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Re: Buspar - "partial" agonist?

Posted by Elizabeth on November 18, 1999, at 1:31:31

In reply to Buspar - "partial" agonist?, posted by Scott L. Schofield on November 17, 1999, at 11:42:07

> I often see buspirone (Buspar) described as being a "partial" agonist at 5-HT1a receptor sites.
> 1. What does "partial" mean?

A full agonist would be something that has the maximal effect at the receptor. (Serotonin, for example, is a full agonist at the 5-HT1a receptor.) A partial agonist has less than the full effect.

> 2. As an agonist, wouldn't it work against the antagonist activity of pindolol?

Pindolol preferentially blocks presynaptic autoreceptors, which serve to compensate for increased levels of neurotransmitter (presynaptic neurons sense that they are getting hit more, so they fire less often).

Pindolol has relatively weak antagonistic effects on the postsynaptic 5-HT1a's.




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