronal inhibition mediated by GABA and patterns of convulsions in baboons with photosensitive epilepsy (Papio papio). In: Harris P, Mawdsley C, eds. Epilepsy. Edinburgh: Churchill Livingstone, 1974:55-64.
63. Hosford DA. Models of primary generalized epilepsy. Curr Opin Neurol 1995;8:121-5.
64. Hosford DA, Wang Y. Utility of the lethargic (lh/lh) mouse model of absence seizures in predicting the effects of lamotrigine, vigabatrin, tiagabine, gabapentin, and topiramate against human absence seizures. Epilepsia 1997;38:408-14.
65. B receptor activation in absence seizures of lethargic (lh/lh) mice. Science 1992;257:398-401.
66. B and gamma-hydroxybutyric acid-mediated mechanisms in generalised absence seizures. Neuropharmacology 1996;35:359-67.
67. Fletcher CF, Lutz CM, O'Sullivan TM, et al. Absence epilepsy in tottering mutant mice is associated with calcium channel defects. Cell 1996;87:607-17.
68. 2+ channel beta subunit gene Cchb4 is associated with ataxia and seizures in the lethargic (lh) mouse. Cell 1997;88:385-92.
69. Gillard SE, Volsen SG, Smith W, Beattie RE, Bleakman D, Lodge D. Identification of pore-forming subunit of P-type calcium channels: an antisense study on rat cerebellar Purkinje cells in culture. Neuropharmacology 1997;36:405-9.
70. Meldrum BS. Update on the mechanism of action of antiepileptic drugs. Epilepsia 1996;37(suppl 6):S4-11.
71. Barrantes GE, Ortells MO, Barrantes FJ. Screening structuralfunctional relationships of neuropharmacologically active organic compounds at the nicotinic acetylcholine receptor. Neuropharmacology 1997;36:269-79.
72. Hogan JC Jr. Directed combinatorial chemistry. Nature 1996;384: 17-22.
73. Akiyama K, Daigen A, Yamada N, et al. Long-lasting enhancement of metabotropic excitatory amino acid receptor-mediated polyphosphoinositide hydrolysis in the amygdala/pyriform cortex of deep prepiriform cortical kindled rats. Brain Res 1992;569: 71-7.
74. During MJ, Ryder KM, Spencer DD. Hippocampal GABA transporter function in temporal-lobe epilepsy. Nature 1995;376:174-7.
75. Köhr G, de Koninck Y, Mody I. Properties of NMDA receptor channels in neurons acutely isolated from epileptic (kindled) rats. J Neurosci 1993;13:3612-27.
76. Mody I. The molecular basis of kindling. Brain Pathol 1993;3: 395-403.
77. Noebels JL. Targeting epilepsy genes. Neuron 1996;16:241-4.
78. Pennacchio LA, Lehesjoki AE, Stone NE, et al. Mutations in the gene encoding cystatin B in progressive myoclonus epilepsy (EPM1). Science 1996;271:1731-4.
79. Lalioti MD, Mirotsou M, Buresi C, et al. Identification of mutations in cystatin B, the gene responsible for the Unverricht-Lundborg type of progressive myoclonus epilepsy (EPM1). Am J Hum Genet 1997;60:342-51.
80. Noebels JL. A single gene error in noradrenergic axon growth synchronizes central neurons. Nature 1994;310:409-11.
81. Beck H, Moulard B, Steilein U, et al. A nonsense mutation in the alpha4 subunit of the nicotinic acetylcholine receptor (CHRNA4) cosegregates with 20q-linked benign neonatal familial convulsions. (EHN1). Neurobiol Dis 1994;1:95-9.
82. Forman SA, Yellen G, Thiele EA. Alternative mechanism for pathogenesis of an inherited epilepsy by a nicotinic AChR mutation. Nature Genet 1996;13:396-7.
83. Weiland S, Witzemann V, Villarroel A, Propping P, Steinlein U. An amino acid exchange in the second transmembrane segment of a neuronal nicotinic receptor causes partial epilepsy by altering its desensitization kinetics. FEBS Lett 1996;398:91-6.
84. Tsirka SE, Gualandris A, Amaral DG, Strickland S. Excitotoxin-induced neuronal degeneration and seizure are mediated by tissue plasminogen activator. Nature 1995;377:340-4.
85. Cain DP, Cant SGN, Saucier D, Hargreaves EL, Kandel ER. Fyn tyrosine kinase is required for normal amygdala kindling. Epilepsy Res 1995;22:107-14.
86. Kokaia M, Ernfors P, Kokaia Z, Elmer E, Jaenisch R, Linvall O. Suppressed epileptogenesis in BDNF mutant mice. Exp Neurol 1995;133:215-24.
87. Sveinbjornsdottir S, Sander JWAS, Upton D, et al. The excitatory amino acid antagonist D-CPP-ene (SDZ EAA-494) in patients with epilepsy. Epilepsy Res 1993;16:165-74.
88. Honavar M, Meldrum BS. Epilepsy. In: Graham DI, Lantos PL, eds. Greenfield's neuropathology. 6th ed. London: Arnold, 1997;931-71.
89. Meldrum BS. Epileptic brain damage: a consequence and a cause of seizures. The first Alfred Meyer Memorial Lecture. Neuropathol Appl Neurobiol 1997;23:185-202.
90. Gall CM, Isackson PJ. Limbic seizures increase neuronal production of messenger RNA for nerve growth factor. Science 1989; 245:758-61.
91. Bengzon J, Söderström S, Kokaia Z, et al. Widespread increase of nerve growth factor protein in the rat forebrain after kindling-induced seizures. Brain Res 1992;587:338-42.
92. Thoenen H. Neurotrophins and neuronal plasticity. Science 1995; 270:593-8.
93. Van der Zee CEEM, Rashid K, Le K, et al. Intraventricular administration of antibodies to nerve growth factor retards kindling and blocks mossy fiber sprouting in adult rats. J Neurosci 1995; 15:5316-23.
94. Martinez-Serrano A, Bjorklund A. Protection of the neostriatum against excitotoxic damage by neurotrophin-producing, genetically modified neural stem cells. J Neurosci 1996;16:4604-16.
95. Hyman SE. Regulation of gene expression of neural signals. Neuroscientist 1996;2:217-24.
96. Kiessling M, Gass P. Immediate early gene expression in experimental epilepsy. Brain Pathol 1993;3:381-93.
97. During MJ, Mirchandani GR, Leone P, et al. Direct hippocampal injection of a HSV-1 vector expressive GLUR6 results in spontaneous seizures, hyperexcitability in CA1 cells and loss of CA1, hilar and CA3 neurons [Abstract]. Soc Neurosci Abstr 1993;19:21.