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Re: inverse agonist,- partial agonist ??

Posted by SLS on January 18, 2004, at 11:05:23

In reply to inverse agonist,- partial agonist ??, posted by linkadge on January 18, 2004, at 9:25:27

> Does anyone here know what an 'inverse agonist' is, or what a 'partial agonist' is.

A partial agonist binds to a receptor (strongly or weakly), but doesn't always stimulate it to perform its function. Sometimes it does and sometimes it doesn't I don't know the molecular details, but perhaps there are variable allosteric interactions that occur upon binding.

An inverse agonist of a receptor produces an effect opposite to what would occur upon stimulation. I guess an example of that would be the resting potential of a neuron (values are not physiological). Let us say that without receptor stimulation, the intrinsic resting potential of the cell is 5V. Upon stimulation of the receptors, the potential increases to 10V, the threshold upon which the neuron fires. When an inverse agonist binds to these same receptors, the potential of the cell drops to 2V. Now, in order to get the cell to fire, it will take a greater number of receptors to be stimulated in order to reach the 10V threshold. It will take an additional 8V in order to make up for the number of receptors affected by the inverse agonist.

I hope that helped.


- Scott

 

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poster:SLS thread:302265
URL: http://www.dr-bob.org/babble/20040118/msgs/302298.html