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Inverse agonist

Author : Pierre Allain Date : 2010-1-30

The concept of inverse agonist is based on the idea that the receptor and its transduction system leading to an effect has a basal activity in absence of any agonist (transmitter), the agonist increases this basal activity and the inverse agonist decreases it, the antagonist inhibits the effect of the agonist.

The concept of inverse agonist can be interesting in well defined experimental conditions but appears not very useful in clinical pharmacology and therapeutics where multiple direct and indirect effects are observed and it seems sometimes used to promote new drugs with limited interest.

The concept of transmitter, agonist/receptor in which the transmitter or agonist is necessary to induce an activity and the concept of antagonist (competitive or not) in which the antagonist prevent the action of the agonist appear generally sufficient as a pharmacological basis.


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