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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]

The lower the IC50 or K, the higher the affinity. Results can also be expressed as a K, the inhibitory (or affinity) constant of the displacer compound for the receptor. and IC50 are not independent and are very simply related when the displacement is non-competitive (/T = IC50), but the relationship becomes more complicated (Cheng-Prusoff" equation) for a competitive displacement [/T = ICsq/) + [L]/A d) where [L] is the concentration of the radioactive ligand]. [Pg.75]

Lazareno, S. and Birdsall, N.J.M. (1993) Estimation of competitive antagonist affinity from functional inhibition curves using the Gaddum, Schild and Cheng-Prusoff equations. Br. J. Pharmacol 109 1110-1119. [Pg.49]

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

See other pages where Cheng-Prusoff equation is mentioned: [Pg.116]    [Pg.131]    [Pg.133]    [Pg.154]    [Pg.155]    [Pg.213]    [Pg.107]    [Pg.272]    [Pg.167]    [Pg.49]    [Pg.256]    [Pg.36]    [Pg.265]    [Pg.252]    [Pg.380]    [Pg.380]    [Pg.383]    [Pg.304]    [Pg.305]    [Pg.326]    [Pg.332]    [Pg.56]    [Pg.341]    [Pg.478]    [Pg.481]    [Pg.4181]    [Pg.369]    [Pg.130]    [Pg.166]    [Pg.275]   
See also in sourсe #XX -- [ Pg.131 , Pg.191 ]



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