Neurochemical actions of the desglycinyl metabolite of remacemide hydrochloride (ARL 12495AA) in mouse brain

British Journal of Pharmacology

Volumn 121, Issue 5, 1997, Pages 923-926

  Leach, John Paul ^a   Sills, Graeme J ^a   Butler, Elaine ^a   Forrest, Gerard ^a   Thompson, George G ^a   Brodie, Martin J ^a  

^a WESTERN INFIRMARY   (United Kingdom)

Author keywords

aminobutyric acid (GABA); aminobutyric acid transaminase (GABA T); Active metabolite; Antiepileptic drugs; Epilepsy; Glutamate; Glutamic acid decarboxylase (GAD); Glutamine; Remacemide

Indexed keywords

1 METHYL 1,2 DIPHENYLETHYLAMINE; 4 AMINOBUTYRATE AMINOTRANSFERASE; 4 AMINOBUTYRIC ACID; ANTICONVULSIVE AGENT; DRUG METABOLITE; GLUTAMATE DECARBOXYLASE; GLUTAMIC ACID; GLUTAMINE; REMACEMIDE;

4 AMINOBUTYRIC ACID BRAIN LEVEL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRAIN LEVEL; BRAIN TISSUE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG MECHANISM; ENZYME ACTIVITY; INTRAPERITONEAL DRUG ADMINISTRATION; MALE; MOUSE; NEUROCHEMISTRY; NONHUMAN; PRIORITY JOURNAL;

4-AMINOBUTYRATE TRANSAMINASE; ANIMALS; BRAIN CHEMISTRY; EXCITATORY AMINO ACID ANTAGONISTS; GAMMA-AMINOBUTYRIC ACID; GLUTAMATE DECARBOXYLASE; GLUTAMIC ACID; GLUTAMINE; MALE; MICE; MICE, INBRED ICR; PHENETHYLAMINES; STEREOISOMERISM;

EID: 0030996332     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0701219     Document Type: Article

References (26)

1. CRAMER, C.L., STAGNITTO, M.L., KNOWLES, M.A. & PALMER, G.C. (1994). Kainic acid and 4-aminopyridine seizure models in mice: Evaluation of efficacy of antiepileptic agents and calcium antagonists. Life Sci., 54, 271-275.
2. GALE, K. (1989). GABA in epilepsy: The pharmacologic basis. Epilepsia, 30, S1-S11.
3. GALE, K. GABA and epilepsy: Basic concepts from preclinical research. Epilepsia, 33, S3-S12.
4. GARSKE, G.E., PALMER, G.C., NAPIER, J.J., GRIFFITH, R.C., FREEDMAN, L.R., HARRIS, E.W., RAY, R., MCCREEDY, S.A., BLOSSER, J.C., WOODHEAD, J.H., WHITE, H.S. & SWINYARD, E.A. (1991). Preclinical profile of the anticonvulsant remacemide and its enantiomers in the rat. Epilepsy Res. 9, 161-174.
5. GOLDLUST, A., SU, T-Z., WELTY, D.F., TAYLOR, C.P. & OXENDER, D.L. (1995). Effects of anticonvulsant drug gabapentin on the enzymes in metabolic pathways of glutamate and GABA. Epilepsy Res., 22, 1-11.
6. HEYN, H., MCCARTHY, D.J., CURRY, S.H., EISMAN, M.S. & ANDERS, M.W. (1994). Brain uptake and biotransformation of remacemide hydrochloride, a novel anticonvulsant. Drug Metab. Disp., 22, 443-446.
7. HU, R.Q. & DAVIES, J.A. (1995). The effect of the desglycinyl metabolite of remacemide on cortical wedges prepared from DBA/2 mice. Eur. J. Pharmacol. 287, 251-256.
8. LEACH, J.P. & BRODIE, M.J. (1995). New antipileptic drugs - an explosion of activity. Seizure, 4, 5-17.
9. LEACH, J.P., GIRVAN, J., JAMIESON, V., JONES, T., RICHENS, A. & BRODIE, M.J. (1996). Pharmocokinetic interactions between remacemide and carbamazepine: two drugs with active metabolites. Epilepsia, 37, 1100-1106.
10. LEACH, J.P., GIRVAN, J., JAMIESON, V., JONES, T., RICHENS, A. & BRODIE, M.J. (1997a). Mutual interaction between remacemide hydrochloride and phenytoin. Epilepsy Res., 26, 381-388.
11. LEACH, J.P., SILLS, G.J., BUTLER, E., FORREST, G., THOMPSON, G.G. & BRODIE, M.J. (1997b). Neurochemical actions of gabapentin in mouse brain. Epilepsy Res., (in press).
12. LEACH, J.P., SILLS, G.J., BUTLER, E., FORREST, G., THOMPSON, G.G. & BRODIE, M.J. (1997c). Neurochemical actions of vigabatrin and tiagabine alone and in combination in mouse cortex. Gen. Pharmacol., (in press).
13. MUIR, K.T. & PALMER, G.C. (1991). Remacemide. In New Antiepileptic Drugs (Epilepsy Res. Suppl. 3). ed. Pisani F., Perucca, E., Avanzini, G. & Richens, A. pp. 147-152. Amsterdam: Elsevier.
14. MURPHY, J.M., MOTIWALA, R. & DEVINSKY, O. (1991). Phenytoin intoxication. South. Med. J., 84, 1199-1204.
15. OSORIO, J., BURNSTINE, T.H., REMLER, B., MANON-ESPAILLAT, R. & REED, R.C. (1989). Phenytoin-induced seizures: A paradoxical effect at toxic concentrations in epileptic patients. Epilepsia, 30, 230-234.
16. PALMER, G.C., CLARK, B. & HUTCHISON, J.B. (1993). Antiepileptic and neuroprotective potential of remacemide hydrochloride. Drugs Future, 18, 1021-1042.
17. PALMER, G.C., HARRIS, E.W., RAY, R., STAGNJTTO, M.L. & SCHMIESING, R.J. (1992). Classification of compounds for prevention of NMDLA-induced seizures/mortality, or maximal electroshock and pentylenetetrazol seizures in mice and antagonism of MK-801 binding in vitro. Arch. Int. Pharmacodyn. Ther., 317, 16-34.
18. PALMER, G.C., STAGNITTO, M.L., ORDY, J.M., GRIFFITH, R.C., NAPIER, J.J., GENTILE, R.J., WOODHEAD, J.H., WHITE, H.S. & SWINYARD, E.A. (1991). Preclinical profile of stereoisomers of the anticonvulsant remacemide in mice. Epilepsy Res., 8, 36-48.
19. REYNOLDS, E.H. (1989). Phenytoin toxicity. In Antiepileptic Drugs, Third Edition. ed. Levy, R., Mattson, R., Meldrum, B., Penry, J.K. & Dreifuss, F.E. pp. 241-255. New York: Raven Press.
20. ROGAWSKI, M.A. & PORTER, R.J. (1990). Antiepileptic drugs: Pharmacological mechanisms and clinical efficacy with consideration of promising developmental stage compounds. Pharmacol. Rev., 42, 223-286.
21. SILLS, G.J., LEACH, J.P., ERASER, C.M., FORREST, G., PATSALOS, P.N. & BRODIE, M.J. (1997). Neurochemical studies with the novel anticonvulsant levetiracetam in mouse brain. Eur. J. Pharmacol., (in press).
22. SRINIVASAN, J., RICHENS, A. & DAVIES, J.A. (1995). The effect of the desglycinyl metabolite of remacemide hydrochloride (FPL 12495AA) and dizocilpine (MK-801) on endogenous amino acid release from mouse cortex. Br. J. Pharmacol., 116, 3087-3092.
23. STABLES, J.P., BIALER, M., JOHANNESSEN, S.I., KUPFERBERG, H.J., LEVY, R.H., LOISEAU, P. & PERUCCA, E. (1995). Progress report on new antiepileptic drugs. A summary of the Second Eilat Conference. Epilepsy Res., 22, 235-246.
24. STAGNITTO, M.L., PALMER, G.C., ORDY, J.M., GRIFFITH, R.C., NAPIER, J.J., BECKER, C.W., GENTILE, R.J., GARSKE, G.E., FRANKENHEIM, J.M., WOODHEAD, J.H. & SWINYARD, E.A. (1990). Preclinical profile of remacemide: A novel anticonvulsant effective against maximal electroshock seizures in mice. Epilepsy Res., 7, 11-28.
25. SUBRAMANIAM, S., DONEVAN, S.D. & ROGAWSKI, M.A. (1996). Block of the N-methyl-D-aspartate receptor by remacemide and its des-glycine metabolite. J. Pharmacol. Exp. Ther., 276, 161-168.
26. WAMIL, A.W., CHEUNG, H., HARRIS, E.W. & MCLEAN, M.J. (1996). Remacemide HCl and its metabolite, FPL 12495AA, limit action potential firing frequency and block NMDA responses of mouse spinal cord neurons in cell culture. Epilepsy Res., 23, 1-14.