1-acetyl- LSD, a better LSD-alternative? (aka ALD-52)

Would you want to try 1-ACETYL-LSD/ ALD52 ?

  • Yes

    Votes: 4 66.7%
  • Maybe

    Votes: 2 33.3%
  • No

    Votes: 0 0.0%

  • Total voters
    6

Mauritio

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A few days ago I did a post on 2-bromo-LSD as a better LSD alternative .
2-bromo-lsd ,lacks the hallucinogenic effect of LSD ,which might be due to a stronger anti-serotonin effect .
The problem is: it is very hard to get and pretty expensive, plus its illegal .

Today I stumbled upon1-acetyl-LSD ,which is commonly sold as an LSD prodrug. It seems to be the case that it does have slightly different binding affinities to certain receptor and thus might be more or less serotonergic .

As it turns it it might be more anti-serotonergic ! This is what wikipedia says on it:

" The Hallucinogens by Hoffer and Osmond (1967), ALD-52 is listed as having a lower (approximately 1/5) intravenous toxicity (in rabbits), a lower (approximately 1/8) pyretogenic effect, an equal psychological effect in humans, and double the "antiserotonin" effect as compared with LSD.

One account found that there was less visual distortion than with LSD and it seemed to produce less anxiety and tenseness and that it was somewhat less potent"


So Hoffer himself confirms stronger anti-serotonin effects than with LSD.


Coincidentally theres a very recent study that supports the claim that it is less serotonergic/ more anti-serotonergic. Remember a good chunk of it is going to end up as LSD ,so there is going to be hallucinations, but it seems that this is a less serotonergic alternative to LSD .

"1-Acyl-substitution reduced the affinity of LSD for most monoamine receptors, including 5-HT2A sites, by one to two orders of magnitude. Although LSD acts as an agonist at 5-HT2 subtypes, ALD-52, 1P-LSD and 1B-LSD have weak efficacy or act as antagonists in Ca2+-mobilization assays."

From an article :
"The data showed that ALD-52, 1P-LSD, and 1B-LSD were very weak partial agonists at the human 5-HT2A compared to LSD. Interestingly, despite showing comparatively high affinity for 5-HT2B and 5-HT2C, the compounds showed no agonist activity at those receptors. This behavior is in contrast to LSD, which is an agonist at recombinant human 5-HT2B and 5-HT2C receptors."

This means that ALD52 is an antagonist at 5ht2b and c ! Plus a its just a very weak agonist on 5ht2a . Awesome.



Here's a report of guy who says that uses ald52 to get rid of his cluster headaches. Which are probably caused by serotonin .



This study shows that 1-acetyl-LSD, which is ALD52 ,is less potent at elevating brain serotonin and 2-bromo-lsd is actually even less potent at that .


Last but not least ALD52/ 1-acetyl-LSD is legal or at least tolerated in most countries. Which makes it a great legal LSD and 2-bromo-lsd alternative with a stronger anti-serotonin effect .
2-bromo-lsd still seems to be a bit stronger, but for now we have to go with ALD52.
 
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Mauritio

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This old study compared various LSD derivatives in terms of anti-serotonin effects and hallucinations.
Normal LSD has a 100 on both.
ALD-52 has a 100 on hallucinations and 210 on anti-serotonin effects ! Showing twice the capacity of LSD in that regard .

What is at least as interesting is that there's a chemical that has a 4 on hallucinations and a whooping 835 on anti-serotonin effects ! So it's almost non hallucinogenic but has very ,very strong anti-serotonin effects.
The name of the drug is :
d-1-methyl lysergic acid monoethylamide


 

Mauritio

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Looking a bit further I found a chemical that almost seems like a perfect anti-serotonin chemical.
It almost zero hallucinogenic potential and has an anti-serotonin effect that is more than 5 times higher than LSD .
The name is MBL61.
 

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Aad

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What about 1P-LSD?

I can get that quite easily here in the Netherlands.
 

Mauritio

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What about 1P-LSD?

I can get that quite easily here in the Netherlands.
Isnt ALD52 also legal ?
At least theres a shop from the Netherlands that sells it. It would be weird if they could sell it but people can't buy it .



But 1P-LSD seems to be pretty similar!
 
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Mauritio

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This part of the study shows how potent those substances are ,in activating the head head twitch response, which is a measure of serotonergic activity.
Interestingly ALD52 had 50% of lsd's potency, 1P-LSD one third and 1blsd had only 14% of lsd's serotonergic activity
So as 1b-lsd and 1P-LSD have similar activity at the 5ht2a, b and c receptors they might actually be an even better choice as they are less serotonergic.
This part is extra important as it was an in vivo experiment .

"Interestingly, the rank
order of potency of the four lysergamides is inversely proportional to the length of the
substituent present on the indole nitrogen. LSD, with an ED50 value of 132.8 nmol/kg
(Halberstadt and Geyer 2013), is the most potent compound in this series; ALD-52 and 1P-LSD
have about half and one-third of the potency of LSD, respectively, whereas 1B-LSD is even less
potent, acting with ~14%
of the potency of LSD. An extra-sum-of-squares F-test confirmed that
ALD-52 (F(1,22) = 12.08, p=0.0021) is less potent than LSD in mice; similar results were reported previously for 1P-LSD and 1B-LSD (Brandt et al. 2016; Brandt et al. 2019)."
 

Mauritio

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It's seems not clear how much of their own effects on the 5ht receptors they can really bring to the table, as they're rapidly metabolized into lsd and other derivatives. Plus they have do compete with LSD for the binding at the 5ht2a receptor .
On the other if the effect was completely congruent with lsd there wouldnt be a different head twitch response ,indicating lower serotonin activity.

"Although ALD-52, 1P-LSD, and 1B-LSD likely act as prodrugs for LSD, they do retain some
affinity and efficacy at the 5-HT2A receptor, which makes it difficult to completely exclude the
possibility that some of their in vivo effects occur because they interact directly with 5-HT
receptors. It seems unlikely, however, that direct receptor interactions play a role in the
mechanism of action of ALD-52 and 1P-LSD. First, ALD-52 and 1P-LSD have considerably
lower affinity and functional potency compared to LSD at 5-HT2A, so they would have to
compete with LSD for access to the receptor."
 

Mauritio

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To go full circle here : 1cP-LSD also seems to behave similarly to the 3 lsd derivatives mentioned above .
Which means :similar head twitch response of about one third of the potency of LSD . Plus possible antagonism at 5ht2b and c . And weak agonism at 5ht2a. And of course serving as a prodrug for LSD .
1cP-LSD seems to have 99% bioavailability, so you need to dose about one fourth less than with normal LSD (75%)
Peat approved doses are below 20mg .
From my own experience with 1cp I'd say start with 5mcg and work your way up .

"1CP‐LSD also induces the head‐twitch response (HTR) in C57BL/6 J mice, indicating that it produces an LSD‐like behavioural profile. 1CP‐LSD induced the HTR with an ED50 = 430.0 nmol/kg which was comparable to 1P‐LSD (ED50 = 349.6 nmol/kg) investigated previously."
 
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