Abstract
Several lines of evidence have well established that the cage convulsant t-butylbicyclophosphorothionate (TBPS) inhibits the function of the central GABAergic transmission by binding to specific recognition sites present at the level of the chloride ionophore coupled to the GABAA/benzodiazepine receptor complex (Squires et al., 1983; Van Renterghem et al., 1987). This finding has given a rather unique tool to study biochemically the function of the GABA-dependent chloride channel. In fact, the specific binding of 35S-TBPS to the recognition sites associated to the GABAA receptor complex is modulated in an opposite manner by different compounds which specifically enhance (GABA agonists, benzodiazepines, imidazopyridines, anxiolytic and anticonvulsant ß-carbolines etc.) and inhibit (GABA antagonists, anxiogenic and convulsant ß-carbolines etc.) the function of the GABA-dependent chloride channel, respectively (Squires et al., 1983; Gee et al., 1986; Concas et al., 1988; Biggio et al., 1989; Serra et al., 1989; Sanna et al., 1990).
This is a preview of subscription content, log in via an institution to check access.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
References
Allan, A.M., Huidobro-Toro, J.P., Bleck, V. and Harris, R.A., 1987, Alcohol and the GABA receptor-chloride channel complex of brain, Alcohol, 1: 643–646.
Barnard, E.A., and Seeburg, P.H., 1988, Structural basis of the GABA-activated chloride channel: molecular biology and molecular electrophysiology, in: “Chloride Channel and Their Modulation by Neurotransmitters and Drugs”, G. Biggio and E. Costa, eds., Raven Press, New York, 1–18.
Biggio, G., Brodie, B.B., Guidotti, A. and Costa, E., 1977, Mechanism by which diazepam, muscimol and other drugs change the content of cyclic GMP in cerebellar cortex, Proc. Natl. Acad. Sci. U.S.A., 74: 3592–3595.
Biggio, G., Concas, A., Corda, M.G. and Serra, M., 1989, Enhancement of GABAergic transmission by Zolpidem, an imi-dazopyridine with preferential affinity for Type I benzodiazepine receptors, Eur. J. Pharmacol., 161: 173–180.
Biggio, G., Corda, M.G., Concas, A. and Gessa, G.L., 1981, Denervation supersensitivity for benzodiazepine recep tors in the rat substantia nigra, Brain Res., 220: 344–349.
Bonetti, E.P., Burkard, W.P., Galb, M. and Mohler, H., 1985, The partial inverse benzodiazepine agonist Ro 15–4513 antagonizes acute ethanol effects in mice and rats, Br. J. Pharmacol., 86: 463p.
Bormann, J., Hamill, O.P. and Sakmann, B., 1987, Mechanism of anion permeation through channels gated by glycine and ϒ-aminobutyric acid in mouse cultured spinal neurons, J. Physiol., 385: 243–286.
Bormann, J., 1988, Electrophysiology of GABAA and GABAB receptor subtypes, TINS, 11: 112–116.
Burt, D.R., Creese, I. and Snyder, S.H., 1977, Antischizophre-nic drugs: chronic treatment elevates dopamine receptor binding in brain, Science, 196: 326–328.
Concas, A., Serra, M., Atsoggiu, T. and Biggio, G., 1988, Foot-shock stress and anxiogenic ß-carbolines increase [35S]t-butylbicyclophosphorothionate binding in the rat cerebral cortex, an effect opposite to anxiolytics and ϒ-aminobutyric acid mimetics, J. Neurochem., 51: 1868–1876.
Corda, M.G., Costa, E. and Guidotti, A., 1983, Involvement of GABA in the facilitation of punishment-suppressed behaviour induced by ß-carbolines in rat, in: “Benzodiazepine Recognition Site Ligands: Biochemistry and Pharmacology”, G. Biggio and E. Costa, eds., Raven Press, New York, 121–128.
Gallager, D.W., 1978, Benzodiazepines: potentiation of a GABA inhibitory response in the dorsal raphe nucleus, Eur. J. Pharmacol.. 49: 133–143.
Gee, K.W., Lawrence, L.J. and Yamamura, H.I., 1986, Modulation of the chloride ionophore by benzodiazepine receptor ligands: influence of ϒ-aminobutyric acid and ligand efficacy, Mol. Pharmacol., 30: 218–225.
Godyn, Y., Heiner, L., Mark, J. and Mandel, P., 1969, Effect of d-n-propylacetate, an anticonvulsant compound on GABA metabolism, J. Neurochem., 16: 869–873.
Guidotti, A., Gale, K., Suria, A. and Toffano, G., 1979, Biochemical evidence for two classes of GABA receptors in rat brain, Brain Research, 172: 566–571.
Haefely, W., Kyburz, E., Gerecke, M. and Mohler, H., 1985, Recent advances in the molecular pharmacology of benzodiazepine receptors and in the structure-activity relationships of their agonists and antagonists, Adv. Drug Res., 14: 165–322.
Horton, W.R., 1980, GABA and seizures induced by inhibitors of glutamic acid decarboxylase, Brain Res. Bull., 5: 605–608.
Horton, W.R., Chapman, A.G. and Meldrum, B.S., 1979, Isoniazid, as a glutamic acid decarboxylase inhibitor, J. Neurochem., 33: 745–750.
Liljequist, S. and Engel, J., 1982, Effects of diazepam and ethanol on punished responding of rats in a conflict test situation, Acta Pharmacol. Toxicol., Suppl. 1, 51: 5.
Mereu, G. and Gessa, G.L., 1985, Low doses of ethanol inhibit the firing of neurons in the substantia nigra pars reticulata: a GABAergic effect?, Brain Res., 360: 325–330.
Mereu, G., Passino, N., Carcangiu, G.P., Boi, V. and Gessa, G.L., 1987, Electrophysiological evidence that Ro 15–4513 is a benzodiazepine receptor inverse agonist, Euro pean J. Pharmacol., 135: 453–454.
Nestoros, J.N.., 1980, Ethanol specifically potentiates GABA-mediated neurotransmission in feline cerebral cortex, Science, 209: 708–710.
Polc, P. and Haefely, W., 1976, Effects of two benzodiazepines, phenobarbitone, and baclofen on synaptic transmission in the cat cuneate nucleus, Naunyn-Schmiedebergs Arch. Pharmacol., 294: 121–131.
Porceddu, M.L., Ongini, E. and Biggio, G., 1985, 3H-SCH 23390 binding sites increase after chronic blockade of D-l dopamine receptors, Eur. J. Pharmacol., 118: 367–370.
Pritchett, D.B., Luddens, H. and Seeburg, P.H., 1989, Type I and Type II GABAA-benzodiazepine receptors produced in transfected cells, Science. 245: 1389–1392.
Sanna, E., Concas, A., Serra, M. and Biggio, G., 1990, In vivo administration of ethanol enhances the function of the ϒ-aminobutyric acid-dependent chloride channel in the rat cerebral cortex, J. Neurochem., 54: 696–698.
Sanna, E., Serra, M., Pepitoni, S. and Biggio, G., 1989, Dramatic increase in nigral t-[35S]butylbicyclophosphoro-thionate binding sites elicited by the degeneration of the striato-nigral GABAergic pathway: reversal by diazepam, Brain Res., 501: 144–149.
Serra, M., Sanna, E. and Biggio, G., 1989, Isoniazid, an in hibitor of GABAergic transmission, enhances [35S]TBPS binding in rat cerebral cortex, Eur. J. Pharmacol., 164: 385–388.
Shivers, B.D., Killisch, I., Sprengel, R., Sontheimer, H., Kohler, M., Schofield, P.R. and Seeburg, P.H., 1989, Two novel GABAA receptor subunits exist in distinct neuronal subpopulations, Neuron., 3: 327–337.
Squires, R.F., Casida, J.E., Richardson, M. and Saederup, E., 1983, 35S-t-butylbicyclophosphorothionate binds with high affinity to brain-specific sites coupled to . -aminobutyric acid-A and ion recognition sites, Mol. Pharmacol., 23: 326–336.
Suzdak, P.D., Schwartz, R.D., Skolnick, P. and Paul, S.M., 1986a, Ethanol stimulates ϒ-aminobutyric acid receptor-mediated chloride transport in rat brain synaptoneurosomes, Proc. Natl. Acad. Sci. U.S.A., 83: 4071–4075.
Suzdak, P.D., Glowa, J.R., Crawley, J.N., Schwartz, R.D., Skolnick, P. and Paul, S.M., 1986b, A selective imidazo-benzodiazepine antagonist of ethanol in the rat, Science, 234: 1243–1247.
Trullas, R., Havoundjian, H. and Skolnick, P., 1987, Stress-induced change in t-[35S]butylbicyclophosphorothionate binding to ϒ-aminobutyric acid-gated chloride channels are mimicked by in vitro occupation of benzodiazepine receptors, J. Neurochem., 49: 968–974.
Van Renterghem, C., Bilbe, G., Moss, S., Smart, T.G., Constanti, A., Brown, D.A. and Barnard, E.A., 1987, GABA receptors induced in xenopus oocytes by chick brain mRNA: evaluatation of TBPS as a use-dependent channel blocker, Mol. Brain Res., 2: 21–31.
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 1991 Plenum Press, New York
About this chapter
Cite this chapter
Biggio, G., Sanna, E., Serra, M., Serra, G.P., Concas, A. (1991). “In Vivo” Inhibition of GABAergic Transmission Increases 35S-TBPS Binding in the Rat Brain. In: Kito, S., Segawa, T., Olsen, R.W. (eds) Neuroreceptor Mechanisms in Brain. Advances in Experimental Medicine and Biology, vol 287. Springer, Boston, MA. https://doi.org/10.1007/978-1-4684-5907-4_34
Download citation
DOI: https://doi.org/10.1007/978-1-4684-5907-4_34
Publisher Name: Springer, Boston, MA
Print ISBN: 978-1-4684-5909-8
Online ISBN: 978-1-4684-5907-4
eBook Packages: Springer Book Archive