Receptor-ligand binding parameters

Table 3.11 Some Receptor-Ligand Binding Parameters... 

Receptor occupancy refers to the ratio of receptors occupied by a ligand at equilibrium and the total number of receptors available, usually expressed as a percentage of the total number of receptors. Since it is often not possible to quantify the total number of receptors or the number of receptors occupied by a ligand, another parameter called binding potential is often used to measure receptor occupancy. Binding potential (BP) refers to the ratio of the maximum number of receptors and the equilibrium dissociation constant of the drug, so that % receptor occupancy equals to... 

The above discussion provides only a brief overview of how fluorescence techniques can be used to study the interactions of ligands with their receptors. We have focused on the quantitation of the binding parameters and compared the data with that which may be obtained with those from radiolabelled ligand binding studies. The number of applications of fluorescence in the study of neurochemistry and molecular biology is ever increasing. Outside the scope of this review is, for example, the use of fluorescence microscopy to monitor cell surface expression and targeting of receptors or the use of fluorescence probes to monitor ion transport into and out of cells. 

Borea PA, Varani K, Dalpiaz A, Capuzzo A, Fabbri E, IJzerman AP (1994) Full and partial agonistic behavior and thermodynamic binding parameters of adenosine A3 receptor ligands. Eur J Pharmacol 267(1) 55-61... 

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