Surmountable antagonist

Competitive blocker A surmountable antagonist one that can be overcome by increasing the dose of agonist... 

FIGURE 6.1 Effects of antagonists on agonist dose-response curves, (a) Surmountable antagonism with no diminution of maxima and no limiting antagonism (competitive antagonists). 

The kinetics of offset of the antagonist from the receptor can dictate whether surmountable or insurmountable antagonism is observed. 

The most common method used to measure the affinity of surmountable competitive antagonists is Schild analysis. This method is visual and also is useful to detect nonequilibrium steady states in receptor preparations. 

Used to estimate system-independent potency of a simple competitive antagonist that produces surmountable antagonism of agonist response. 

Surmountable antagonism, an antagonist-induced shift to the right of an agonist dose-response curve with no diminution of the maximal response to the agonist (observed with simple competitive antagonists and some types of allosteric modulators). 

The action of the antagonist can be overcome by a sufficient increase in the concentration of agonist (i.e., the antagonism is surmountable). 

If the antagonism is of the equilibrium type, the antagonism increases as the concentration of the antagonist increases. Conversely, the antagonism can be overcome (surmounted) if the concentration of the agonist in the biophase (the region of the receptors) is in-... 

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