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which serotonin receptors are involved in anxiety

Agonism at 5-HT1A and antagonism at 5-HT2 (notably 2A) receptors induces anxiolysis. I don't know much about 5-HT6 but I would assume antagonism would tend towards promoting anxiolysis more so than agonism would at this receptor. 5-HT3 agonists are anxiogenic, and with a lot of antidepressants and antipsychotics acting as antagonists this receptor it would seem that it indeed plays a part in their anxiolytic effects.

Edit: Quick look around determined that it is actually agonism, not antagonism, that may induce anxiolytic effects when it comes to the 5-HT6 receptor.
 
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how important are 5ht1,5h4 receptors and 5ht5?? You never see drugs that acts on them. Usually just 5h2,5ht6,5ht7,5h3
 
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trainman04 said:
how important are 5ht1,5h4 receptors and 5ht5?? You never see drugs that acts on them. Usually just 5h2,5ht6,5ht7,5h3
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The 5HT1 family of receptors is actually a pretty important target for a number of psychiatric drugs.

Partial agonism of 5HT1A is thought to produce mood-lifting and anti-anxiety effects, which is why it is present with certain novel antidepressants (vilazodone), antipsychotics like Abilify and atypical anxiolytics like buspirone.

Also, triptan-class anti-migraine drugs seem to exert their effects by inducing vasoconstriction via 5HT1B/5HT1D agonism..
 
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So guys what type of receptors are there? What receptors do drugs act on for the mood effect? I know there are serotonin,dopamine histamine, alpha, beta receptors. Im not sure what alpha or beta receptors do but I think I know the other 3 . Histamine I think just like affects how tired you are right? and I know some drugs inhibit either of these SERT,NET or DAT to increase said neurontransmitter. but thats all I know. is there anything else to know?
what are the sigma receptors ?
 
Another class of receptors important for anxiety/fear conditioning are the glutamate receptors, including AMPA receptors. AMPA receptor antagonists are being investigated with promise for the treatment of fear related disorders like PTSD.

Much of glutamate is fundamentally responsible for learning, and anxiety/fear is a very learning based disorder.
 
i have a question about buspirone. its anti anxiety pill that affects serotonin, but why does it make me feel stoned and weird, not in any good way. i dont get its specific action if someone can try to explain??
 
Buspirone's primary activity is activating presynaptic 5-HT1a autoreceptors, which should result in decreased release of serotonin.
Buspirone has antagonist activity at D2, D3, and D4 dopamine receptors, and by blocking D2 autoreceptors it increases dopamine release.
In addition buspirone binds to some other subtypes of serotonin receptors (5HT-2a, 2b, 2c, 6, and 7), but much weaker than 5-HT1a.
It also has a metabolite (2-pyrimidylpiperazine) that acts as an alpha-2a adrenoreceptor antagonist, like yohimbine.

There's a chart of receptors and binding affinities on wiki. And a big list of possible side effects.
 
sekio said:
Buspirone's primary activity is activating presynaptic 5-HT1a autoreceptors, which should result in decreased release of serotonin.
Buspirone has antagonist activity at D2, D3, and D4 dopamine receptors, and by blocking D2 autoreceptors it increases dopamine release.
In addition buspirone binds to some other subtypes of serotonin receptors (5HT-2a, 2b, 2c, 6, and 7), but much weaker than 5-HT1a.
It also has a metabolite (2-pyrimidylpiperazine) that acts as an alpha-2a adrenoreceptor antagonist, like yohimbine.

There's a chart of receptors and binding affinities on wiki. And a big list of possible side effects.
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do you know why Buspirone made me dizzy/nauseous and gave me digestive issues
 
Cotcha Yankinov said:
Another class of receptors important for anxiety/fear conditioning are the glutamate receptors, including AMPA receptors. AMPA receptor antagonists are being investigated with promise for the treatment of fear related disorders like PTSD.

Much of glutamate is fundamentally responsible for learning, and anxiety/fear is a very learning based disorder.
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Zyprexa is the only med that has cured my anxiety do you know why?I always thought it was because it blocked so many serotonin receptors. thats why I wanted Mianserin, but there are many other things on zyprexas Pharmacology I have never heard about thats why I wonderd about different receptors etc.
 
trainman04 said:
do you know why Buspirone made me dizzy/nauseous and gave me digestive issues
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Those side effects are 5-HT1A activation related, and are apparently the reason why 5-HT1A full agonists haven't made it to market even though they may otherwise be helpful for some conditions.

With regards to Zyprexa's efficacy for your anxiety, this could be due to any number of reasons. Have you tried other antipsychotics that achieve appreciable dopamine receptor blockade, e.g. Risperidone? I wouldn't count Seroquel/quetiapine unless you've been up to very high doses, and even then its still different from other antipsychotics. The anti-dopamine properties can occasionally be helpful for some issues in particular people, such as intrusive thoughts/OCD/anxiety.
 
Cotcha Yankinov said:
Those side effects are 5-HT1A activation related, and are apparently the reason why 5-HT1A full agonists haven't made it to market even though they may otherwise be helpful for some conditions.

With regards to Zyprexa's efficacy for your anxiety, this could be due to any number of reasons. Have you tried other antipsychotics that achieve appreciable dopamine receptor blockade, e.g. Risperidone? I wouldn't count Seroquel/quetiapine unless you've been up to very high doses, and even then its still different from other antipsychotics. The anti-dopamine properties can occasionally be helpful for some issues in particular people, such as intrusive thoughts/OCD/anxiety.
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Only zyprexa and seroquel I have tried. Seorquel didnt work I tried up to 800mg. zyprexa worked first dosage. Seroquel also blocks serotonin receptors so i thought it would work but nop. thats why there must be some other mechanism .. Zyprexa is an Antagonist on 5ht1a
 
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I got mirtazapine today first time ever tried 30mg felt nothing wtf?????? Just got a little bit tired but thats it. I thought it was a potent antagonist on 5ht2
 
trainman04 said:
Only zyprexa and seroquel I have tried. Seorquel didnt work I tried up to 800mg. zyprexa worked first dosage. Seroquel also blocks serotonin receptors so i thought it would work but nop. thats why there must be some other mechanism .. Zyprexa is an Antagonist on 5ht1a
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Zyprexa is also a potent antagonist at the D2 dopamine receptor. If seroquel didn't work, maybe that's what you were lacking.
However, zyprexa also has additional functions, like alpha-adrenergic antagonism ("noradrenaline antagonism", if you will) that may contribute to its therapeutic efficacy.

OTOH, it might be that ultra-high-dose seroquel didn't work because even though it will show moderate dopaminergic effects at such an extreme dose, you will also produce larger amounts of the metabolite norquetiapine, which acts as a noradrenaline reuptake inhibitor (which is normally a good thing, but I could see how increased noradrenaline levels could become a problem for extremely anxious people).
 
trainman04 said:
I got mirtazapine today first time ever tried 30mg felt nothing wtf?????? Just got a little bit tired but thats it. I thought it was a potent antagonist on 5ht2
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Well, mirtazapine isn't an antipsychotic. I mean yes, it does relieve anxiety by blocking specific receptors like 5HT2a, but first and foremost it is generally regarded as an "atypical antidepressant":

Several of the other receptors it blocks are receptors that, when activated, actually limit the amount of neurotransmitters that can be released into the synapse everytime a signal hits that neuron. Consequently, blocking these receptors will allow your neurons to release *more* neurotransmitters. So in a way, it can be considered an "indirect SNRI" or (as Wikipedia describes it) an "indirect 5HT1A agonist", since it prevents those other receptors from killing your 5HT1A-mediated mood lift.
 
something is odd here
when i took white willow bark which blocks 5-HT2A & 5-HT2C I felt a little relief first dose!

mirtazapine however nothing!!!!!!!

....

 
What's the compound in willow bark that has affinity for 5HT receptors? I was under the impression that willow bark extract is mostly salicin (salicylic acid glucoside)
 
Salicin is the beta-glucoside of salicyl alcohol (o-hydroxybenzyl alcohol):

Salicin.jpg


More of willow bark phytochemicals: Phytochemicals and Constituents of Salix alba. The inner bark of the White Willow (Salix alba L.) contains tannins, flavonoids, phenolic glycosides, and anti-inflammatory and fever-reducing salicylates. Nov 13, 2017

Here'as a pdf with a rundown on willow bark phytochemicals: http://longwoodherbal.org/willowbark/willow.pdf

I found a reference to activity at 5HT receptors here but no specific phytochemical is described:
https://area1255.blogspot.com/2014/06/4-natural-otc-serotonin-antagonists.html
 
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A blog that opens with "The next Natural serotonin antagonist is called "Shilajit"." ... hmm no.
 
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