GABA-level increasing and anticonvulsant effects of three different GABA uptake inhibitors

Neuropharmacology

Volumn 39, Issue 12, 2000, Pages 2399-2407

  Dalby, Nils Ole ^a  

^a NOVO NORDISK A S   (Denmark)

Author keywords

Electroshock; Epilepsy; GABA transporter; Microdialysis; Microinjection

Indexed keywords

1 [2 [TRIS(4 METHOXYPHENYL)METHYL]ETHYL] 3 PIPERIDINECARBOXYLIC ACID; 4 AMINOBUTYRIC ACID; ANTICONVULSIVE AGENT; NCC 052045; NEUROTRANSMITTER UPTAKE INHIBITOR; TIAGABINE; UNCLASSIFIED DRUG;

4 AMINOBUTYRIC ACID UPTAKE; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CENTRAL NERVOUS SYSTEM; CONTROLLED STUDY; EPILEPSY; GABAERGIC TRANSMISSION; HIPPOCAMPUS; MALE; MICRODIALYSIS; NIGRONEOSTRIATAL SYSTEM; NONHUMAN; PRIORITY JOURNAL; RAT; THALAMUS; TONIC SEIZURE;

ACOUSTIC STIMULATION; ANESTHESIA; ANIMALS; ANISOLES; ANTICONVULSANTS; CARBAZOLES; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CONVULSANTS; ELECTROSHOCK; FEMALE; GABA AGONISTS; GABA ANTAGONISTS; GAMMA-AMINOBUTYRIC ACID; HIPPOCAMPUS; MALE; MICE; MICE, INBRED DBA; MICRODIALYSIS; NEUROTRANSMITTER UPTAKE INHIBITORS; NIPECOTIC ACIDS; PENTYLENETETRAZOLE; PIPERIDINES; SEIZURES; SUBSTANTIA NIGRA; THALAMUS;

EID: 0033884270     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0028-3908(00)00075-7     Document Type: Article

References (39)

1. Ahn J., Mundigl O., Muth T.R., Rudnick G., Caplan M.J. Polarized expression of gaba transporters in madin-darby canine kidney-cells and cultured hippocampal-neurons. J. Biol. Chem. 271:1996;6917-6924.
2. Borden L.A., Smith K.E., Hartig P.R., Branchek T.A., Weinshank R.L. Molecular heterogeneity of the gamma-aminobutyric acid (GABA) transport system. Cloning of two novel high affinity GABA transporters from rat brain. J. Biol. Chem. 267:1992;21098-21104.
3. Borden L.A., Murali Dhar T.G., Smith K.E., Weinshank R.L., Branchek T.A., Gluchowski C. Tiagabine, SK&F 89976-A, Cl-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur. J. Pharmacol. 269:1994;219-224.
4. Borden L.A., Smith K.E., Gustafson E.L., Branchek T.A., Weinshank R.L. Cloning and expression of a betaine/GABA transporter from human brain. J.Neurochem. 64:1995;977-984.
5. Burnham C.E., Buerk B., Schmidt C., Bucuvalas J.C. A liver-specific isoform of the betaine/GABA transporter in the rat: cDNA sequence and organ distribution. Biochim. Biophys. Acta. 1284:1996;4-8.
6. Chen L.S., Millington D.S., Maltby D.A., McNamara J.O. Effects of intranigral application of clinically-effective anticonvulsants on electroshock-induced seizures. Neuropharmacology. 28:1989;781-786.
7. Clark J.A., Deutch A.Y., Gallipoli P.Z., Amara S.G. Functional expression and CNS distribution of a beta-alanine-sensitive neuronal GABA transporter. Neuron. 9:1992;337-348.
8. Croucher M.J., Meldrum B.S., Krogsgaard-Larsen P. Anticonvulsant activity of GABA uptake inhibitors and their prodrugs following central or systemic administration. Eur. J. Pharmacol. 89:1983;217-228.
9. Dalby N.O., Nielsen E.B. Comparison of the preclinical anticonvulsant profiles of tiagabine, lamotrigine, gabapentin and vigabatrin. Epilepsy Res. 28:1997;63-72.
10. Dalby N.O., Nielsen E.B. Tiagabine exerts an anti-epileptogenic effect in amygdala kindling epileptogenesis in the rat. Neurosci. Lett. 229:1997;135-137.
11. Dalby N.O., Thomsen C., Fink-Jensen A., Lundbeck J., Sokilde B., Man C.M., Sørensen P.O., Meldrum B. Anticonvulsant properties of two GABA uptake inhibitors NNC 05 2045 and NNC 05-2090, not acting preferentially on GAT-1. Epilepsy Res. 28:1997;51-61.
12. De Biasi S., Vitellaro-Zuccarello L., Brecha N.C. Immunoreactivity for the GABA transporter-1 and GABA transporter-3 is restricted to astrocytes in the rat thalamus. A light and electron-microscopic immunolocalization. Neuroscience. 83:1998;815-828.
13. Dhar T.G., Borden L.A., Tyagarajan S., Smith K.E., Branchek T.A., Weinshank R.L., Gluchowski C. Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. J. Med. Chem. 37:1994;2334-2342.
14. Fink-Jensen A., Suzdak P.D., Swedberg M.D., Judge M.E., Hansen L., Nielsen P.G. The gamma-aminobutyric acid (GABA) uptake inhibitor, tiagabine, increases extracellular brain levels of GABA in awake rats. Eur. J. Pharmacol. 220:1992;197-201.
15. Gale K. GABA and epilepsy: basic concepts from preclinical research. Epilepsia. 5(Suppl.):1992;3-12.
16. Garant D.S., Gale K. Substantia nigra-mediated anticonvulsant actions: role of nigral output pathways. Exp. Neurol. 97:1987;143-159.
17. Guastella J., Nelson N., Nelson H., Czyzyk L., Keynan S., Miedel M.C., Davidson N., Lester H.A., Kanner B.I. Cloning and expression of a rat brain GABA transporter. Science. 249:1990;1303-1306.
18. Horton R.W., Collins J.F., Anlezark G.M., Meldrum B.S. Convulsant and anticonvulsant actions in DBA/2 mice of compounds blocking the reuptake of GABA. Eur. J. Pharmacol. 59:1979;75-83.
19. ladarola M.J., Gale K. Substantia nigra: site of anticonvulsant activity mediated by gamma-aminobutyric acid. Science. 218:1982;1237-1240.
20. Ikegaki N., Saito N., Hashima M., Tanaka C. Production of specific antibodies against GABA transporter subtypes (GAT1, GAT2, GAT3) and their application to immunocytochemistry. Mol. Brain Res. 26:1994;47-54.
21. Litchfield J.T., Wilcoxon F. A simplified method of evaluating dose-effect experiments. J. Pharmacol. Exp. Ther. 96:1949;99-113.
22. Liu Q.R., Lopez-Corcuera B., Mandiyan S., Nelson H., Nelson N. Molecular characterization of four pharmacologically distinct gamma-aminobutyric acid transporters in mouse brain. J. Biol. Chem. 268:1993;2106-2112.
23. Lopez-Corcuera B., Liu Q.R., Mandiyan S., Nelson H., Nelson N. Expression of a mouse brain cDNA encoding novel gamma-aminobutyric acid transporter. J. Biol. Chem. 267:1992;17491-17493.
24. Meldrum B.S. GABAergic mechanisms as treatment of epilepsy. Br. J. Clin. Pharmacol. 27:1988;35-115.
25. Miller J.W., Kleven D.T., Domin B.A., Fremeau R.T. Cloned sodium-(and chloride-) dependent high-affinity transporters for GABA, glycine, proline, betaine, taurine, and creatine. Reith M.E.A. Neurotransmitter Transporters - Structure, Function and Regulation. 1997;101-128 Humana Press, New Jersey.
26. Muth T.R., Ahn J., Caplan M.J. Identification of sorting determinants in the c-terminal cytoplasmic tails of the gamma-aminobutyric-acid transporters gat-2 and gat-3. J. Biol. Chem. 273:1998;25616-25627.
27. Nielsen E.B., Suzdak P.D., Andersen K.E., Knutsen L.J., Sonnewald U., Braestrup C. Characterization of tiagabine (NO-328), a new potent and selective GABA uptake inhibitor. Eur. J. Pharmacol. 196:1991;257-266.
28. Paxinos G., Watson C. The Rat Brain in Stereotaxic Coordinates. 1986;Academic Press, New York.
29. Ribak C.E., Tong W.M., Brecha N.C. GABA plasma membrane transporters, GAT-1 and GAT-3, display different distributions in the rat hippocampus. J. Comp. Neurol. 367:1996;595-606.
30. Richards D.A., Bowery N.G. Comparative effects of the GABA uptake inhibitors, tiagabine and NNC-711, on extracellular GABA levels in the rat ventrolateral thalamus. Neurochem. Res. 21:1996;135-140.
31. Roth M. Flourescence reaction for amino acids. Analyt. Chem. 43:1971;880-882.
32. Smith S.E., Parvez N.S., Chapman A.G., Meldrum B.S. The gamma-aminobutyric acid uptake inhibitor, tiagabine, is anticonvulsant in two animal models of reflex epilepsy. Eur. J. Pharmacol. 273:1995;259-265.
33. Suzdak P.D., Frederiksen K., Andersen K.E., Sørensen P.O., Knutsen L.J., Nielsen E.B. NNC-711, a novel potent and selective gamma-aminobutyric acid uptake inhibitor: pharmacological characterization. Eur. J. Pharmacol. 224:1992;189-198.
34. Suzdak P.D. Lipophilic GABA uptake inhibitors: biochemistry, pharmacology and therapeutic potential. Drugs of the Future. 18:1993;1129-1136.
35. Thomsen C., Sørensen P.O., Egebjerg J. 1-(3-(9H-carbazol-9-yl)-l-propyl)-4-(2-methoxyphenyl)-4-piperidinol, a novel subtype selective inhibitor of the mouse type II GABA-transporter. Br. J. Pharmacol. 120:1996;983-985.
36. Thomsen C., Dalby N.O. Roles of metabotropic glutamate receptor subtypes in modulation of pentylenetetrazol-induced seizure activity in mice. Neuropharmacology. 37:1998;1465-1473.
37. Waldmeier P.C., Stocklin K., Feldtrauer J.J. Weak effects of local and systemic administration of the GABA uptake inhibitor, SK&F 89976, on extracellular GABA in the rat striatum. Naunyn-Schmiedeberg. Archiv. Pharmacol. 345:1992;544-547.
38. Wood J.D., Sidhu H.S. A comparative study and partial characterization of multi-uptake systems for gamma-aminobutyric acid. J. Neurochem. 49:1987;1202-1208.
39. Yamauchi A., Uchida S., Kwon H.M., Preston A.S., Robey R.B., Garcia-Perez A., Burg M.B., Handler J.S. Cloning of a Na(+)- and CI(-)-dependent betaine transporter that is regulated by hypertonicity. J. Biol. Chem. 267:1992;649-652.