Portal de Periódicos da CAPES

GABA and Glutamate Receptors as Therapeutic Targets in Neurodegenerative Disorders *

1992; Wiley; Volume: 70; Issue: 2 Linguagem: Inglês

10.1111/j.1600-0773.1992.tb00436.x

1600-0773

Povl Krogsgaard‐Larsen,

Mitochondrial Function and Pathology

Pharmacology & ToxicologyVolume 70, Issue 2 p. 95-104 GABA and Glutamate Receptors as Therapeutic Targets in Neurodegenerative Disorders* Povl Krogsgaard-Larsen, Povl Krogsgaard-Larsen PharmaBiotec Research Center, Department of Organic Chemistry, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK-2100 Copenhagen Ø, DenmarkSearch for more papers by this author Povl Krogsgaard-Larsen, Povl Krogsgaard-Larsen PharmaBiotec Research Center, Department of Organic Chemistry, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK-2100 Copenhagen Ø, DenmarkSearch for more papers by this author First published: February 1992 https://doi.org/10.1111/j.1600-0773.1992.tb00436.xCitations: 16 * Presented as the Astra Award Lecture at the Joint Meeting of the British Pharmacological Society and the Nordic Pharmacological Society, September 17–20, 1991, Southampton, U. K. AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onEmailFacebookTwitterLinkedInRedditWechat References G. Biggio & E. Costa (Eds.): GABA and benzodiazepine receptor subtypes. Raven Press, New York, 1990. Google Scholar Bowen, D. M.: Treatment of Alzheimer's disease. Brit. J. Psychiat. 1990, 157, 327–330. 10.1192/bjp.157.3.327 CASPubMedWeb of Science®Google Scholar Brehm, L., F. S. Jorgensen, J. J. Hansen & P. Krogsgaard-Larsen: Agonists and antagonists for central glutamic acid receptors. Drug News Perspect. 1988, 1, 138–144. Google Scholar Brioni, J. D., M. W. Decker, L. P. Gamboa, I. Izquierdo & J. L. McGaugh: Muscimol injections in the medial septum impair spatial learning. Brain Res. 1990, 522, 227–234. 10.1016/0006-8993(90)91465-S CASPubMedWeb of Science®Google Scholar Brioni, J. D., A. H. Nagahara & J. L. McGaugh: Involvement of the amygdala GABAergic system in the modulation of memory storage. Brain Res. 1989, 487, 105–112. 10.1016/0006-8993(89)90945-1 CASPubMedWeb of Science®Google Scholar Bruno, G., N. L. Foster, P. Fedio, E. Mohr, C. Cox, M. M. Gillespie & T. N. Chase: THIP therapy of Alzheimer's disease. Neurology 1984, Suppl. 34, 225. Google Scholar Bureau, M. & R. W. Olsen: Multiple distinct subunits of the γ-aminobutyric acid-A receptor protein show different ligandbinding affinities. Mol Pharmacol. 1990, 37, 497–502. CASPubMedWeb of Science®Google Scholar Byberg, J. R., I. M. Labouta, E. Falch, H. Hjeds, P. Krogsgaard-Larsen, D. R. Curtis & B. D. Gynther: Synthesis and biological activity of a GABAA agonist which has no effect on benzodiazepine binding and structurally related glycine antagonists. Drug Des. Del. 1987, 1, 261–274. CASPubMedGoogle Scholar Christensen, I. T., A. Reinhardt, B. Nielsen, B. Ebert, U. Madsen, E. Ø. Nielsen, L. Brehm & P. Krogsgaard-Larsen: Excitatory amino acid agonists and partial agonists. Drug Des. Del. 1989, 5, 57–71. Google Scholar Coyle, J. T.: Neurotoxic action of kainic acid. J. Neurochem. 1983, 41, 1–11. 10.1111/j.1471-4159.1983.tb00899.x CASPubMedWeb of Science®Google Scholar De Amici, M., B. Frølund, H. Hjeds & P. Krogsgaard-Larsen: Analogues of the low-efficacy partial GABAA agonist 4-PIOL. Syntheses and in vitro pharmacological studies. Eur. J. Med. Chem. 1991, 26, 625–631. 10.1016/0223-5234(91)90198-V CASWeb of Science®Google Scholar Deutsch, S. I., J. Mastropaolo, B. L. Schwartz, R. B. Rosse & J. M. Morihisa: A “glutamatergic hypothesis” of schizophrenia. Rationale for pharmacotherapy with glycine. Clin. Neuropharmacol. 1989, 12, 1–13. 10.1097/00002826-198902000-00001 CASPubMedWeb of Science®Google Scholar G. DiChiara & G. L. Gessa (Eds.): GABA and the basal ganglia. Raven Press, New York, 1981. Google Scholar Falch, E., P. Jacobsen, P. Krogsgaard-Larsen & D. R. Curtis: GABA-mimetic activity and effects on diazepam binding of aminosulphonic acids structurally related to piperidine-4-sulphonic acid. J. Neurochem. 1985, 44, 68–75. 10.1111/j.1471-4159.1985.tb07114.x CASPubMedWeb of Science®Google Scholar Falch, E., O. M. Larsson, A. Schousboe & P. Krogsgaard-Larsen: GABA-A agonists and GABA uptake inhibitors: structure-activity relationships. Drug Dev. Res. 1990, 21, 169–188. 10.1002/ddr.430210304 CASWeb of Science®Google Scholar Foster, N. L., T. N. Chase, A. Denaro, T. A. Hare & C. A. Tamminga: THIP treatment and Huntington's chorea. Neurology 1983, 33, 637–639. 10.1212/WNL.33.5.637 CASPubMedWeb of Science®Google Scholar Frandsen, Aa., P. Krogsgaard-Larsen & A. Schousboe: Novel gluta-mate receptor antagonists selectively protect against kainic acid induced neurotoxicity in cultured cerebral cortex neurones. J. Neurochem. 1990, 55, 1821–1823. 10.1111/j.1471-4159.1990.tb04976.x CASPubMedWeb of Science®Google Scholar Frølund, B. F., U. Kristiansen, T. Nathan, E. Falch, J. D. C. Lambert & P. Krogsgaard-Larsen: 4-PIOL, a low-efficacy partial GA-BAA agonist. In: Drug research related to neuroactive amino acids. Eds.: A. Schousboe, N. H. Diemer & H. Kofod Munksgaard, Copenhagen, 1992 (in press). Google Scholar Greenamyre, J. T. & A. B. Young: Excitatory amino acids and Alzheimer's disease. Neurobiol. Ag. 1989, 10, 593–602. 10.1016/0197-4580(89)90143-7 CASPubMedWeb of Science®Google Scholar Hansen, J. J. & P. Krogsgaard-Larsen: Structural, conformational, and stereochemical requirements of central excitatory amino acid receptors. Med. Res. Rev. 1990, 10, 55–94. 10.1002/med.2610100103 CASPubMedWeb of Science®Google Scholar Honoré, T.: Excitatory amino acid receptor subtypes and specific antagonists. Med. Res. Rev. 1989, 9, 1–23. 10.1002/med.2610090102 CASPubMedWeb of Science®Google Scholar Honoré, T., J. Lauridsen & P. Krogsgaard-Larsen: The binding of 3H-AMPA, a structural analogue of glutamic acid, to rat brain membranes. J. Neurochem. 1982, 38, 173–178. 10.1111/j.1471-4159.1982.tb10868.x CASPubMedWeb of Science®Google Scholar Huettner, J. E.: Competitive antagonism of glycine at the N-methyl-D-aspartate (NMDA) receptor. Biochem. Pharmacol. 1991, 41, 9–16. 10.1016/0006-2952(91)90004-O CASPubMedWeb of Science®Google Scholar Jensen, M. S. & J. D. C. Lambert: Modulation of the response to the GABA-mimetics, XHIP and piperidine-4-sulphonic acid, by agents which interact with the benzodiazepine receptors. Neuropharmacology 1984, 23, 1441–1450. 10.1016/0028-3908(84)90087-X CASPubMedWeb of Science®Google Scholar Keinänen, K., W. Wisden, B. Sommer, P. Werner, A. Herb, T. A. Verdoon, B. Sakmann & P. H. Seeburg: A family of AMPA-selective glutamate receptors. Science 1990, 249, 556–560. 10.1126/science.2166337 CASPubMedWeb of Science®Google Scholar G. A. Kerkut & H. V. Wheal (Eds.) : Electrophysiology of isolated mammalian CNS preparations. London. Academic Press, New York, 1981. Google Scholar Korsgaard, S., D. E. Casey, J. Gerlach, O. Hetman, B. Kaldan & L. B. Mikkelsen: The effect of tetrahydroisoxazolopyridinol (XHIP) in tardive dyskinesia. Arch. Gen. Psychiatry 1982, 39, 1017–1021. 10.1001/archpsyc.1982.04290090021005 CASPubMedWeb of Science®Google Scholar Kristiansen, U., J. D. C. Lambert, E. Falch & P. Krogsgaard-Larsen: Electrophysiological studies of the GABAA receptor ligand, 4-PIOL, on cultured hippocampal neurones. Brit. J. Pharmacol. 1991, 104, 85–90. 10.1111/j.1476-5381.1991.tb12389.x CASPubMedWeb of Science®Google Scholar Krogsgaard-Larsen, P., L. Brehm, J. S. Johansen, P. Vinzents, J. Lauridsen & D. R. Curtis: Synthesis and structure-activity studies on excitatory amino acids structurally related to ibotenic acid. J. Med. Chem. 1985, 28, 673–679. 10.1021/jm50001a023 CASPubMedWeb of Science®Google Scholar Krogsgaard-Larsen, P., J. W. Ferkany, E. Ø. Nielsen, U. Madsen, B. Ebert, J. S. Johansen, N. H. Diemer, T. Bruhn, D. T. Beattie & D. R. Curtis: Novel class of amino acid antagonists at non-N-methyl-D-aspartic acid excitatory amino acid receptors. Synthesis, in vitro and in vivo pharmacology, and neuroprotection. J. Med. Chem. 1991, 34, 123–130. 10.1021/jm00105a019 CASPubMedWeb of Science®Google Scholar Krogsgaard-Larsen, P., H. Hjeds, E. Falch, F. S. Jørgensen & L. Nielsen: Recent advances in GABA agonists, antagonists and uptake inhibitors: structure-activity relationships and therapeutic potential. Adv. Drug Res. 1988, 17, 381–456. 10.1016/B978-0-12-013317-8.50009-5 CASGoogle Scholar Krogsgaard-Larsen, P. & T. Honoré: Glutamate receptors and new glutamate agonists. Trends Pharmacol. Sci. 1983, 4, 31–33. 10.1016/0165-6147(83)90272-9 CASWeb of Science®Google Scholar Krogsgaard-Larsen, P., T. Honoré, J. J. Hansen, D. R. Curtis & D. Lodge: New class of glutamate agonist structurally related to ibotenic acid. Nature (London) 1980, 284, 64–66. 10.1038/284064a0 CASPubMedWeb of Science®Google Scholar Krogsgaard-Larsen, P., B. Jensen, E. Falch & F. S. Jorgensen: Heterocyclic muscarinic agonists: structural and therapeutic aspects. Drugs Fut. 1989, 14, 541–561. Google Scholar Krogsgaard-Larsen, P., G. A. R. Johnston, D. Lodge & D. R. Curtis: A new class of GABA agonist. Nature (London) 1977, 268, 53–55. 10.1038/268053a0 CASPubMedWeb of Science®Google Scholar Krogsgaard-Larsen, P., E. Ø. Nielsen & D. R. Curtis: Ibotenic acid analogues. Synthesis and biological and in vitro activity of conformationally restricted agonists at excitatory amino acid receptors. J. Med. Chem. 1984, 27, 585–591. 10.1021/jm00371a005 CASPubMedWeb of Science®Google Scholar Lapchak, P. A., D. M. Araujo, R. Quirion & B. Collier: Presynaptic cholinergic mechanisms in the rat cerebellum: evidence for nicotinic, but not muscarinic autoreceptors. J. Neurochem. 1989, 53, 1843–1851. 10.1111/j.1471-4159.1989.tb09251.x CASPubMedWeb of Science®Google Scholar Lauridsen, J., T. Honoré & P. Krogsgaard-Larsen: Ibotenic acid analogues. Synthesis, molecular flexibility, and in vitro activity of agonists and antagonists at central glutamic acid receptors. J. Med. Chem. 1985, 28, 668–672. 10.1021/jm50001a022 CASPubMedWeb of Science®Google Scholar D. Lodge (Ed.): Excitatory amino acids in health and disease. John Wiley & Sons, Chichester, 1988. Google Scholar Lund, T. M., U. Madsen, B. Ebert, F. S. Jórgensen & P. Krogsgaard-Larsen: Conformational and pharmacological characterization of 4-AHCP, a bicyclic homologue of the excitatory amino acid receptor agonist AMPA. Med. Chem. Res. 1991, 1, 136–141. CASGoogle Scholar Madsen, U., J. W. Ferkany, B. E. Jones, B. Ebert, T. N. Johansen, T. Holm & P. Krogsgaard-Larsen: NMDA receptor agonists derived from ibotenic acid. Preparation, neuroexcitation and neurotoxicity. Eur. J. Pharmacol. Mol. Pharmacol. Sect. 1990, 189, 381–391. 10.1016/0922-4106(90)90035-V CASPubMedWeb of Science®Google Scholar Mathers, D. A.: The GABAA receptor: new insights from singlechannel recording. Synapse 1987, 1, 96–101. 10.1002/syn.890010113 CASPubMedWeb of Science®Google Scholar Meldrum, B. S.: Pharmacology of GABA. Clin. Neuropharmacol. 1982, 5, 293–316. 10.1097/00002826-198205030-00004 CASPubMedWeb of Science®Google Scholar B. S. Meldrum, F. Moroni, R. P. Simon & J. H. Woods, Eds.: Excitatory amino acids. Raven Press, New York, 1991. Google Scholar Monaghan, D. T., R. J. Bridges & C. W. Cotman: The excitatory amino acid receptors. Annu. Rev. Pharmacol. Toxicol. 1989, 29, 365–402. 10.1146/annurev.pa.29.040189.002053 CASPubMedWeb of Science®Google Scholar Murphy, D. E., E. W. Snowhill & M. Williams: Characterization of quisqualate recognition sites in rat brain tissue using DL-[3H]α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) and a filtration assay. Neurochem. Res. 1987, 12, 775–782. 10.1007/BF00971514 CASPubMedWeb of Science®Google Scholar G. Nappi, O. Hornykiewics, R. G. Fariello, A. Agnoli & H. Klawans (Eds.): Neurodegenerative disorders: The role played by endotoxins and xenobiotics. Raven Press, New York, 1988. Google Scholar Nathan, T., M. S. Jensen & J. D. C. Lambert: The slow inhibitory postsynaptic potential in rat hippocampal CA1 neurones is blocked by intracellular injection QX-314. Neurosci. Lett. 1990, 110, 309–313. 10.1016/0304-3940(90)90865-7 CASPubMedWeb of Science®Google Scholar Nielsen, E. Ø., A. Schousboe, S. H. Hansen & P. Krogsgaard-Larsen: Excitatory amino acids: studies on the biochemical and chemical stability of ibotenic acid and related compounds. J. Neurochem. 1985, 45, 725–731. 10.1111/j.1471-4159.1985.tb04052.x CASPubMedWeb of Science®Google Scholar Perouansky, M. & R. Grantyn: Separation of quisqualate- and kainate-selective glutamate receptors in cultured neurons from the rat superior colliculus. J. Neurosci. 1989, 9, 70–80. CASPubMedWeb of Science®Google Scholar Petersen, H. R., I. Jensen & M. Dam: XHIP: a single-blind controlled trial in patients with epilepsy. Acta neurol. scand. 1983, 67, 114–117. 10.1111/j.1600-0404.1983.tb04552.x PubMedWeb of Science®Google Scholar Rassendren, F. A., P. Lory, J. P. Pin, J. Bockaert & J. Nargeot: A specific quisqualate agonist inhibits kainate responses induced in Xenopus oocytes injected with rat brain RNA. Neurosci. Lett. 1989, 99, 333–339. 10.1016/0304-3940(89)90469-2 CASPubMedWeb of Science®Google Scholar Rothman, S. M. & J. W. Olney: Glutamate and the pathology of hypoxic/ischemic brain damage. Ann. Neurol. 1986, 19, 105–111. 10.1002/ana.410190202 CASPubMedWeb of Science®Google Scholar Schoepp, D., J. Bockaert & F. Sladeczek: Pharmacological and functional characteristics of metabotropic excitatory amino acid receptors. Trends Pharmacol. Sci. 1990, 11, 508–515. 10.1016/0165-6147(90)90052-A CASPubMedWeb of Science®Google Scholar Schoepp, D. D. & B. G. Johnson: Comparison of excitatory amino acid-stimulated phosphoinositide hydrolysis and N-[3]acetylaspartylglutamate binding in rat brain: selective inhibition of phosphoinositide hydrolysis by 2-amino-3-phosphonopropionate. J. Neurochem. 1989, 53, 273–278. 10.1111/j.1471-4159.1989.tb07324.x CASPubMedWeb of Science®Google Scholar Shinozaki, H.: Pharmacology of the glutamate receptor. Prog. Neurobiol. 1988, 30, 399–435. 10.1016/0301-0082(88)90009-3 CASPubMedWeb of Science®Google Scholar Sugiyama, H., M. Watanabe, H. Taji, Y. Yamamoto & I. Ito: Pharmacological properties of quisqualate- and kainate-preferring glutamate receptors induced in Xenopus oocytes by rat and chick brain mRNA. Neurosci. Res. 1989, 7, 164–167. 10.1016/0168-0102(89)90057-6 CASPubMedWeb of Science®Google Scholar Supavilai, P. & M. Karobath: Modulation of acetylcholine release from rat striatal slices by the GABA/benzodiazepine receptor complex. Life Sci. 1985, 36, 417–426. 10.1016/0024-3205(85)90253-X CASPubMedWeb of Science®Google Scholar Thaker, G. K., J. A. Nguyen & C. A. Tamminga: Increased saccadic distractability in tardive dyskinesia: functional evidence for subcortical GABA dysfunction. Biol. Psychiatry 1989, 25, 49–59. 10.1016/0006-3223(89)90146-7 CASPubMedWeb of Science®Google Scholar Van Ness, P. C., A. E. Watkins, M. O. Bergman, W. W. Tourtelotte & R. W. Olsen: γ-Aminobutyric acid receptors in normal human brain and Huntington's disease. Neurology 1982, 32, 63–68. 10.1212/WNL.32.1.63 CASPubMedWeb of Science®Google Scholar Venault, P., G. Chapouthier, L. Prado de Carvalho, J. Simiand, M. Morre, R. H. Dodd & J. Rossier: Benzodiazepine impairs and β-carboline enhances performance in learning and memory tasks. Nature (London) 1986, 321, 864–866. 10.1038/321864a0 CASPubMedWeb of Science®Google Scholar J. C. Watkins & G. L. Collingridge (Eds.) : The NMDA receptor. Oxford University Press, Oxford, 1989. Google Scholar Watkins, J. C., P. Krogsgaard-Larsen & T. Honoré: Structure-activity relationships in the development of excitatory amino acid receptor agonists and competitive antagonists. Trends Pharmacol. Sci. 1990, 11, 25–33. 10.1016/0165-6147(90)90038-A CASPubMedWeb of Science®Google Scholar R. J. Wurtman, S. Corkin, J. H. Growdon & E. Ritter-Walker (Eds.): Advances in neurology. Vol. 51. Alzheimer's disease. Raven Press, New York, 1990. Google Scholar Citing Literature Volume70, Issue2February 1992Pages 95-104 ReferencesRelatedInformation