![Positive allosteric modulator antagonists (PAM-antagonists) move agonist dose-response curves to lower agonist concentrations by increasing agonist affinity, but decrease maximal response by decreasing agonist efficacy via their antagonist capability. Plot shows receptor response (%) as a function of logarithmic agonist concentration ([Ago]). This is just an example and the units of concentration do not matter. Solid curve: original agonist response. Dashed curves: 2 possible response curves (out of many alternatives) after PAM-antagonist addition. Arrows show approximate direction of the shift of curves after addition. Adapted from: Kenakin TP (2017). Pharmacology in drug discovery and development: understanding drug response (2nd ed.). Academic Press. pp. 109–110. ISBN 9780128037539. See also: Br J Pharmacol. 2012;165(6):1659-1669. doi:10.1111/j.1476-5381.2011.01749.x. PMID 22023017.](http://upload.wikimedia.org/wikipedia/commons/7/7e/Positive_allosteric_modulator_antagonist_plot.svg)
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Summary
| Description |
Positive allosteric modulator antagonists (PAM-antagonists) move agonist dose-response curves to lower agonist concentrations by increasing agonist affinity, but decrease maximal response by decreasing agonist efficacy via their antagonist capability.
Plot shows receptor response (%) as a function of logarithmic agonist concentration ([Ago]). This is just an example and the units of concentration do not matter. Solid curve: original agonist response. Dashed curves: 2 possible response curves (out of many alternatives) after PAM-antagonist addition. Arrows show approximate direction of the shift of curves after addition. Adapted from:
See also:
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| Author | 5-HT2AR |
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