The Cheng-Prusoff Equation

It can be seen that the IC50 increases with increasing values of [A ]/Kd in accordance with simple competitive antagonism. This can be tested by comparison of the data to the Cheng-Prusoff equation (Equation 4.12). The data in Table 12.2b... [Pg.256]

The ICS0 is used in a version of the Cheng-Prusoff equation for functional assays. Thus, the apparent Kb (apparent equilibrium dissociation constant for the antagonist-receptor complex) is given by... [Pg.271]

Several brevetoxins have been examined for their respective abilities to competitively displace tritiated brevetoxin PbTx-3 from its specific site of action in brain synaptosomes. Analysis of IC q values revealed no marked differences in the displacing abilities between any of the type-1 toxins, and similarly there was no apparent difference between displacing abilities of PbTx-1 or -7, both type-2 toxins. Although some specific details require correlation, a gross comparison indicates that sodium channels in brain are similar in the systems examined. In the system studied most extensively, the rat brain synaptosome, t-test analysis revealed no significant differences between PbTx-2 and PbTx-3 IC q, or between PbTx-1 and PbTx-7 IC q, but statistically significant differences were found between the two classes (P<0.01) (5). If the Cheng-Prusoff equation (15) is applied ... [Pg.171]

Figure 2.22. The Cheng-Prusoff equation. The relation between the dissociation constant of an inhibitor...

Consideration of the Cheng-Prusoff equation (eqn [5]) provides the rationale. Since and Ki... [Pg.4185]

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