Abstract:
Radiolabelled ligand binding studies remain one of the most widely used techniques in characterizing the biochemical and pharmacological properties of receptors. In this chapter, we provide an overview of radiolabelled ligand binding, discussing both theoretical and practical aspects of these experiments. Specific protocols that have been used in our laboratories to study the binding of radiolabelled ligands to two members of a ligandāgated ion channel family i.e., the nicotinic and GABAA receptors are included.
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Abbreviations
- ACh:
-
acetylcholine
- DNPP:
-
diethylāpānitrophenyl phosphate
- GABA:
-
Ī³āaminobutyric acid
- nAChR:
-
nicotinic acetylcholine receptor
References
Agey MW, Dunn SMJ. 1989. Kinetics of [3H]muscimol binding to the GABAA receptor in bovine brain membranes. Biochemistry 28: 4200.
Boeynaems JM, Dumont JE. 1975. Quantitative analysis of the binding of ligands to their receptors. J Cyclic Nucl Res 1: 123.
Cheng Y, Prusoff W. 1973. Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 22: 3099.
Connors KA. 1987. Binding constants: the measurement of molecular complex stability. New York: John Wiley and Sons.
Cornishā Bowden A, Koshland DE. 1975. Diagnostic uses of the Hill (logit and Nernst) plots. J Mol Biol 95: 201.
Dupont Y. 1984. A rapid filtration technique for membrane fragments or immobilized enzymes: measurements of substrate binding or ion fluxes with a few millisecond time resolution. Anal Biochem 142: 504.
Ehrlich P. 1913. Address to the International Medical Congress, London. Lancet 2: 445.
Elliott J, Blanchard SG, Wu W, Miller J, Strader CD, et al. 1980. Purification of Torpedo californica postāsynaptic membranes and fractionation of their constituent proteins. Biochem J 185: 667.
Hulme EC. 1992. Receptorāligand interactions: a practical approach. Oxford: IRL Press.
Klotz IM. 1982. Numbers of receptor sites from Scatchard graphs: facts and fantasies. Science 217: 1247.
Klotz IM. 1983. Ligandāreceptor interactions: what we can and cannot learn from binding measurements. TIPS 4: 253.
Norby JG, Ottolenghi P, Jensen J. 1980. Scatchard plot: common misinterpretation of binding experiments. Anal Biochem 102: 318.
Scatchard G. 1949. The attractions of proteins for small molecules and ions. Ann NY Acad Sci 51: 660.
Wieland GA, Molinoff PB. 1981. Quantitative analysis of drugāreceptor interactions: I. Determination of kinetic and equilibrium properties. Life Sci 29: 313.
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Martin, I.L., Davies, M., Dunn, S.M.J. (2007). Characterization of Receptors by Radiolabelled Ligand Binding Techniques. In: Lajtha, A., Baker, G., Dunn, S., Holt, A. (eds) Handbook of Neurochemistry and Molecular Neurobiology. Springer, New York, NY. https://doi.org/10.1007/978-0-387-30401-4_10
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DOI: https://doi.org/10.1007/978-0-387-30401-4_10
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