Substrate inhibitors and blockers of excitatory amino acid transporters in the treatment of neurodegeneration: Critical considerations

European Journal of Pharmacology

Volumn 479, Issue 1-3, 2003, Pages 291-296

  Mennini, Tiziana ^a   Fumagalli, Elena ^a   Gobbi, Marco ^a   Fattorusso, Caterina ^b   Catalanotti, Bruno ^b   Campiani, Giuseppe ^b  

^a MARIO NEGRI INSTITUTE FOR PHARMACOLOGICAL RESEARCH   (Italy)

^b UNIVERSITY OF SIENA   (Italy)

Author keywords

Glutamate transporter; Glutamate uptake; Inhibitor; Neurodegeneration; Substrate

Indexed keywords

1 AMINOCYCLOBUTANECARBOXYLIC ACID; 2 (2 CARBOXYCYCLOPROPYL)GLYCINE; 2 AMINO 3 (4' HYDROXYCARBONYLOXAZOLIN 2 YL)PROPIONIC ACID; 2 AMINO 4 (4' HYDROXYCARBONYLOXAZOL 2 YL)BUTYRIC ACID; 2 AMINO 4 (4' HYDROXYCARBONYLOXAZOLIN 2 YL)BUTYRIC ACID; 2 PHENYLOXAZOLE 4,5 DICARBOXYLIC ACID; 2 PHENYLOXAZOLINE 4,5 DICARBOXYLIC ACID; 2,4 METHANOPYRROLIDINE 2,4 DICARBOXYLATE; 2,4 PYRROLIDINEDICARBOXYLIC ACID; 3 HYDROXYASPARTIC ACID; 4 HYDROXYGLUTAMIC ACID; ASPARTIC ACID DERIVATIVE; DEXTRO BENZOYLOXYASPARTIC ACID; DIHYDROKAINIC ACID; EXCITATORY AMINO ACID TRANSPORTER; GLUTAMIC ACID DERIVATIVE; KAINIC ACID; LEVO 3,4 METHANOPYRROLIDINE DICARBOXYLATE; LEVO PYRROLIDINE 2,3 CARBOXYLIC ACID; THREO BETA BENZYLOXYASPARTIC ACID; UNCLASSIFIED DRUG;

BRAIN; DEGENERATIVE DISEASE; DRUG ACTIVITY; DRUG CONFORMATION; DRUG DESIGN; DRUG PROTEIN BINDING; NERVE ENDING; NONHUMAN; PHARMACOPHORE; PRIORITY JOURNAL; PROTON TRANSPORT; REVIEW; THEORETICAL MODEL;

EID: 0242469236     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2003.08.078     Document Type: Article

References (28)

1. Arriza J.L., Eliasof S., Kavanaugh M.P., Amara S.G. Excitatory amino acid transporter 5, a retinal glutamate transporter coupled to a chloride conductance. Proc. Natl. Acad. Sci. U. S. A. 94:1997;4155-4160.
2. Attwell D., Barbour B., Szatkowski M. Nonvesicular release of neurotransmitter. Neuron. 11:1993;401-407.
3. Bridges R.J., Kavanaugh M.P., Chamberlin A.R. A pharmacological review of competitive inhibitors and substrates of high-affinity, sodium-dependent glutamate transport in the central nervous system. Curr. Pharm. Des. 5:1999;363-379.
4. Campiani G., De Angelis M., Armaroli S., Fattorusso C., Catalanotti B., Ramunno A., Nacci V., Novellino E., Grewer C., Ionescu D., Rauen T., Griffiths R., Sinclair C., Fumagalli E., Mennini T. A rational approach to the design of selective substrates and potent nontransportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3). New glutamate and aspartate analogues as potential neuroprotective agents. J. Med. Chem. 44:2001;2507-2510.
5. Campiani G., Fattorusso C., De Angelis M., Catalanotti B., Butini S., Fattorusso R., Fiorni I., Nacci V., Novellino E. Neuronal high-affinity sodium-dependent glutamate transporters (EAATs): targets for the development of novel therapeutics against neurodegenerative diseases. Curr. Pharm. Des. 9:2003;599-925.
6. Chen W., Aoki C., Mahadomrongkul V., Gruber C.E., Wang G.J., Blitzblau R., Irwin N., Rosenberg P.A. Expression of a variant form of the glutamate transporter GLT1 in neuronal cultures and in neuron and astrocytes in the rat brain. J. Neurosci. 22:2002;2142-2152.
7. Danbolt N.C. Glutamate uptake. Prog. Neurobiol. 65:2001;1-105.
8. Daniels K.K., Vicroy T.W. Simultaneous isolation of glial and neuronal fractions from rat brain homogenates: comparison of high-affinity L-glutamate transport properties. Neurochem. Res. 23:1998;103-113.
9. Fonnum F., Storm-Mathisen J., Divac I. Biochemical evidence for glutamate as neurotransmitter in corticostriatal and corticothalamic fibres in rat brain. Neuroscience. 6:1981;863-873.
10. Gegelashvili G., Schousboe A. High affinity glutamate transporters: regulation of expression and activity. Mol. Pharmacol. 52:1997;6-15.
11. Gundersen V., Danbolt N.C., Ottersen O.P., Storm-Mathisen J. Demonstration of glutamate/aspartate uptake activity in nerve endings by use of antibodies recognizing exogenous D-aspartate. Neuroscience. 57:1993;97-111.
12. Gundersen V., Ottersen O.P., Storm-Mathisen J. Selective excitatory amino acid uptake in glutamatergic nerve terminals and in glia in the rat striatum: quantitative electron microscopic immunocytochemistry of exogenous D-aspartate and endogenous glutamate and GABA. Eur. J. Neurosci. 8:1996;758-765.
13. Kanner B.I., Borre L. The dual-function glutamate transporters: structure and molecular characterisation of the substrate-binding sites. Biochim. Biophys. Acta. 1555:2002;92-95.
14. 3H]L-aspartate binding to L-glutamate transporters in rat brain: structure-activity studies using L-trans-pyrrolidine-2,4-dicarboxylate (L-t-PDC) and 2-(carboxycyclopropyl)- glycine (CCG). Neurochem. Int. 36:2000;319-327.
15. Lucas D.R., Newhouse J.P. The toxic effect of sodium L-glutamate on the inner layer of the retina. Arch. Ophtalmol. 58:1957;193-201.
16. Maragakis N.J., Rothstein J.D. Glutamate transporters in neurologic disease. Arch. Neurol. 58:2001;365-370.
17. Nakamura Y., Iga K., Shibata T., Shudo M., Kataoka K. Glial plasmalemmal vesicles: a subcellular fraction from rat hippocampal homogenate distinct from synaptosomes. Glia. 9:1993;48-56.
18. Ogata T., Nakamura Y., Shibata T., Kataoka K. Release of excitatory amino acids from cultured hippocampal astrocytes induced by a hypoxic-hypoglycemic stimulation. J. Neurochem. 58:1992;1957-1959.
19. Phillis J.W., Ren J., O'Regan M.H. Transporter reversal as a mechanism of glutamate release from the ischemic rat cerebral cortex: studies with DL-threo-β-benzyloxyaspartate. Brain Res. 868:2000;105-112.
20. Roettger V.R., Amara S.G. GABA and glutamate transporters: therapeutic and etiologic implications for epilepsy. Adv. Neurol. 79:1999;551-560.
21. Rossi D.J., Oshima T., Attwell D. Glutamate release in severe brain ischaemia is mainly by reversed uptake. Nature. 403:2000;316-321.
22. Rothstein J.D., Martin L.J., Kuncl R.W. Decreased glutamate transport by the brain and spinal cord in amyotrophic lateral sclerosis. N. Engl. J. Med. 326:1992;1464-1468.
23. Seki Y., Feustel P.J., Keller R.W. Jr., Tranmer B.J., Kimelberg H.K. Inhibition of ischemia-induced glutamate release in rat striatum by dihydrokainate and an anion channel blocker. Stroke. 30:1999;433-440.
24. Sonnewald U., Qu H., Aschner M. Pharmacology and toxicology of astrocyte-neuron glutamate transport and cycling. J. Pharmacol. Exp. Ther. 301:2002;1-6.
25. Suchak S.K., Baloyianni N.V., Perkinton M.S., Williams R.J., Meldrum B.S., Rattray M. The 'glial' glutamate transporter, EAAT2 (Glt-1) accounts for high affinity glutamate uptake into adult rodent nerve endings. J. Neurochem. 84:2003;522-532.
26. Tanaka K., Watase K., Manabe T., Yamada K., Watanabe M., Takahashi K., Iwama H., Nishikawa T., Ichihara N., Hori S., Takimoto M., Wada K. Epilepsy and exacerbation of brain injury in mice lacking the glutamate transporter GLT-1. Science. 276:1997;1699-1702.
27. Taxt T., Storm-Mathisen J. Uptake of D-aspartate and L-glutamate in excitatory axon terminals in hippocampus: autoradiographic and biochemical comparison with gamma-aminobutyrate and other amino acids in normal rats and in rats with lesions. Neuroscience. 11:1984;79-100.
28. Wang G.J., Chung J.C., Schnuer J., Pratt K., Zable A.C., Kavanaugh M.P., Rosenberg P.A. High affinity glutamate transport in rat cortical neurons in culture. Mol. Pharmacol. 53:1998;88-96.