5-MeO Tryptamine

[DL-ark]

This is a chemical which has been used as a precursor many times in the synthesis of certain chemicals. However it is also a full agonist of all 5HT receptors except for 5HT3. This includes 5HT2a. There is an erowid report of it which reports light psychedelia and visuals at doses of 40mg. This of course is anecdotal, yet promising. -cut-

 

[endotropic]

I know it seems innocuous, but we don't allow even general references to synthesis routes.



Very convenient that it doesn't activate 5-HT3, that would really limit its potential.

 

[DL-ark]

Sorry about the synthesis, was trying to comment on its availibilty. MY BAD

 

[DL-ark]

Also, if it is not very psychedelic in action it would likely have a relaxing effect due to 5HT6 release of gaba. However, 5-HT2C and 5-HT1a are anxiogenic, so this may counteract the action of 5HT6. another problem however is of course 5ht2b toxicity.

 

[WSH]

Also, if it is not very psychedelic in action it would likely have a relaxing or euphoriant effect due to 5ht6/5ht1a or 5ht2c. One problem however is of course 5ht2b

Out of the receptors you mentioned only 5-ht6 is relaxing, 5-ht2c is anxiogenic and even though the postsynaptic 5-ht1a can also be relaxing, the more relevant presynaptic 5-ht1a obviously has the opposite effect.

 

[DL-ark]

I mean that respectively: 5-HT2C is euphoriant in nature, and 5ht6 and 5ht1a. I did not know that 5ht1a could be anxiogenic.

Thank you for the info, I fixed it.

 

[endotropic]

Out of the receptors you mentioned only 5-ht6 is relaxing, 5-ht2c is anxiogenic and even though the postsynaptic 5-ht1a can also be relaxing, the more relevant presynaptic 5-ht1a obviously has the opposite effect.

But the 5-HT1A partial agonists are anxiolytic. That's a strange receptor, that one.

 

[WSH]

I mean that respectively: 5-HT2C is euphoriant in nature, and 5ht6 and 5ht1a. I did not know that 5ht1a could be anxiogenic.

5-ht2c is anxiogenic too:

Overexpression of 5-HT2C receptors in forebrain leads to elevated anxiety and hypoactivity

In general, it is accepted that 5-HT2C receptor agonists increase anxiety behaviours and induce hypophagia.

 

[DL-ark]

5-ht2c is anxiogenic too:

Overexpression of 5-HT2C receptors in forebrain leads to elevated anxiety and hypoactivity

I know it is, but it is still responsible for dopamine release. ​Nevermind

Does anyone know how inhibitory 5HT6 is?

 

[WSH]

I know it is, but it is still responsible for dopamine release.

Nope, 5-ht2c actually INHIBITS dopamine release:

Modulation of dopamine release by striatal 5-HT2C receptors.

These data contribute to a body of evidence indicating that 5-HT2C receptors inhibit nigrostriatal dopaminergic transmission.

 

[DL-ark]

Nope, 5-ht2c actually INHIBITS dopamine release:

Modulation of dopamine release by striatal 5-HT2C receptors.

Oh god, I am terribly sorry - I think I was thinking of another receptor.

 

[WSH]

Oh god, I am terribly sorry - I think I was thinking of another receptor.

Maybe you confused 5-ht2c with 5-ht2a, because 5-ht2a is the one that INCREASES dopamine release:

The activation of 5-HT receptors in prefrontal cortex enhances dopaminergic activity.

These results indicate that the activity of VTA DA neurones is under the excitatory control of 5-HT 2A receptors in the mPFC.

Also, if it is not very psychedelic in action it would likely have a relaxing effect due to 5HT6 release of gaba. However, 5-HT2C and 5-HT1a are anxiogenic, so this may counteract the action of 5HT6.

Yes, the question is how high are the affinities for 5-ht6 vs 5-ht2c and presynaptic 5-ht1a?

edit: here they are:
5-ht1a: ~3 nM
5-ht2a: ~5 nM
5-ht2c: 45 nM
5-ht6: ~50 nM

 

[DL-ark]

Maybe you confused 5-ht2c with 5-ht2a, because 5-ht2a is the one that INCREASES dopamine release:

The activation of 5-HT receptors in prefrontal cortex enhances dopaminergic activity.





Yes, the question is how high are the affinities for 5-ht6 vs 5-ht2c and presynaptic 5-ht1a?

edit: here they are:
5-ht1a: ~3 nM
5-ht2a: ~5 nM
5-ht2c: 45 nM
5-ht6: ~50 nM

Interesting, where did you get these numbers, I want to look at some of the other affinities.

 

[WSH]

Interesting, where did you get these numbers, I want to look at some of the other affinities.

5-Methoxytryptamine

 

[DL-ark]

Interesting, thank you.

 

[blueberries]

But the 5-HT1A partial agonists are anxiolytic. That's a strange receptor, that one.

This is what I have found. Agonising 5HT1a releases norepinephrine and dopamine, modulates serotonin and as a result produces euphoria, anxiolysis, anti-depression, anti-emetic properties and has also been shown to interact with BDNF (in what way, though, we do not know).

 

[WSH]

This is what I have found. Agonising 5HT1a releases norepinephrine and dopamine, modulates serotonin and as a result produces euphoria, anxiolysis, anti-depression, anti-emetic properties and has also been shown to interact with BDNF (in what way, though, we do not know).

Just to make that clear, these effects (euphoria, anxiolysis, anti-depression, anti-emetic properties) are POSTSYNAPTIC.

When you take a 5-ht1a agonist, it mainly activates PRESYNAPTIC receptors, giving directly opposite effects (dysphoria, anxiogenesis, pro-depression, pro-emetic properties).

 

[DL-ark]

Then what is the point of anti-anxiety drugs like buspirone, which work based on the 5-ht1a receptor?

 

[WSH]

Then what is the point of anti-anxiety drugs like buspirone, which work based on the 5-ht1a receptor?

After a couple of weeks, the presynaptic 5-ht1a receptors desensitize, leading to enhanced postsynaptic transmission and anxiolysis.

It's just that this initial phase can be VERY unpleasant (depending on the dosage, but a low dose is obviously also less effective).

 

[DL-ark]

Still, do you think that activity on 5-ht1a is going to affect 5-meo-tryptamines positive effects? It has very high affinity for 5-ht2a which is very promising. If 5-meo-T is taken, what do you guess the effects would be?