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Related Concept Videos

Dose-Response Relationship: Overview01:03

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Agonists can bind with and activate receptors, resulting in the formation of drug-receptor complexes. Once formed, these complexes catalyze many biochemical processes at the cellular level and subsequently induce a pharmacologic response. The degree of response is directly proportional to the fraction of activated receptors, which in turn, depends on the concentration of the drug at the receptor site as well as the sensitivity of the receptor. An increase in the administered dose contributes to...
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The receptor occupancy theory connects a drug's response to the number of occupied receptors. With higher drug concentrations, more receptors are occupied, leading to increased responses. The formation of drug-receptor complexes involves association and dissociation rates, which reach equilibrium when the forward and backward reactions are equal. The equilibrium association constant (Ka) and its inverse, the equilibrium dissociation constant (Kd), indicate drug affinity. Higher Ka and lower...
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Dose-Response Relationship: Potency and Efficacy01:22

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The potency of a drug is the measure of its ability to produce a biological response and can be compared by looking at the half-maximum effective concentration or EC50 values of different drugs. A lower EC50 value indicates higher potency of the drug. In the dose–response curve of two antihypertensive drugs, candesartan and irbesartan, a significant difference is observed in their EC50 values. A lower EC50 value for candesartan indicates that it is more potent than irbesartan, as it...
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Drug-receptor interaction describes the binding of receptors by drugs, but not all drug-receptor interactions result in activation and tissue response. For instance, the binding of agonists activates the receptor to generate a cellular reaction, while antagonists bind to receptors without causing their activation.
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The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
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When drugs are administered, they can elicit either an agonist or antagonist effect on the body. Agonism occurs when a drug activates a specific receptor, triggering a biological response. On the other hand, antagonism happens when a drug binds to the same receptors but blocks their activation, thereby preventing a biological response.
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Quantifying Agonist Activity at G Protein-coupled Receptors
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Agonist efficiency from concentration-response curves: Structural implications and applications.

Dinesh C Indurthi1, Anthony Auerbach1

  • 1Department of Physiology and Biophysics, State University of New York at Buffalo, Buffalo, New York.

Biophysical Journal
|March 6, 2021
PubMed
Summary
This summary is machine-generated.

Researchers developed a new method to calculate agonist efficiency (η) from concentration-response curves (CRCs). This efficiency metric, related to binding energy and receptor activation, can predict full CRCs and receptor activity from single measurements.

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Molecular Biology

Background:

  • Agonists are characterized by concentration-response curves (CRCs) detailing potency (EC50), efficacy, and constitutive activity.
  • Agonist efficiency (η), the fraction of binding energy driving receptor activation, is a crucial but less understood attribute.
  • Current methods for CRC analysis do not fully capture the nuances of agonist-induced receptor conformational changes.

Purpose of the Study:

  • To introduce and validate a novel method for calculating agonist efficiency (η) from existing CRC data.
  • To explore the relationship between agonist headgroup size and efficiency in nicotinic acetylcholine receptors.
  • To demonstrate how η can be used to estimate entire CRCs and receptor activation parameters.

Main Methods:

  • Calculation of agonist efficiency (η) using EC50 and asymptote values from single-channel or whole-cell CRCs.
  • Analysis of η distribution for 20 agonists acting on skeletal muscle nicotinic receptors.
  • Correlation analysis between agonist headgroup volume and calculated efficiency values.

Main Results:

  • Agonist efficiency (η) can be accurately derived from EC50 and CRC asymptotes.
  • A bimodal distribution of η was observed for nicotinic receptor agonists, with distinct populations around 51% and 40%.
  • High-efficiency agonists exhibited smaller headgroup volumes (70 ų) compared to low-efficiency agonists (102 ų).

Conclusions:

  • Agonist efficiency (η) is a quantifiable attribute derivable from standard CRC parameters.
  • The size of an agonist's headgroup is inversely related to its efficiency, influencing receptor activation.
  • Knowledge of η allows for the estimation of complete CRCs and constitutive activity from minimal data, streamlining drug discovery.