Literature DB >> 24866501

A pharmacological paradox: may a neutral antagonist shift an agonist concentration-response curve to the left?

Thomas J Feuerstein1.   

Abstract

It is generally accepted that the presence of a competitive antagonist shifts an agonist concentration-response curve to the right. However, this may not always be the case: The concentration-response curve of an inverse receptor agonist may be shifted to the left by a neutral antagonist; a condition, which can be hypothetically explained by the assumption of both negative cooperativity of dimeric receptors plus a receptor reserve.

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Year:  2014        PMID： 24866501     DOI： 10.1007/s00210-014-0993-1

Source DB:  PubMed          Journal:  Naunyn Schmiedebergs Arch Pharmacol        ISSN： 0028-1298            Impact factor:   3.000


  7 in total

Review 1.  Mathematical analysis of the control of neurotransmitter release by presynaptic receptors as a supplement to experimental data.

Authors:  T J Feuerstein; N Limberger
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1999-05       Impact factor: 3.000

Review 2.  Dimerization of G protein-coupled receptors: CB1 cannabinoid receptors as an example.

Authors:  James Wager-Miller; Ruth Westenbroek; Ken Mackie
Journal:  Chem Phys Lipids       Date:  2002-12-31       Impact factor: 3.329

Review 3.  Basic concepts in G-protein-coupled receptor homo- and heterodimerization.

Authors:  Rafael Franco; Vicent Casadó; Antoni Cortés; Carla Ferrada; Josefa Mallol; Amina Woods; Carme Lluis; Enric I Canela; Sergi Ferré
Journal:  ScientificWorldJournal       Date:  2007-11-02

4.  Differential inhibitory effects of drugs acting at the noradrenaline and 5-hydroxytryptamine transporters in rat and human neocortical synaptosomes.

Authors:  M Mantovani; D J Dooley; A Weyerbrock; R Jackisch; T J Feuerstein
Journal:  Br J Pharmacol       Date:  2009-12       Impact factor: 8.739

5.  O-2050 facilitates noradrenaline release and increases the CB1 receptor inverse agonistic effect of rimonabant in the guinea pig hippocampus.

Authors:  Bernd Jergas; Kirsten Schulte; Laura Bindila; Beat Lutz; Eberhard Schlicker
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2014-05-23       Impact factor: 3.000

6.  Binding affinity and agonist activity of putative endogenous cannabinoids at the human neocortical CB1 receptor.

Authors:  Marc Steffens; Josef Zentner; Jürgen Honegger; Thomas J Feuerstein
Journal:  Biochem Pharmacol       Date:  2005-01-01       Impact factor: 5.858

Review 7.  Signal transduction of the CB1 cannabinoid receptor.

Authors:  Gábor Turu; László Hunyady
Journal:  J Mol Endocrinol       Date:  2009-07-20       Impact factor: 5.098
  7 in total
  1 in total

1.  O-2050 facilitates noradrenaline release and increases the CB1 receptor inverse agonistic effect of rimonabant in the guinea pig hippocampus.

Authors:  Bernd Jergas; Kirsten Schulte; Laura Bindila; Beat Lutz; Eberhard Schlicker
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2014-05-23       Impact factor: 3.000
  1 in total

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