Literature DB >> 2329803

Estimation of agonist affinity and efficacy by direct, operational model-fitting.

P Leff1, D J Prentice, H Giles, G R Martin, J Wood.   

Abstract

A few years ago Black and Leff (1983) presented a theoretical model for agonist action that can be fitted directly to experimental agonist concentration-effect data in order to estimate affinities and relative efficacies of agonists. The model has been successfully applied to data obtained using experimental designs commonly employed in pharmacologic experiments. This article describes the methodology used to fit the model equations to data for full and partial agonists, shows how affinity and efficacy estimates are calculated for these values, and shows how experimental design influences these calculations.

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Year:  1990        PMID: 2329803     DOI: 10.1016/0160-5402(90)90066-t

Source DB:  PubMed          Journal:  J Pharmacol Methods        ISSN: 0160-5402


  29 in total

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2.  Classification of platelet and vascular prostaglandin D2 (DP) receptors: estimation of affinities and relative efficacies for a series of novel bicyclic ligands. With an appendix on goodness-of-fit analyses.

Authors:  P Leff; H Giles
Journal:  Br J Pharmacol       Date:  1992-08       Impact factor: 8.739

3.  Conformational changes in the M2 muscarinic receptor induced by membrane voltage and agonist binding.

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4.  Modelling of alpha1-adrenoceptor-mediated temporal dynamics of inotropic response in rat heart to assess ligand binding and signal transduction parameters.

Authors:  P Sermsappasuk; M Weiss
Journal:  Br J Pharmacol       Date:  2009-02-13       Impact factor: 8.739

5.  Endothelial modulation of alpha 1-adrenoceptor contractile responses in the tail artery of spontaneously hypertensive rats.

Authors:  A Tabernero; J Giraldo; N M Vivas; A Badia; E Vila
Journal:  Br J Pharmacol       Date:  1996-10       Impact factor: 8.739

6.  A method for the quantification of biased signalling at constitutively active receptors.

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Journal:  Br J Pharmacol       Date:  2018-04-25       Impact factor: 8.739

7.  5-HT7 receptor efficacy distribution throughout the canine stomach.

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Journal:  Br J Pharmacol       Date:  2004-08-31       Impact factor: 8.739

8.  Analysis of the effects of alpha 1-adrenoceptor antagonists on noradrenaline-mediated contraction of rat small mesenteric artery.

Authors:  P H Van der Graaf; N P Shankley; J W Black
Journal:  Br J Pharmacol       Date:  1996-07       Impact factor: 8.739

9.  Hydromorphone efficacy and treatment protocol impact on tolerance and mu-opioid receptor regulation.

Authors:  Priyank Kumar; Soujanya Sunkaraneni; Sunil Sirohi; Shveta V Dighe; Ellen A Walker; Byron C Yoburn
Journal:  Eur J Pharmacol       Date:  2008-08-30       Impact factor: 4.432

10.  Estimation of partial agonist affinity by interaction with a full agonist: a direct operational model-fitting approach.

Authors:  P Leff; I G Dougall; D Harper
Journal:  Br J Pharmacol       Date:  1993-09       Impact factor: 8.739

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