Literature DB >> 974318

The use of different agonists in antagonist affinity constant estimations.

F Roberts, R P Stephenson.   

Abstract

1 The affinities of 4 muscarinic antagonists were estimated on intact pieces of guinea-pig ileum using the agonists carbachol and pentyl trimethylammonium both in separate experiments and in the same experiment. 2 The apparent affinities were slightly but consistently higher when estimated from the responses produced by pentyl trimethylammonium than when estimated from the responses produced by carbachol. 3 This difference was greatly reduced or abolished if totally denervated logitudinal muscle strips were used rather than intact pieces of ileum. It is therefore suggested that the difference is due to the presence of receptors in the ganglionic layer. 4 To explain the difference in apparent affinity of the antagonists these receptors can not be identical to the muscarinic receptors on the smooth muscle. 5 In addition they can not be nicotinic ganglionic receptors as the difference did not appear to be affected by the presence or absence of hexamethonium.

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Year:  1976        PMID: 974318      PMCID: PMC1667273          DOI: 10.1111/j.1476-5381.1976.tb07679.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  5 in total

1.  THE UPTAKE OF ATROPINE AND RELATED DRUGS BY INTESTINAL SMOOTH MUSCLE OF THE GUINEA-PIG IN RELATION TO ACETYLCHOLINE RECEPTORS.

Authors:  W D PATON; H P RANG
Journal:  Proc R Soc Lond B Biol Sci       Date:  1965-08-24

2.  Specificity of some ganglion stimulants.

Authors:  R B Barlow; F Franks
Journal:  Br J Pharmacol       Date:  1971-05       Impact factor: 8.739

3.  On the measurement of the affinity of partial agonists for receptors.

Authors:  D R Waud
Journal:  J Pharmacol Exp Ther       Date:  1969-11       Impact factor: 4.030

4.  Relationships between chemical structure and affinity for acetylcholine receptors.

Authors:  F B Abramson; R B Barlow; M G Mustafa; R P Stephenson
Journal:  Br J Pharmacol       Date:  1969-09       Impact factor: 8.739

5.  Actions of some esters of 3,3-dimethylbutan-1-ol (the carbon analogue of choline) on the guinea-pig ileum.

Authors:  R B Barlow; J H Tubby
Journal:  Br J Pharmacol       Date:  1974-05       Impact factor: 8.739

  5 in total

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