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deonylzolpidem

Adrenochrome

Adrenochrome

Ex-Bluelighter
Joined
Dec 3, 2004
Messages
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What would happen if we took off the double bonded oxygen in zolpidem and replaced it with 2 hydrogens?
more SERT?
 
Zolpidem.png


so, you want to change the amide to an amine?
 
Are you looking for it's 'psychedelic' effects? Are zolpidem's visual effects due to serotonin or gaba?
 
Couldn't one cleave off the whole 1-methylbenzyl group from zolpidem and have a possibly more active tryptamine derivative?

zolpidemcleavent8.gif


Wouldn't this just be a nitrogenated form of the beta-ketone form of 5-Me-DMT??

Smiles is included in the picture.

This could also be combined with the original posters idea to make the form minus the beta ketone which could be more active.
 
I doubt the drawing in post #5 would be active at all. What is the goal of deonylzolpidem? CE/OEVs? Drunken Euphoria?

Maybe it'll still produce the visuals that ambien does, but I can only think of one depressant that doesn't have a double bonded oxygen. I don't know if that's requirement for activity in the SARs of these Z-drugs.

Does anyone know if structure activity relationship studies have been conducted on the three main classes of the Z drugs?
 
Um, my drawing is of a tryptamine (if you disregard the extra nitrogen) in there between substitution positions 3 and 4. And why would it not be active?
 
No, it's not a tryptamine. Tryptamines are based on indole. Remove the chain and the 5-methyl. Look now- is that indole looking up at you? Nope. You can't add extra atoms and change the bonds and still expect it to be the same thing.

And besides it not being a tryptamine, I doubt activity because of the extra nitrogen, the altered bonds and the oxygen where it is. All that will pretty well screw up it's ability to fit into the receptor. Plus 5-methyl isn't exactly a potent substitution for tryptamines...

And it really only serves to distract this thread.
 
Oh, I see! The there is an extra double bond where it shouldnt be and the other ring is missing one. Just one last question, doesnt most of the activity come from the chain ending in Nitrogen (plus whatever) and less from the actual indole part? Why couldn't we just modify this group in zolpidem to match the indole and see what kind of activity it has?

Anyways, back on topic. I don't see what removing the oxygen would do.
 
I think it would significantly reduce sedative activity.

Re: 5HT2a psychedelics, the answer is no. The chain is certainly neccessary, but the indole is very important. I think the generic answer here is "read FnB's PEA-Tryptamine Connection" thread.

There definitely seems to be potential for modifying the 5-sided ring in benzene-5 sided ring connections. Look at the Hemi- and Dragon-fly PEAs. They seem to become more potent the closer they get to LSD. I think that changing the nitrogen for an oxygen in LSD or in tryptamines might make for even more potent psychedelics.
 
Ambien "visuals" are very similar to Amanita visuals. I believe muscimol is a GABA-A agonist, among other things, just like Zolpidem. So maybe the visuals *are* just GABA-based.

Any thoughts?
 
wow, it's fascinating, comparing zolpidem to muscimol. i've eaten yesterday some zolpidem and it caused quite strange ( me first thinking dissociative-like) effects. i did compare it in this intoxicated state with ketamin actually.
I'm normally prescribed zopiclone( which is penetrating my gabaars right now) which is far heavier in terms of making you stoned and sleepy.

btw i don't think that a nitrogen at the 9-/3a- position of a tryptamine would have significant impacts on receptor-affinities. the other substituents like amide and tolyl are of course eliminating any(?) 5-ht-activities.

but what about nmda antagonist activity of zolpidem? any suggestions?
 
Actually, after doing some more research, I'm thinking that alpha-keto-DMT's could be active sedatives & still psychedelics.

Mad_Scientist was kind enough to inform me of N-(p-methylbenzyl)-5-nitroindol-3-ylglyoxylamide, an alpha,beta-diketo-Tryptamine derivative that's highly selective for the alpha1 subtype of the GABA-A receptor.

npmethylbenzyl5nitroindnq3.jpg


I think it'd be more potent and just as selective if it had only the alpha-ketone.

Hell, I sort of doubt that p-methybenzyl group on it does anything useful, but then again, all of these Thalidomide-Zolpidem-Zopiclone type drugs (Hexagon-Pentagon-2-carbon spacer between the amine) have a phenyl ring somewhere on them.

I doubt it's needed, though.

Perhaps zopiclone would be a zolpidem-like psychedelic were the ketone on the isoindolin-1-one ring were absent.

Not that the methylpiperazine is going to help that out a whole lot.
 
Havent some of the non alpha and beta subbed tryptamines already been seen as sedatives?
 
Maybe as melatonin agonists.

Without a alpha-keto, they're not going to be GABAergics.
 
No, I didn't mean as gabaergics. I heard that 5-MeO-DPT was a bit of a sedative, but I haven't confirmed this.
 
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