“Potency” and “Efficacy” of Drugs

Mehta, Mitali

doi:10.1002/j.1552-4604.1963.tb00055.x

Cited by 7 publications

(3 citation statements)

References 2 publications

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“…Potency of a drug refers to the amount of drug required to achieve a defined biological effect-the smaller the dose required, the more potent the drug, which is the same with EC 50 . 27,28) The p-synephrine targeting NMU2R efficacy, EC 50 , and potency values were 7.207, 6.604, 0.227 µmol/L, respectively, which manifested the high potency and high efficacy. And the potency and efficacy of p-synephrine are essentially the same with that of NMU by this screening system.…”

Section: Discussionmentioning

confidence: 96%

<i>p</i>-Synephrine: A Novel Agonist for Neuromedin U2 Receptor

Zheng

Guo

Wang

et al. 2014

Biological & Pharmaceutical Bulletin

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In the brain, Neuromedin U2 receptor (NMU2R) is prominent in the hypothalamic regions and is known to be associated with regulation of several important physiological functions, including food intake, energy balance, stress response, and nociception. In this article, by random screening of compounds using the model of high-throughput screening for NMU2R stable expression, NMU2R negative and NMU2R short hairpin RNA (shRNA) knockdown HEK293 cell lines, for the first time, we discovered that p-synephrine, which is the primary protoalkaloid in Citrus aurantium (bitter orange) and is widely used in weight loss and weight management products, is a highly potent and selective NMU2R agonist. In NMU2R activating ability experiments, p-synephrine was found binding to NMU2R with high efficacy and potency; the efficacy, 50% of the maximum possible effect (EC 50 ) and potency values were determined to be 7.207, 6.604 and 0.227 µmol/L for the NMU2R, respectively. Our researches have important theoretical value for elucidating the mechanisms of p-synephrine in body weight and energy balance regulation. These data provide further evidence for widespread roles for p-synephrine and its receptors in the brain.

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Section: Discussionmentioning

confidence: 96%

<i>p</i>-Synephrine: A Novel Agonist for Neuromedin U2 Receptor

Zheng

Guo

Wang

et al. 2014

Biological & Pharmaceutical Bulletin

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“…Potency and Efficacy A key issue in clinical pharmacology is the distinction between potency and efficacy (Mehta 1963). The potency of a drug is the dosage necessary to achieve a given effect.…”

Section: 'Member Of Scientific Staff Medical Research Councilmentioning

confidence: 99%

Clinical Pharmacology and Psychiatry

Lader

1967

Proceedings of the Royal Society of Medicine

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“…Efficacy relates to the maximum amplitude of a signaling response, whereas potency refers to the agonist concentration where signaling reaches the half-maximal response. Given their importance in describing such systems, efficacy and potency have been characterized for numerous ligand-receptor systems for several decades ( 13 ). In the case of GPCRs and their endogenous agonists, the amino acid sequence of a receptor and its 3D structure have been subject to strong selection pressure so that ligand efficacy and potency are within physiologically tolerable range.…”

Section: Introductionmentioning

confidence: 99%

Dissecting the allosteric networks governing agonist efficacy and potency in G protein-coupled receptors

Heydenreich

Martí-Solano

Sandhu

et al. 2021

Preprint

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G protein-coupled receptors (GPCRs) translate binding of extracellular ligands into intracellular responses through conformational changes. Ligand properties are described by the maximum response (efficacy) and the agonist concentration at half-maximal response (potency). Integrating structural changes with pharmacological properties remains challenging and has not yet been performed at the resolution of individual amino acids. We use epinephrine and β2-adrenergic receptor as a model to integrate residue-level pharmacology data with intramolecular residue contact data describing receptor activation. This unveils the allosteric networks driving ligand efficacy and potency. We provide detailed insights into how structural rearrangements are linked to fundamental pharmacological properties at single-residue level in a receptor-ligand system. Our approach can be used to determine such pharmacological networks for any receptor-ligand complex.

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“Potency” and “Efficacy” of Drugs

Cited by 7 publications

References 2 publications

<i>p</i>-Synephrine: A Novel Agonist for Neuromedin U2 Receptor

<i>p</i>-Synephrine: A Novel Agonist for Neuromedin U2 Receptor

Clinical Pharmacology and Psychiatry

Dissecting the allosteric networks governing agonist efficacy and potency in G protein-coupled receptors

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