Literature DB >> 2024288

How we describe competitive antagonists: three questions of usage.

D H Jenkinson1.   

Abstract

Competitive antagonists are used by pharmacologists in a definitive manner in the identification of receptor subtypes. However, despite the many decades of their use, there is still some confusion over terms and terminology. Don Jenkinson, a member of the IUPHAR Committee on Receptor Nomenclature, points to terms that are often used imprecisely: pA2 is frequently used interchangeably, but erroneously, for log KB; the term 'competitive' itself has been used ambiguously, and it is even possible that confusion can arise by the expression of the constant from the Schild equation in different ways (affinity/equilibrium/dissociation constants).

Mesh:

Year:  1991        PMID: 2024288     DOI: 10.1016/0165-6147(91)90497-g

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


  18 in total

1.  Functional and electrophysiological effects of a novel imidazoline-based K(ATP) channel blocker, IMID-4F.

Authors:  G A McPherson; K L Bell; J L Favaloro; M Kubo; N B Standen
Journal:  Br J Pharmacol       Date:  1999-12       Impact factor: 8.739

2.  Characterization of muscarinic receptor subtypes inhibiting Ca2+ current and M current in rat sympathetic neurons.

Authors:  L Bernheim; A Mathie; B Hille
Journal:  Proc Natl Acad Sci U S A       Date:  1992-10-15       Impact factor: 11.205

3.  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

4.  Antisecretory actions of a novel vasoactive intestinal polypeptide (VIP) antagonist in human and rat small intestine.

Authors:  Matthew R Banks; Michael J G Farthing; Patrick Robberecht; David E Burleigh
Journal:  Br J Pharmacol       Date:  2005-04       Impact factor: 8.739

5.  Increased alphaCGRP potency and CGRP-receptor antagonist affinity in isolated hypoxic porcine intramyocardial arteries.

Authors:  Philip Hasbak; Karen Eskesen; Søren Schifter; Lars Edvinsson
Journal:  Br J Pharmacol       Date:  2005-07       Impact factor: 8.739

6.  Modulation of inwardly rectifying currents in rat sympathetic neurones by muscarinic receptors.

Authors:  H S Wang; D McKinnon
Journal:  J Physiol       Date:  1996-04-15       Impact factor: 5.182

7.  Pharmacological analysis of the CCKB/gastrin receptors mediating pentagastrin-stimulated gastric acid secretion in the isolated stomach of the immature rat.

Authors:  D M Hills; V P Gerskowitch; S P Roberts; N J Welsh; N P Shankley; J W Black
Journal:  Br J Pharmacol       Date:  1996-12       Impact factor: 8.739

8.  Pharmacological analysis of CCK2 receptor antagonists using isolated rat stomach ECL cells.

Authors:  E Lindström; M Björkqvist; R Håkanson
Journal:  Br J Pharmacol       Date:  1999-05       Impact factor: 8.739

9.  Analysis of the pharmacokinetic/pharmacodynamic relationship of a small molecule CXCR3 antagonist, NBI-74330, using a murine CXCR3 internalization assay.

Authors:  L A Jopling; G F Watt; S Fisher; H Birch; S Coggon; M I Christie
Journal:  Br J Pharmacol       Date:  2007-11-05       Impact factor: 8.739

10.  Comparison of the cromakalim antagonism and bradycardic actions of a series of novel alinidine analogues in the rat.

Authors:  J L Challinor-Rogers; T K Hay; G A McPherson
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1994-08       Impact factor: 3.000

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