Literature DB >> 2180161

Errors in agonist affinity estimation: do they and should they occur in isolated tissue experiments?

P Leff1, I G Dougall, D H Harper, I A Dainty.   

Abstract

Two plausible theories of agonist action - the isomerization and ternary complex mechanisms - predict that agonist affinity measured using the inactivation method may be subject to overestimation. Moreover, the greater the intrinsic efficacy, the greater the predicted error. But are these predictions correct, and are they borne out by experimental data? Paul Leff and colleagues argue that accurate agonist affinity constants can be measured despite these predictions, but that effort must be made to detect any potential errors that might be anticipated from theory.

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Year:  1990        PMID: 2180161     DOI: 10.1016/0165-6147(90)90319-4

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


  11 in total

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Review 2.  Drugs and receptors. An overview of the current state of knowledge.

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Review 3.  The role of G proteins in transmembrane signalling.

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4.  The role of alpha 1-adrenoceptor subtypes in the phasic and tonic responses to phenylephrine in the longitudinal smooth muscle of the rat portal vein.

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5.  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

6.  Characterization of histamine-H3 receptors controlling non-adrenergic non-cholinergic contractions of the guinea-pig isolated ileum.

Authors:  S J Taylor; G J Kilpatrick
Journal:  Br J Pharmacol       Date:  1992-03       Impact factor: 8.739

7.  Central alpha 2-autoreceptors: agonist dissociation constants and recovery after irreversible inactivation.

Authors:  E Agneter; H Drobny; E A Singer
Journal:  Br J Pharmacol       Date:  1993-02       Impact factor: 8.739

8.  Pharmacological estimation of agonist affinity: detection of errors that may be caused by the operation of receptor isomerisation or ternary complex mechanisms.

Authors:  P Leff; D Harper; I A Dainty; I G Dougall
Journal:  Br J Pharmacol       Date:  1990-09       Impact factor: 8.739

9.  Rabbit isolated renal artery contractions by some tryptamine derivatives, including 2-methyl-5-HT, are mediated by a 5-HT1-like receptor.

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Journal:  Br J Pharmacol       Date:  1992-10       Impact factor: 8.739

10.  Mediation by the same muscarinic receptor subtype of phasic and tonic contractile activities in the rat isolated portal vein.

Authors:  M Pfaffendorf; P A Van Zwieten
Journal:  Br J Pharmacol       Date:  1993-01       Impact factor: 8.739

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