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Could Buspar produce Psychedelic symptoms?

chicken hoagie

chicken hoagie

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I was doing research on Buspar (a medication I had been given by my doctor for anxiety, added on to my suboxone maintenance), and I saw that Buspar was an Agonist for the 5HT2A serotonin receptor. Knowing that agonists of this receptor are typically drugs of the psychedelic class, it made me wonder if it was possible that Buspar maybe had any psychedelic effects or at least psychedelic-like symptoms.


Anyones thoughts on this?

It is also said that Buspar releases oxytocin through 5HT1A agonism. Seems like an interesting drug, but anecdotes don't seem to bring up much interest for it.
 
138nM binding affinity at 5HT2a is quite high, so that would suggest it could produce psychedelic effects in high enough dosages. However my thinking is the dosages required will be many times higher than the dosages in standard preparations. Also it might activate a different signalling pathway which does not produce psychedelic effects.
 
Buspirone is probably a 5-HT2A antagonist, meaning it doesn't activate 5-HT2A. In any event, buspirone is selective for several other receptors vs. 5-HT2A, meaning that it may not interact with 5-HT2A at reasonable doses.
 
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according to this chart it is a 5HT2a Agonist, not sure if that is significant.
wQXKGJE.jpg


OP or anyone else, has Buspar been effective for treating anxiety?
 
Sigmond said:
according to this chart it is a 5HT2a Agonist, not sure if that is significant.
wQXKGJE.jpg


OP or anyone else, has Buspar been effective for treating anxiety?
Click to expand...

Source for the chart ? Ive read everywhere else that its an antagonist.
 
Its from the wikipedia page- the source from there is http://kidbdev.med.unc.edu/databases/pdsp.php..

I am unsure if its reliable..curious if this drug has been proven effective for anxiety.

I searched a bit..sekio should have an accurate answer...

sekio said:
5ht1a receptor activation is associated with anxiolysis and euphoria, 5ht2a agonism is responsible for "classical" hallucinatory/psychedelic effects.

Compare buspirone (5ht1a) to 25I-NBOMe (5ht2a)
Click to expand...

after more searching I believe that chart is probably inaccurate...blame wikipedia.
 
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serotonin2A said:
The PDSP is a database of affinities, not of functional effects.
Click to expand...

Can you elaborate on this? I thought affinities were a matter of how well a molecule is attracted and attaches to a ligand? If it is indeed an agonist of the 5HT2A receptor, then it should produce classical psychedelic effects correct?
 
chicken hoagie said:
Can you elaborate on this? I thought affinities were a matter of how well a molecule is attracted and attaches to a ligand? If it is indeed an agonist of the 5HT2A receptor, then it should produce classical psychedelic effects correct?
Click to expand...
It's not an agonist, it's an antagonist. Does it really make sense to you that they would develop a 5-HT2A agonist as an antianxiety medicine?

Another way to tell its an antagonist is to look at the structure. The pyrimidinylpiperazine part of the molecule could fit into the 5-HT2A agonist site, but the 8-azaspiro[4.5]decane-7,9-dione tail is too long.
 
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Actually, I personally do believe a 5HT2A agonist could be an anxiolytic...at times. but in all practicality, yes i do see how it could be an antagonist. Okay, so would Buspar be chemically related to trazodone?
 
Also, I'm wondering about the side effect of premature ejaculation...

you see, I've been having DELAYED ejaculation...and a bit of ED...


So i've been curious about how it may help this problem.

So far, I have really had no improvement from what I have been taking...3 x 5mg a day.
 
Guys, I'm almost sure buspar is a 5ht2a antagonist. Such action would contribute to anxiolysis. I have also found that snorting buspar while on the comedown from 25c-nbome deals a big blow to lingering psychedelia and insomnia
 
So you find it helpful for anxiety? I ask because most people seem to find it rather useless.
 
yea, prozac and zoloft have gone through an absurd amount of clinical trials where each drug was proven unquestionably effective for treating depression. yet 40-50% of the population considers them about as effective as chewing gum. I am aware of its intended purpose I just wanted to know how it worked for you.
 
chicken hoagie said:
Actually, I personally do believe a 5HT2A agonist could be an anxiolytic...at times. but in all practicality, yes i do see how it could be an antagonist. Okay, so would Buspar be chemically related to trazodone?
Click to expand...

they are similar both have a piperazine with an aromatic ring on one nitrogen and a tail with a H bond acceptor on the other nitrogen but trazodone it's more potent as a 5HT2A antagonist than 5HT1A (partial) agonist while for buspirone it's the inverse...ipsapirone that has an aromatic ring on the tail seems structurally more similar to trazodone
 
I found the stuff didn't suit me at all but those dopamine antagonist values read like a neuroleptic and the structure also LOOKS like a neuroleptic. If it's the 5HT1a agonist activity that mediates the effects, that's a dirty drug. Tandospirone is even dirtier
 
clubcard said:
I found the stuff didn't suit me at all but those dopamine antagonist values read like a neuroleptic and the structure also LOOKS like a neuroleptic. If it's the 5HT1a agonist activity that mediates the effects, that's a dirty drug. Tandospirone is even dirtier
Click to expand...

All drugs have off-target effects. Selectivity also matters. The D2 affinity of buspirone is much lower than the affinity for 5-HT1A. Testing has confirmed that even high doses of buspirone (120 mg) do not produce clinically relevant levels of D2 blockade.

http://www.ncbi.nlm.nih.gov/pubmed/26089182

In contrast to those results, typical antipsychotics are usually dosed to produce ~70% D2 occupation in schizophrenia patients.
 
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