Posted by SLS on May 25, 2003, at 12:05:28
In reply to Partial agonists » SLS, posted by Ritch on May 25, 2003, at 11:10:18
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.
> 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?
Perhaps one way to conceptualize a partial agonist is to think of it as a duplicate key that wasn't cut properly. Sometimes it unlocks the door and sometimes it fails to unlock the door, depending on how you jiggle it in or out. It is possible to turn the key half-way before it stops, thereby changing the length of the bolt, but not enough to clear the hole. The door cannot be opened.I tried. :-)
Regarding Abilify, I haven't read enough about the details regarding how and why it behaves differently in the presence of varying concentrations of dopamine within the synapse.
- Scott
poster:SLS
thread:227600
URL: http://www.dr-bob.org/babble/20030525/msgs/229024.html