Summary
GABA receptor agonists, e.g. progabide, modify the activity of several brain neuronal systems which are implicated in the pathogenesis of some neuropsychiatric disorders. Thus, alterations in noradrenergic and serotoninergic transmissions induced by progabide may be a mechanism involved in the antidepressant action of this drug in the clinic. The antagonism of the neuroleptic-induced increase in dopamine receptor sensitivity and the decrease in dopamine synthesis and release may be responsible for the effectiveness of the GABA receptor agonists in the treatment of neuroleptic- and L-DOPA-induced dyskinesia. This action of GABA receptor agonists also suggests their therapeutic potential in mania. Finally, decrease in cellular excitability induced by GABA receptor agonists, e.g. progabide, accounts for their efficacy in epilepsy.
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References
Banerjee, S. P., Kung; L. S., Riggi, S.J., Chanda, S. K.: Development of beta-adrenergic receptor subsensitivity by antidepressants. Nature 268, 455–456 (1977).
Bartholini, G., Lloyd, K. G., Worms, P., Constantinidis,J., Tissot, R.: GABA and GABA-ergic medication: Relation to striatal dopamine function and parkinsonism. In: Advances in Neurology, Vol. 24: The Extrapyramidal System and Its Disorders (Poirier, L.J., Sourkes, T. L., Bédard, P.J., eds.), pp. 253–257. New York: Raven Press. 1979 a.
Bartholini, G., Scatton, B., Zivkovic, B., Lloyd, K. G.: On the mode of action of SL 76 002, a new GABA receptor agonist. In: GABA-Neurotransmitters (Krogsgaard-Larsen, P., Scheel-Kruger, J., Kofod, H., eds.), pp. 326–339. Copenhagen: Munksgaard. 1979 b.
Baruzzi, A., Pazzaglia, P., Loiseau, P., Cenraud, B., Zarifian, E., Mitchard, M., Morselli, P. L.: Preliminary observations on the effects of SL 76 002, a new GABA agonist in the epileptic patient. In: Advances in Epileptology. The Xth Epilepsy International Symposium (Wada, J. A., Penry, J. K., eds.), p. 356. New York: Raven Press. 1980.
Brunello, N., Chuang, D. M., Costa, E.: Use of specific brain lesions to study the site of action of antidepressants. In: New Vistas in Depression (Langer, S.Z., Takahashi, R., Segawa, T, Briley, M., eds.), pp. 141–145. Oxford: Pergamon Press. 1982.
De Montigny, C., Aghajanian, G. K.: Tricyclic antidepressants: Long-term treatment increases responsivity of rat forebrain neurons to serotonin. Science 202, 1303–1306 (1978).
Emrich, H. M., Altmann, H., v. Zerssen, D.: Prophylactic action of sodiumvalproate in manic depression: The GABA-hypothesis of affective disorders. In: New Vistas in Depression (Langer, S.Z., Takahashi, R., Segawa, T, Briley, M., eds.), pp. 81–85. Oxford: Pergamon Press. 1982.
Guyenet, P. G., Aghajanian, G. K.: ACh, substance P and met-enkephalin in the locus coeruleus: pharmacological evidence for independent sites of action. Eur. J. Pharmacol. 53, 319–328 (1979).
Kaplan, J. P., Raizon, B. M., Desarmenien, M., Feltz, P., Headley, P. M., Worms, P., Lloyd, K. G., Bartholini, G.: New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide. J. Med. Chem. 23, 702–704 (1981).
Lloyd, K. G., Worms, P., Depoortere, H., Bartholini, G.: Pharmacological profile of SL 76 002, a new GABA-mimetic drug. In: GABA-Neurotransmitters (Krogsgaard-Larsen, P., Scheel-Kruger, J., Kofod, H., eds.), pp. 308–325. Copenhagen: Munksgaard. 1979.
Lloyd, K. G., Worms, P.: Sustained gamma-aminobutyric acid receptor stimulation and chronic neuroleptic effects. In: Long Term Effects of Neuroleptics (Cattabeni, F., Racagni, G., Spano, P. F., Costa, E., eds.), pp. 253–258. New York: Raven Press. 1980.
Lloyd, K. G., Arbilla, S., Beaumont, K., Briley, M., De Montis, G., Scatton, B., Langer, S. Z., Bartholini, G.: Gamma-aminobutyric acid (GABA) receptor stimulation. II. Specificity of progabide (SL 76 002) and SL 75 102 for the GABA receptor. J. Pharmacol. Exp. Ther. 220, 672–677 (1982).
Lloyd, K. G., Garrigou, D., Broekkamp, C. L. E.: The action of monoaminergic, cholinergic and GABA-ergic compounds in the olfactory bulbectomized rat model of depression. In: New Vistas in Depression (Langer, S.Z., Takahashi, R., Segawa, T., Briley, M., eds.), pp. 179–186. Oxford: Pergamon Press. 1982.
Loiseau, P., Cernaud, B., Bossi, L., Morselli, P. M.: A double-blind controlled study versus placebo with progabide (SL 76 002) in severe epilepsy. In: Advances in Epileptology. The XIIth Epilepsy International Symposium (Dam, M., Gram, L., Pnry, J. K., eds.), pp. 135–139. New York: Raven Press. 1981.
Löscher, W.: Comparative assay of anticonvulsant and toxic potencies of sixteen GABA-mimetic drugs. Neuropharmacology 21, 803–810 (1982).
Meldrum, B. S.: Epilepsy and gamma-aminobutyric acid mediated inhibition. Int. Rev. Neurobiol. 17, 1–36 (1975).
Morselli, P. L., Bossi, L., Henry, J. F., Zarifian, E., Bartholini, G.: On the therapeutic action of SL 76 002, a new GABA-mimetic agent: preliminary observations in neuropsychiatric disorders. Brain Res. Bull. 5, Suppl. 2, 411–414 (1980).
Morselli, P. L., Henry, J. F., Macher, J. P., Botti, P., Huber, J. P., Van Landeghem, V. H.: Progabide and mood. In: Biological Psychiatry (Perris, C., Struwe, G.,Jansson, B., eds.), pp. 440–443. Amsterdam: Elsevier/North-Holland, Biomedical Press. 1981.
Naik, S. R., Guidotti, A., Costa, E.: Central GABA receptor agonists: Comparison of muscimol and baclofen. Neuropharmacology 15, 479–484 (1976).
Peroutka, S.J., Snyder, S.H.: Long-term antidepressant treatment lowers spiroperidol-labelled serotonin receptors. Science 210, 88–90 (1980).
Pert, A., Rosenblatt, J. E., Sivit, C., Pert, C. B., Bunney, W. E., jr.: Long-term treatment with lithium prevents the development of dopamine receptor supersensitivity. Science 201, 171–173 (1978).
Scatton, B., Bartholini, G.: Modulation by GABA of cholinergic transmission in the striatum. Brain Res. 183, 211–216 (1980).
Scatton, B., Zivkovic, B., Dedek, J., Lloyd, K. G., Constantinidis, J., Tissot, R., Bartholini, G.: Gamma-aminobutyric acid (GABA) receptor stimulation. III. Effect of progabide (SL 76 002) on norepinephrine, dopamine and 5-hydroxytryptamine turnover in rat brain areas. J. Pharmacol. Exp. Ther. 220, 678–688 (1982).
Schildkraut, J.J.: The catecholamine hypothesis of affective disorders: a review of supporting evidence. Am. J. Psychiat. 122, 509–522 (1965).
Schildkraut,J.J., Roffman, M., Orsulak, P., Schatzberg, A., Kling, M., Reigle, Th.: Effects of short- and long-term administration of tricyclic antidepressants and lithium on norepinephrine turnover in brain. Pharmakopsychiat. Neuropsychopharmakol. 9, 193–202 (1976).
Sevestre, P., Rondot, P., Bathien, N., Morselli, P. L., Van Landeghem, V. H.: The effect of progabide, a specific GABA-agonist, on neuroleptic-induced tardive dyskinesia. Results of a pilot study. Abstracts, Vol. 2, 13th C.I.N.P. Congress, Jerusalem, Israel, June 20–25, p. 663. 1982.
Tamminga, C.A., Crayton, J. W, Chase, T.N.: Improvement in tardive dyskinesia after muscimol therapy. Arch. Gen. Psychiat. 36, 595–598 (1979).
Tapia, R.: The role of gamma-aminobutyric acid metabolism in the regulation of cerebral excitability. In: Neurohumoral Coding of Brain Function (Myers, R. D., Drucker-Colin, R.R., eds.), pp. 3–26. New York: Plenum Press. 1974.
Tower, D. B.: GABA and seizures: clinical correlates in man. In: GABA in Nervous System Function (Roberts, E., Chase, T. N., Tower, D. B., eds.), pp. 461–478. New York: Raven Press. 1976.
Van der Linden, G.J., Meinardi, H., Meyer, J. W. A., Bossi, L., Gomeni, C.: A double-blind cross-over trial with progabide (SL 76 002) against placebo in patients with secondary generalized epilepsy. In: Advances in Epileptology. The XIIth Epilepsy International Symposium (Dam, M., Gram, L., Pertly, J. K., eds.), pp. 141–144. New York: Raven Press. 1981.
Worms, P., Willi gens, M. T, Lloyd, K. G.: GABA involvement in neuroleptic-induced catalepsy. J. Pharm. Pharmacol. 30, 716–718 (1978).
Worms, P., Depoortere, H., Durand, A., Morselli, P. L., Lloyd, K. G., Bartholini, G.: Gamma-aminobutyric acid (GABA) receptor stimulation. I. Neuropharmacological profiles of progabide (SL 76 002) and SL 75102, with emphasis on their anticonvulsant spectra. J. Pharmacol. Exp. Ther. 220, 660–671 (1982).
Zivkovic, B., Scatton, B., Dedek, J., Bartholini, G.: GABA influence on noradrenergic and serotonergic transmissions: implications in mood regulation. In: New Vistas in Depression (Langer, S. Z., Takahashi, R., Segawa, T, Briley, M., eds.), pp. 195–201. Oxford: Pergamon Press. 1982.
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Zivkovic, B., Scatton, B., Worms, P., Lloyd, K.G., Bartholini, G. (1983). Pharmacological and Therapeutic Actions of GABA Receptor Agonists. In: Goldstein, M., Jellinger, K., Riederer, P. (eds) Basic Aspects of Receptor Biochemistry. Journal of Neural Transmission, vol 18. Springer, Vienna. https://doi.org/10.1007/978-3-7091-4408-4_31
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DOI: https://doi.org/10.1007/978-3-7091-4408-4_31
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