Posted by Quintal on August 17, 2007, at 22:54:37
In reply to Re: Beta-carbolines and benzos, posted by linkadge on August 17, 2007, at 22:32:24
Well benzodiazepine antagonists apparently have no clinical effects on healthy persons, whereas inverse agonists have the opposite effect of an agonist i.e. GABA-A agonist will mimic the effect of GABA, whereas a GABA-A inverse agonist will not simply oppose the effect of GABA, but produce the opposite effects such as anxiety, convulsions etc. Antagonists neutralize the effects of both agonists and antagonists. So, for example, flumazenil has no effect on people not dependent on, or who have no tolerance to benzodiazepines. So tolerance is more complicated than simple receptor downregulation because the brain may also upregulate the production of endogenous GABA-A inverse agonists to counteract the effect.
Wiki explains it better:
__________________________________________________Receptor agonists, antagonists and inverse agonists bind to the same receptor types. The pharmacological effect of an inverse agonist is measured as the negative value of the agonist primarily due to the historical findings of the already known agonist. Therefore, if the agonist has a positive value and the inverse agonist has a negative value, the antagonist for the receptor takes both the agonist and inverse agonist back to a neutral state.
http://en.wikipedia.org/wiki/Inverse_agonist
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poster:Quintal
thread:776629
URL: http://www.dr-bob.org/babble/20070815/msgs/776873.html