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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 4 of 4. This is the beginning of the thread.
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?
(pre-synaptic vs post-synaptic?)2. As an agonist, wouldn't it work against the antagonist activity of pindolol?
Thanks.Scott
Posted by Rick on November 18, 1999, at 1:17:12
In reply to Buspar - "partial" agonist?, posted by Scott L. Schofield on November 17, 1999, at 11:42:07
The following site addresses your questions and related issues. This is a page from the middle of the presentation, but the bullet point at the end is particularly pertinent (...and surprising: it suggests that a Buspar/pindolol combination has a potent and rapid-onset antidepressant effect).
Rick
http://www.med.nyu.edu/Psych/aug/sld035.htm
> I often see buspirone (Buspar) described as being a "partial" agonist at 5-HT1a receptor sites.
>
> 1. What does "partial" mean?
> (pre-synaptic vs post-synaptic?)
>
> 2. As an agonist, wouldn't it work against the antagonist activity of pindolol?
>
>
> Thanks.
>
> Scott
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.
Posted by Scott L. Schofield on November 19, 1999, at 9:23:59
In reply to Re: Buspar - "partial" agonist?, posted by Elizabeth on November 18, 1999, at 1:31:31
> > 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.Next question.
Is this less-than-full effect the result of a weaker binding affinity or due to a lack of stimulation of the receptor, even though it may be tightly bound?
Thanks again.
Oh yeah... Next question
I was under the impression that there is a high density of axono-dendridic 5-HT1a autoreceptors. Are these inhibitory or excitatory?
Thanks again.
Oh yeah... Oh forget it.
- Scott
This is the end of the thread.
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