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Biotech / Medical : ACADIA Pharmaceuticals Inc (ACAD) -- Ignore unavailable to you. Want to Upgrade?


To: tuck who wrote (410)4/7/2007 1:16:02 PM
From: tommysdad  Read Replies (2) | Respond to of 588
 
<<So they are apparently looking for an inverse agonist that will have the same neuropsychiatric effects as an antagonist, but without the side effects of antagonism. Or in any case, they are trying to sidestep the side effects, whether they have to antagonize or inverse agonize. Have I got that right?>>

It is pretty tough to argue that a so-called inverse agonist will avoid any side effect of an antagonist against the same target. In fact, the whole concept of "inverse agonism" being relevant to the in vivo situation is still quite controversial. Think global warming without Al Gore.

But the second paper is about partial agonists. This is very different from an inverse agonist. A partial agonist will do whatever the natural ligand (agonist) will do, just not as well ("well" defined as efficacy, not potency). An antagonist blocks the effects of agonists (theoretically, any agonist). An "inverse agonist" blocks not only the effects of agonists, but blocks any "constituitive" activity of the receptor (i.e., activity of receptor that occurs in the absence of binding of the natural agonist).

I apologize if this is old news to you -- by comparing the two papers it appeared you were equating "partial agonist" with "inverse agonist".