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A dose response curve showing the normalised tissue response to stimulation by an agonist. Low doses are insufficient to generate a response, while high doses generate a maximal response. The steepest point of the curve corresponds with an EC 50 of 0.7 molar.
1 de dez. de 2004 · Agonists bind to receptors to produce a functional response. Agonists can be full, partial or inverse. Antagonists reverse the effects of agonists. Antagonists can be competitive or non-competitive. Receptors.
- DG Lambert
- 2004
The addition of a competitive antagonist to an agonist will lead to a shift in the agonist dose–response curve to the right because higher agonist concentrations are now required to achieve a given percentage receptor occupancy (and therefore effect) (Fig B).
Dose-response, which involves the principles of pharmacokinetics and pharmacodynamics, determines the required dose and frequency as well as the therapeutic index for a drug in a population. The therapeutic index (ratio of the minimum toxic concentration to the median effective concentration) helps determine the efficacy and safety of a drug.
- Abimbola Farinde
5 de mai. de 2021 · Agonists are evaluated by a concentration-response curve (CRC), with a midpoint (EC 50) that indicates potency, a high-concentration asymptote that indicates efficacy, and a low-concentration asymptote that indicates constitutive activity.
- Dinesh C. Indurthi, Anthony Auerbach
- 10.1016/j.bpj.2021.02.034
- 2021
- Biophys J. 2021 May 4; 120(9): 1800-1813.
Here, we show that agonist efficiency can be estimated from a single concentration-response curve (CRC) and estimate efficiencies of 20 nicotinic receptor agonists. These have a bimodal distribution with larger agonists belonging to the lower
Parallel rightward shifts in an agonist concentration–response curve with no effect on the maximal response are widely accepted as the cardinal features of a simple competitive interaction, but are also characteristic of an allosteric modulator which reduces agonist affinity for the receptor (see, for example, Hall, 2000 ).
