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.
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
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.
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.
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.
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.
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.
Bylund, D. B. 1980, “Receptor Binding Techniques”, Society for Neuroscience, Bethesda, Maryland.
Burt, D. R. Creese, I. and Snyder, S. H. 1977, Antischizophrenic drugs: chronic treatment elevates dopamine receptor binding in brain. Science 196: 326.
Chang, R. and Snyder, S. H. 1978, Benzodiazepine receptors: labeling in intact animals with 3H-flunitrazepam. Eur. J. Pharmacol, 48:213.
Costa, E. and Guidotti, A. 1979, Molecular mechanisms in the receptor action of benzodiazepines. Ann. Rev. Pharmacol. Toxicol, 19:531.
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.
Simantov, R. Childers, S. and Snyder, S. H,, 1977, Opioid peptides: differentiation by radioimmunoassay and radioreceptor assay, Brain Res, 135: 358.
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.
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.
Yamamura, H. I. Enna, S. J. and Kuhar, M. J. 1978, Neurotransmitter Receptor Binding“, Raven Press, New York.
Creese, I. Schneider, R. and Snyder, S. H. 1977, 3H-Spiroperidol labels dopamine receptors in pituitary and brain. Eur. J. Pharmacol, 46:377.
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.
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.
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.
Enna, S. J. 1983b, Receptor regulation in, “Handbook of, Neurochemistry”, Vol. 6, A. Lajtha, ed. Plenum Press, New York
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.
Enna, S. J. and Kendall, D. A. 1981, Interaction of antidepressants with brain neurotransmitter receptors. J. Clin. Psychopharmacol, 1:12S.
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.
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.
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.
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.
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.
Gavish, M. Chang, R. S. and Snyder, S. H. 1979, Solubilization of histamine H-1, GABA and benzodiazepine receptors. Life Sci. 25: 783.
Hill, A. W. 1910, The possible effects of the aggregation of the molecules of hemoglobin on its dissociation curves. J. Physiol, 40:iv.
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.
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”
B. Haber, J. R. Perez-Polo and J. D. Coulter, Alan R. Liss Inc. New York.
Kendall, D. A. Taylor, D. P. and Enna, S. J.. 1983, 3H-Tetrahydrotrazodone binding: association with serotoninl binding sites. Mol. Pharmacol, in press.
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.
Miller, R. J. and Hiley, C. R. 1974, Anti-muscarinic properties of neuroleptics and drug-induced parkinsonism. Nature (London) 248: 596.
MS’hler, H. Polc, P. Cumin, R. Pieri, L. and Kettler, R. 1979, Nicotinamide, a brain constituent with benzodiazepine-like actions. Nature 278: 563.
Pert, C. and Snyder, S. H. 1974, Opiate receptor binding of agonists and antagonists affected differentially by sodium. Mol. Pharmacol, 10:868.
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.
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.
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.
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.
Rosenthal, H. E. 1967, Graphic method for the determination and presentation of binding parameters in a complex system. Anal. Biochem, 20:525.
Scatchard,G. 1949, The attraction of protein for small molecules and ions. Ann. N.Y. Acad. Sci, 51:660.
Schulster, D. and Levitzki, A. 1980, “Cellular Receptors for Hormones and Neurotransmitters”, John Wiley & Sons, New York.
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.
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 1984 Springer Science+Business Media New York
About this chapter
Cite this chapter
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
Download citation
DOI: https://doi.org/10.1007/978-1-4757-1577-4_2
Publisher Name: Springer, Boston, MA
Print ISBN: 978-1-4757-1579-8
Online ISBN: 978-1-4757-1577-4
eBook Packages: Springer Book Archive