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The Large and Nifty Not-quite-advanced Drug Chemistry, Pharmacology and More Thread

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Phenibut is supposed to induce relaxation and sleep, well it makes me hyper...energized with no intention of relaxing....weird.
 
How dumb is this LSD analogue?

Sorry if this might sound a bit dumb. This is going to be a very short thread I guess but I didn't know where to ask.
After some research on 5-HT2a receptors and overlapping various psychedelics like Bromodragonfly, 5-MeO-DMT, DOB and LSD, a certain scheme seems to emerge (at least in my head).
Also on chemspider and pubchem I also saw a couple LSD analogues never discussed here. Theese where 5-OH-LSD, 5-MeO-LSD (and also the dimethylaziridine version of LA-ss-Az BTW but let's put that aside). Wiki also states that the trifluoromethyl version of 2CB-FLY is much more potent than the former.
Well I know that psychoactive chemestry isn't really like playing Lego but i wanned to hear from you your expectations on the following substance and how it could be bettered.

56furan7trifluorolassaz.png


I pur an R since I was really undecided what to put on the 6-N considering that ETH-LAD is more potent but has a greater tendency to spontaneously decay even at 0°C. PRO-LAD is more pontet but shorter acting. AL-LAD also seems to be nothing that special and I haven't found any concrete info on CYP-LAD and FLUORETH-LAD (though this last one seems to fascinate some BLs)

I apologize in advance if this might be a naive suggestion.
(Murphy please be gentle this time)
 
Fluoreth-LAD seems like one of shulgin's worse ideas to me... wouldn't that produce fluoroacetate as a metabolite?

As for your chemwank... I don't think you can extrapolate from phen/trypt SAR to lysergamides. They bind differently I think...
 
Well, I don't think that the dimethylazetidide really adds much potency, and at the same time it makes it way harder to synthesize and it probably (this is just a guess) decreases action at a number of other non-5ht2a receptors that may have partially been responsible for LSD's magic.

I've wondered for a while if 7-substitution of tryptamines would add something interesting, though, ever since I heard about this stuff.

dread said:
Fluoreth-LAD seems like one of shulgin's worse ideas to me... wouldn't that produce fluoroacetate as a metabolite?
Click to expand...

If it's active in the 100 ug range, it'll produce a scary 5 ug of fluoroacetate. I think that's not terribly concerning. When your doses are as small as they are with the lysergamides, you tend to not worry as much about toxic metabolites.
 
Somehow it seems that both psych-phens and trypts share some SAR when speaking of 5-HT2a.

To confirm this a subtance like (4S) N,N-dimethyl-1,3,4,5-tetrahydrobenzoindol-4-amine should be tested for psychedelic activity.

Though this does not explain why primary amine tryptamines are almost non active while primary amine psychedelic phenylethylamines are...
 
atara said:
Tryptamine is active, for about seven minutes:

http://www.erowid.org/library/books_online/tihkal/tihkal53.shtml

I'd assume they're destroyed really quickly by MAO, since AMT is perfectly active and it's a primary amine tryptamine.
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I've been wondering what effects(if any) tryptamine produced, thanks. I was certainly thinking it would be active since it is very similar to dmt and serotonin.

He also says that tryptophan is converted to tryptamine while from what I can see the pathway is tryptophan > 5-htp > serotonin > normelatonin > melatonin. Is it converted to tryptamine, maybe to a lesser amount or did he have the wrong information?

I've tried l-tryptophan sublingually in the past and I had intermittent visuals(moving things had an acceleration and kept moving even after they had stopped, trails, after images, things looked bright and novel), however I had done DPT the night before so I'm not so sure I can attribute it to tryptophan.
 
hmm did shulgin ever try 4-ho-tryptamine, just thought if it worked IV that could actually be REALLY experimental to have a super FAST acting psycadelic.
 
Assuming that the byproducts really aren't produced in big enough quantities, then an Ethyl on the 6-N may be interesting if it was stable. Personally I'm not too thrilled about continuously tacking on subtle changes, ie. 2C-I,B,T,T7, oh-lsd, meo-variants, etc. But it may be worth pursuing
 
/navarone/ said:
[Your molecule]
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D.E. Nichols has mentioned he was planning on making a few LSD metabolites to test the activity of with his Purdue research team. He specifically mentioned one with a hydroxyl on the benzene (13-HO-LSD, if I recall correctly) giving his personal suspicion of why it would be active, lab rat changes in response to light and sound over time, etc. that jazz in detail. This was supposed to be published July/June 2010 but I've yet to see/hear anything of it yet. Either way I think it makes sense (re: 13-OH-LSD) both logically and when you look at the binding pocket.

As for your specific molecule I personally don't think it will fair so well at 5-HT2A. My reasons are;
1) The furan ring's oxygen is on the the incorrect side, as far as I see it working - sure, in a phenethylamine it would be correct, however LSD is tilted quite different than PEAs when docking.
2) It makes more sense (for me) to start with OH, MeO, Me, Eth working way up to a trifluoromethyl group instead of copy-pasting from 2C-TFM.
3) Furan might destroy pi-pi interaction in general, specifically with the benzene on LSD with phenylalanine (Phe340), if not most likely hinder it. Any chemists want to correct me?

That's my thoughts, can't promise it is without fault however.
 
^ I see, however i don't quite get what u said about the furan oxygen, The oxygen is exactly at the same carbon than 5-Meo-DMT, and for what I've seen so far LSD seems to follow all th tryptamine rules when speaking of pychedelic activity. I don't see how the oxygen at the other side would allow hydrogen bonding. (BTW has a furan or dihydrofuran analogue of 5-MeO-DXT ever been tested?)
Also about the furan interacting with the pi-pi activity, I knew that BOD was quite active as well even if it has a beta methoxy wich compensates for the negative charge activity of the LSD 9-10 doublebond. Do these 2 groups compete for the same hydrogen bonding when docking?

I obviously don't know that much about 5-HT2a docking. A grat deal of what i know so far comes from an amazing thread by F&B about 5-HT2a SAR which I'll link below.

http://www.bluelight.ru/vb/showthread.php?t=167978
 
nuke said:
After some really large doses I got really bad tremors and I would be afraid that if you used it regularly for a while and suddenly stopped it might cause seizures, like benzodiazepines.
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My wife has taken gabapentin at grams daily, with whole bottle taken in a day often. Long term, perhaps ten years, though of course doses did not start at that level. Recently she was in jail for about a week without meds and when she was released I obseved what gabapentin WD's at what I assume are about as bad as they likely get. And of course the underlying bi-bolar which she is prescibed these she has other scripts for fibromyalgia (sp?) among others but the BP is the true reason. While she was a mental wreck (jails probably didn't help) I saw no physical issues. No tremors and certainly no seizures. However she had feeling of suicide. The with WD's seem to be purely mental but very bad.One person is not a case study of course.
 
/navarone/ said:
^ I see, however i don't quite get what u said about the furan oxygen, The oxygen is exactly at the same carbon than 5-Meo-DMT, and for what I've seen so far LSD seems to follow all th tryptamine rules when speaking of pychedelic activity.
Click to expand...

The methoxy can more freely accommodate the oxygen unlike the furan ring however. As I said, it's from my understanding and is given with no guarantee of being 100% correct. From the docking layouts it seems like it wouldn't work on LSD, but who knows.

You should read Towards a biophysical understanding of hallucinogen action., some other Nichols' work and RA Glennon (if you haven't) if you want to better understand the binding pocket of 5-HT2A. There are other works by other researchers but I'm not on my computer currently. You'd be able to answer your own question about the drawn compound after, most likely.
 
Production

Ok, so i can get 1kg of coke paste.
How do i cut it? I was thinking of adding 2 - 5% beta blockers. This can prevent your heart from going haywire in case the user takes to much. Might even extend the level where od happens!
Whats your thougts?
 
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