Antagonizing Dopamine receptor (Buspirone)

[F1n1shed]

Buspirone is an anxiolytic drug which exerts several central effects. It antagonizes presynaptic inhibitory DA2 autoreceptors at dopaminergic neurons.

It later says Buspirone significantly increased levels of noradrenaline, dopamine, and free serotonin but did not affect levels of adrenaline etc.


Doesn't antagonizing the DA2 receptor mean less dopamine for that recepor, less firing? Or does it mean it blocks the reuptake, i am a bit confused on how this drug causes an increase of dopamine levels.

 

[sekio]

Doesn't antagonizing the DA2 receptor mean less dopamine for that recepor, less firing?

Yup, exactly. However autoreceptors are special, they are the body's way of sensing and controlling neurotransmitter concentration. When they are blocked and don't get signalled as much your body thinks "oh, there must not be enough dopamine" and increases release.

There are autoreceptors for serotonin, norepinephrine/adrenaline, dopamine, and so on.

 

[dopamimetic]

Oh, this is new data - previously buspirone was thought to be a "mild" neuroleptic, but then it is more like (ami)sulpride which also raises dopamine levels when using low doses.

But buspirone binds around 10 times stronger to D3/D4 receptors than D2, doesn't this mean that in a dose where the D2 auto receptors are blocked but not (many) of the post-synaptic ones, it will already exhibit neuroleptic action at the D3/D4 receptors?

I found buspirone to be completely useless (and causing much the same brain-zap sensation as on discontinuing a SSRI) when I've tried it as an anxiolytic in doses from 5 to 50mg.. maybe I've just missed the sweet spot or it is even below 5mg?

 

[F1n1shed]

Oh, this is new data - previously buspirone was thought to be a "mild" neuroleptic, but then it is more like (ami)sulpride which also raises dopamine levels when using low doses.

But buspirone binds around 10 times stronger to D3/D4 receptors than D2, doesn't this mean that in a dose where the D2 auto receptors are blocked but not (many) of the post-synaptic ones, it will already exhibit neuroleptic action at the D3/D4 receptors?

I found buspirone to be completely useless (and causing much the same brain-zap sensation as on discontinuing a SSRI) when I've tried it as an anxiolytic in doses from 5 to 50mg.. maybe I've just missed the sweet spot or it is even below 5mg?

My doc wrote me a script for it and i don't know if i want to try it. I do know that in most cases you always want to be on an SSRI then combine the buspirone as they work together ... or more efficiently together. I would like more dopamine as i know higher levels of serotonin cause dopamine levels to decrease. I read about sex drive going up with it which is needed obv as SSRI's hurt you in that field.

How long were you on this drug? I am thinking of giving it a try soon ... but don't know

 

[danglesmcgee]

hmm im interested in buspirone. Doc prescribed it for me for anxiety and add. It took 3 weeks before it helped with anxiety, he said it helps to manage anxiety as a whole. it requires you to build up the drug in your system before it begins to work. I have been using it daily for about 5 months now, very few if any side effects, it does help with anxiety, i take 15mg x3 times a day, also take concerta 36mg/day. Im curious as to how these two drugs interact?

Any input anyone? much appreciated.

 

[danglesmcgee]

ive been on it for months. I think its great for anxiety, does help with being able to focus too. just kind of calms you down. But its a very suttle drug, dont let this fool you, after a few weeks or more then it begins to really take effect. Its great because it has no side effects that i can think of. First time taking 15mg i went into a weird serotonin type headspin, like coming up on magic mushrooms. but only lasts 10 mins or so. Its a weird drug, i dont fully understand it.

 

[Dresden]

I didn't like Buspar.