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Partial agonists » SLS

Posted by Ritch on May 25, 2003, at 11:10:18

In reply to Re: abilify/trileptal/zoloft, posted by SLS on May 24, 2003, at 12:14:29

> Hi Mitch.
>
> A partial agonist binds to a receptor just as does an agonist or antagonist. However, it does not always stimulate the receptor into action. I would guess that it probably depends on which of the alternating states (conformations) the molecules exist as they switch back and forth between their different three dimensional arrangements. I'm not sure though.
>
>
> - Scott
>
>

Scott- here are two lines in the link you posted that comes the closes for me to understand this I think ;)

B. When is a partial agonist a good therapeutic agent?

1. the safe dose range can be greatly extended (the maximum response only reaches the sub-100% value and stays there as a plateau)

2. when the antagonist properties of the partial agonist are desirable (blunting effects of endogenous substances, for example)(example: pindolol)


Would a partial agonist be analogous to a pistol that is cocked and ready to fire which is easy to uncock relative to other pistols? This is that "goldilocks" thing with Abilify isn't it? It isn't supposed to bind tightly (hence it is a partial agonist), so the molecule doesn't stay "stuck" on receptor?


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poster:Ritch thread:227600
URL: http://www.dr-bob.org/babble/20030525/msgs/229015.html