Literature DB >> 2408209

Agonist potency and apparent affinity: interpretation using classical and steady-state ternary-complex models.

D Mackay1.   

Abstract

The relative potencies of agonists have been used in the past to classify receptors. This could be justified on the basis of ideas and equations developed using the occupancy model of drug action. Although attempts have been made recently to develop methods of analysis based on other models, these have not been entirely satisfactory. In this article Dennis Mackay explores possible interpretations of relative potency, apparent affinity and efficacy on the basis of a steady-state ternary-complex model. He concludes that use of these quantities to classify receptor-transducer systems may not be entirely dependable. However the steady-state model can explain why use of agonists to classify receptors has been successful in the past and why properties of agonists deduced from ligand binding studies may differ from their properties deduced from experiments on intact tissues.

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Year:  1990        PMID: 2408209     DOI: 10.1016/0165-6147(90)90036-8

Source DB:  PubMed          Journal:  Trends Pharmacol Sci        ISSN: 0165-6147            Impact factor:   14.819


  7 in total

Review 1.  Agonist binding, agonist affinity and agonist efficacy at G protein-coupled receptors.

Authors:  P G Strange
Journal:  Br J Pharmacol       Date:  2008-01-28       Impact factor: 8.739

Review 2.  The role of G proteins in transmembrane signalling.

Authors:  C W Taylor
Journal:  Biochem J       Date:  1990-11-15       Impact factor: 3.857

3.  Desensitization and functional antagonism by beta-adrenoceptor and muscarinic receptor agonists, respectively: a comparison with receptor alkylation for calculation of apparent agonist affinity.

Authors:  R M Eglen; W W Montgomery; R L Whiting
Journal:  Br J Pharmacol       Date:  1991-08       Impact factor: 8.739

4.  Determination of KA values by controlled receptor expression in Xenopus oocytes.

Authors:  H Murakoshi; K Nunoki; K Ishii; N Taira
Journal:  Br J Pharmacol       Date:  1995-10       Impact factor: 8.739

5.  Comparison of cromakalim-induced relaxation of potassium precontracted rabbit, cat, and rat isolated cerebral arteries.

Authors:  A A Parsons; E Ksoll; J R Mackert; L Schilling; M Wahl
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1991-04       Impact factor: 3.000

6.  Presynaptic alpha 2-autoreceptors in brain cortex: alpha 2D in the rat and alpha 2A in the rabbit.

Authors:  A U Trendelenburg; N Limberger; K Starke
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1993-07       Impact factor: 3.000

7.  The use of 4-diphenylacetoxy-N-(2-chloroethyl)-piperidine (4-DAMP mustard) for estimating the apparent affinities of some agonists acting at muscarinic receptors in guinea-pig ileum.

Authors:  R B Barlow; L S McMillen; M A Veale
Journal:  Br J Pharmacol       Date:  1991-03       Impact factor: 8.739

  7 in total

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