Abstract
Receptor-ionophore proteins which mediate postsynaptic membrane responses to neurotransmitters can be studied in vitro by suitable radioactive ligand binding assays. Radioactive ligands are most appropriate when they act as potent and specific agonists or antagonists on the synapse under study. Drugs or toxins meeting these specifications are available for identification of numerous neurotransmitter receptors (Changeux et al., 1975; Cuatrecasas, 1974); in other cases binding of the radioactive neurotransmitter itself has been utilized (Snyder & Bennett, 1976). In very few cases have ligands been available for potential identification of elements other than the neurotransmitter recognition site (receptor) involved in mediating postsynaptic membrane responses (Young & Snyder, 1974; Bon & Changeux, 1975; Eldefrawi et al. 1977). Identification of binding sites in vitro as physiologically relevant postsynaptic receptor-ionophore proteins requires that numerous criteria be met, such as suitable quantity, binding affinity, tissue and subcellular location, and chemical specificity of the binding sites. In practice this last criterion demands quantitative estimates of dose-effect relationships for drugs active on the tissue under study and at least one such drug which is very specific for the receptor-ionophore as opposed to other potential binding proteins.
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Olsen, R.W., Greenlee, D., Van Ness, P., Ticku, M.K. (1978). Studies on the Gamma-Aminobutyric Acid Receptor/Ionophore Proteins in Mammalian Brain. In: Fonnum, F. (eds) Amino Acids as Chemical Transmitters. NATO Advanced Study Institutes Series, vol 16. Springer, Boston, MA. https://doi.org/10.1007/978-1-4613-4030-0_36
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