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Part of the book series: NATO ASI Series ((NSSA,volume 72))

Abstract

Early work aimed at examining the properties of chemical transmission focused on presynaptic events such as neurotransmitter synthesis, degradation, accumulation and release. In contrast, because of technical limitations, less information was obtained in regard to the biochemical events associated with neurotransmitter receptors. This situation has changed dramatically in the recent years due to the development of techniques which make possible the identification and characterization of these sites. One of the more powerful methods for this purpose has been the radioligand binding assay (Yamamura et al, 1978). With this procedure it is possible to label selectively that portion of the synaptic membrane to which the neurotransmitter must attach in order to alter cellular activity. Because of its simplicity and power, the radioligand binding assay has become one of the more popular tools in neurobiological research. Using this procedure it is possible to study receptor site number, kinetic characteristics, pharmacological properties, and their relationship to other membrane components. Moreover, binding assays have been useful in examining the effects of drugs and disease on neurotransmitter receptors, and the procedure has been adapted for use as a simple and sensitive analytical method for measuring the concentration of neurotransmitters and drugs.

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References

  • Bennett, J. P. 1978, Methods in binding studies, in “Neurotransmitter Receptor Binding”, H. I. Yamamura, S. J. Enna and M. J. Kuhar, Raven Press, New York.

    Google Scholar 

  • Bennett, J.P. Enna, S.J. Bylund, D.B. Gillin, J. C. Wyatt, R. J. and Snyder, S. H. 1979, Neurotransmitter receptors in schizophrenic frontal cortex. Arch. Gen. Psychiat, 36:927.

    Google Scholar 

  • Bennett, J. P. and Snyder, S. H. 1975, Stereospecific binding of d-lysergic acid diethylamide (LSD) to brain membranes: relationship to serotonin receptors. Brain Res, 94: 523.

    CAS  Google Scholar 

  • Bennett, J. P. and Snyder, S. H. 1976, Serotonin and lysergic acid diethylamide binding in rat brain membranes: relationship to serotonin receptors. Mol. Pharmacol, 12: 373.

    Google Scholar 

  • Burt, D. R. 1978, Criteria for receptor identification, in “Neurotransmitter Receptor Binding”, H. I. Yamamura, S. J. Enna, and M. J. Kuhar, Raven Press, New York.

    Google Scholar 

  • Bylund, D. B. 1980, “Receptor Binding Techniques”, Society for Neuroscience, Bethesda, Maryland.

    Google Scholar 

  • Burt, D. R. Creese, I. and Snyder, S. H. 1977, Antischizophrenic drugs: chronic treatment elevates dopamine receptor binding in brain. Science 196: 326.

    CAS  Google Scholar 

  • Chang, R. and Snyder, S. H. 1978, Benzodiazepine receptors: labeling in intact animals with 3H-flunitrazepam. Eur. J. Pharmacol, 48:213.

    Google Scholar 

  • Costa, E. and Guidotti, A. 1979, Molecular mechanisms in the receptor action of benzodiazepines. Ann. Rev. Pharmacol. Toxicol, 19:531.

    Google Scholar 

  • Creese, I. 1978, Receptor binding as a primary drug screening device, in “Neurotransmitter Receptor Binding”, H. I. Yamamura, S. J. Enna and M. J. Kuhar, Raven Press, New York.

    Google Scholar 

  • Simantov, R. Childers, S. and Snyder, S. H,, 1977, Opioid peptides: differentiation by radioimmunoassay and radioreceptor assay, Brain Res, 135: 358.

    CAS  Google Scholar 

  • Sulser, F. and Vetulani, J. 1977, The functional post-synaptic norepinephrine receptor system and its modification by drugs which either alleviate or precipitate depression, in “Models in Psychiatry and Neurology”, E. Usdin and I. Hanin, eds. Pergamon Press, New York.

    Google Scholar 

  • Wastek, G. J. Stern, L. Z. Johnson, P. C. and Yamamura, H. I. 1976, Huntington’s disease: regional alterations in muscarinic cholinergic receptor binding in human brain. Life Sci. 19: 1033.

    Google Scholar 

  • Yamamura, H. I. Enna, S. J. and Kuhar, M. J. 1978, Neurotransmitter Receptor Binding“, Raven Press, New York.

    Google Scholar 

  • Creese, I. Schneider, R. and Snyder, S. H. 1977, 3H-Spiroperidol labels dopamine receptors in pituitary and brain. Eur. J. Pharmacol, 46:377.

    Google Scholar 

  • Cuatrecasas, P. and Hollenberg, M. D. 1975, Binding of insulin and other hormones to non-receptor materials: saturability, specificity and apparent “negative cooperativity”. Biochem, Biophys. Res. Comm, 62:31.

    Google Scholar 

  • Enna, S. J. 1982, Radioreceptor assays for neurotransmitters and drugs, in “Handbook of Psychopharmacology”, Vol. 15, L. L. Iversen, S. D. Iversen and S. H. Snyder, Plenum Press, New York.

    Google Scholar 

  • Enna, S. J. 1983a, Principles of receptor binding assays: the GABA receptor, in “Membrane-Located Receptors for Drugs and Endogenous Agents”, A. Reid, G. M. Cook and D. J. Morre, Plenum Press, New York.

    Google Scholar 

  • Enna, S. J. 1983b, Receptor regulation in, “Handbook of, Neurochemistry”, Vol. 6, A. Lajtha, ed. Plenum Press, New York

    Google Scholar 

  • Enna, S. J. Bird, E. D. Bennett, J. P. Bylund, D. B. Yamamura, H. I. Iversen, L. L. and Snyder, S. H. 1976, Huntington’s chorea: changes in neurotransmitter receptors in the brain. N. Engl. J. Med, 294:1305.

    Google Scholar 

  • Enna, S. J. and Kendall, D. A. 1981, Interaction of antidepressants with brain neurotransmitter receptors. J. Clin. Psychopharmacol, 1:12S.

    Google Scholar 

  • Enna, S. J. and Snyder, S. H. 1975, Properties of ‘y-aminobutyric acid (GABA) receptor binding in rat brain synaptic membrane fractions, Brain Res, 100: 81.

    CAS  Google Scholar 

  • Enna, S. J. and Snyder, S. H. 1977, Influences of ions, enzymes, and detergents on GABA receptor binding in synaptic membranes of rat brain. Mol. Pharmacol, 13:442.

    Google Scholar 

  • Enna, S. J. Wood, J. H. and Snyder, S. H. 1977, Y Aminobutyric acid (GAGA) in human cerebrospinal fluid: radioreceptor assay. J. Neurochem, 28:1121.

    Google Scholar 

  • Ferkany, J. W. and Enna, S. J. 1982, Radioreceptor assays, in “Analysis of Biogenic Amines”, G. B. Baker and R. T. Couts, Elsevier/North Holland, New York.

    Google Scholar 

  • Freedberg, K. A. Innis, R. B. Creese, I. and Snyder, S. H. 1979, Antischizophrenic drugs: differential plasma protein binding and therapeutic activity. Life Sci, 24: 2467.

    Google Scholar 

  • Gavish, M. Chang, R. S. and Snyder, S. H. 1979, Solubilization of histamine H-1, GABA and benzodiazepine receptors. Life Sci. 25: 783.

    Article  PubMed  CAS  Google Scholar 

  • Hill, A. W. 1910, The possible effects of the aggregation of the molecules of hemoglobin on its dissociation curves. J. Physiol, 40:iv.

    Google Scholar 

  • Hollenberg, M. D. 1978, Receptor models and the action of neurotransmitters and hormones, in “Neurotransmitter Receptor Binding”, H. I. Yamamura, S. J. Enna and M. J. Kuhar, Raven Press, New York.

    Google Scholar 

  • Kendall, D. A. Slopis, J. Duman, R. Stancel, G. M. and Enna, S. J. 1982, The influence of hormones on drug-induced modifications in neurotransmitter receptor binding, in “Proteins of the Nervous System - Structure and Function”

    Google Scholar 

  • B. Haber, J. R. Perez-Polo and J. D. Coulter, Alan R. Liss Inc. New York.

    Google Scholar 

  • Kendall, D. A. Taylor, D. P. and Enna, S. J.. 1983, 3H-Tetrahydrotrazodone binding: association with serotoninl binding sites. Mol. Pharmacol, in press.

    Google Scholar 

  • Lang, B. Barnard, E. A. Chang, L. R. and Dolly, J. 0. 1979, Putative benzodiazepine receptor: a protein solubilized from brain. FEBS Lett, 104: 149–153.

    Google Scholar 

  • Miller, R. J. and Hiley, C. R. 1974, Anti-muscarinic properties of neuroleptics and drug-induced parkinsonism. Nature (London) 248: 596.

    CAS  Google Scholar 

  • MS’hler, H. Polc, P. Cumin, R. Pieri, L. and Kettler, R. 1979, Nicotinamide, a brain constituent with benzodiazepine-like actions. Nature 278: 563.

    Google Scholar 

  • Pert, C. and Snyder, S. H. 1974, Opiate receptor binding of agonists and antagonists affected differentially by sodium. Mol. Pharmacol, 10:868.

    Google Scholar 

  • Peroutka, S. J. and Snyder, S. H. 1981, Interactions of antidepressants with neurotransmitter receptor sites, in “Antidepressants: Neurochemical, Behavioral and Clinical Perspectives”, S. J. Enna, J. B. Malick, and E. Richelson, Raven Press, New York.

    Google Scholar 

  • Peroutka, S. J. U’Prichard, D. C. Greenberg, D. A. and Snyder, S. H. 1977, Neuroleptic drug interactions with norepinephrine a-receptor binding sites in rat brain. Neuropharmacology 16: 549.

    CAS  Google Scholar 

  • Reisine, T.D. Fields, J. Z. Stern, L. Z. Johnson, P.C. Bird, E. D. and Yamamura, H. I. 1977a, Alterations in dopaminergic receptors in Huntington’s disease. Life Sci. 21:1123.

    Google Scholar 

  • Reisine, T. D. Fields, J. Z. Yamamura, H. I. Bird, E. D. Spokes, E. Schreiner, P. S. and Enna, S. J. 1977b, Neurotransmitter receptor alterations in Parkinson’s disease. Life Sci, 21: 335.

    CAS  Google Scholar 

  • Rosenthal, H. E. 1967, Graphic method for the determination and presentation of binding parameters in a complex system. Anal. Biochem, 20:525.

    Google Scholar 

  • Scatchard,G. 1949, The attraction of protein for small molecules and ions. Ann. N.Y. Acad. Sci, 51:660.

    Google Scholar 

  • Schulster, D. and Levitzki, A. 1980, “Cellular Receptors for Hormones and Neurotransmitters”, John Wiley & Sons, New York.

    Google Scholar 

  • Shibuya, J. Bowie, D. and Pert, C. 1977, Opiate receptor ligand in cerebrospinal fluid: a simple radioreceptor assay requiring no preliminary purification. Proc. Soc. Neurosci, 3:460.

    Google Scholar 

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Enna, S.J. (1984). Radioligand Binding Assays. In: Cattabeni, F., Nicosia, S. (eds) Principles and Methods in Receptor Binding. NATO ASI Series, vol 72. Springer, Boston, MA. https://doi.org/10.1007/978-1-4757-1577-4_2

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  • DOI: https://doi.org/10.1007/978-1-4757-1577-4_2

  • Publisher Name: Springer, Boston, MA

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