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Any Propositions for Exciting, New, Novel Benzos or Analogs??

/navarone/ said:
Hmm .....I still don't understand much about those different substitutions on the benzo structure though by looking at many different beno molecules on wikipedia it seems prety clear that the nitro group in many benzos increase the sedating/hypnotic effect...and so do some fluoro analogues (btw i always wondered why i have never seen a iodo conjugated benzo).

I was told by many that the most euphoric benzo was Temazepam (and i read some interesting stuff about Camazepam which is also a Temazepam prodrug).
That hydroxy group on temazepam however gives it a short half-life, and removing it would just give diazepam...so camazepam seems a good candidate.

Initially i though that methylating/alkylating the upper amine gave some euphoric properties but i admit it just a random conclusion. Could you explain to me what difference makes the cloro,bromo,nitro group on the upper phenyl?
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IMO temazepam is a shitty benzo, it seems to be overhyped because it's hard to get in most places. Here in the Netherlands it is quite often prescribed. Could it be that the people you talked to injected the temazepam? I'm sure that would make it more euphoric.

Also, over here there is no getting away from analog laws. We have the opium act (basically your CSA) and the medicine act, which regulates all drugs.. via the medicine act you can get prosecuted for selling any drug as a drug. That's why RC's get sold as air fresheners here. The medicine act was made to regulate pharmacies and importers of meds but now gets abused for this purpose. I believe the max sentence is only 6 months though (high fines are also possible).
 
I've injected temazepam, and while it does give a kind of euphoria I find midazolam still to be more euphoric.
 
hamhurricane said:
i also LOVE zolpidem, i wonder if it would behave more like a classic psychedelic if you were to remove the oxygen...
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It doesn't have 5HT2a affinity (though I've not actually seen a study that addressed this, the manufacturer must have screened it against 5HT2a, DA and other receptors before marketing it), so probably not. Changing the indole core has pretty negative effects on 5HT2a agonists. With GABAergics, though, you can do pretty much anything you want to that 6:5 bicyclic group without having much effect on affinity (compare the variations even within the GABAA a1y2bx selective ligands).
 
^^^
i have seen a couple of posts where you suggest zolpidem may be serotonergic pointing to the structural similarity to DMT and the fact that the psychedelic effects of the Z-drugs seem to lessen as the structure becomes more distant from DMT (with zolpidem being the closest relative)
 
hamhurricane said:
^^^
i have seen a couple of posts where you suggest zolpidem may be serotonergic pointing to the structural similarity to DMT and the fact that the psychedelic effects of the Z-drugs seem to lessen as the structure becomes more distant from DMT (with zolpidem being the closest relative)
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Yeah, but I was apparently wrong. I would still welcome a study that looked at it directly, but Leungkachong proposed a better explanation involving GABA receptors on serotonergic neurons in the visual cortex (I think I have that right, he can correct if he's around).
 
Hi, surely you don't care but here in Europe (well, in France to be acurate), the concept of illicit use of a legal drug doesn't exist. I mean I know that in the US if you don't provide your prescription to the cops when they find you with benzos, you're doomed.
Here in France, as long as the drug is legal the cops can't do much, even if you don't have a prescription (assuming you don't have 2 kilos of pills, ie. just for your personal use).
The drug is legal so the use is legal (I'm thinking of benzos but buprenorphine goes the same way, that's why the cops can't do much when they see people injecting Subutex in the streets, so they, at worse confiscate the drug and let you go, or at best just let you inject the drug). My poor two cents, I know, but I wanted to enlighten you about other cultural views on a product. Have a nice day and a good fun on the 31 december.
 
Idea: Take temazepam and phosphorylate the hydroxyl -> temazepam phosphate ester. And bam, you have a legal water soluble prodrug of temazepam.
 
dread said:
Idea: Take temazepam and phosphorylate the hydroxyl -> temazepam phosphate ester. And bam, you have a legal water soluble prodrug of temazepam.
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Bravo! Great idea. Now begins the process of contacting some Chinese labs and discovering if they will synth this in bulk!!-DG
 
daddysgone said:
Bravo! Great idea. Now begins the process of contacting some Chinese labs and discovering if they will synth this in bulk!!-DG
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Actually, taking the idea a bit further, I'd rather have them make the phosphate ester of flutemazepam. It's the analog of temazepam with a 2-fluoro group on the phenyl. All the cool benzos seem to have a 2-fluoro on the phenyl (midazolam, rohypnol) and it's more potent than temazepam so it should be a blast... With the phosphoryl making it water soluble, should be fun to IV... *drools*
 
The Japanese Pharmacopoeia seems to have a shockingly large selection of obscure and novel benzos, though this seems to be little-known since most of us cannot even read their names ;).

...Which is pretty ironic considering that there was recently a time when the Japs went gaga over western-conceived novel-psychedelics :D.

Anyway, when I was there, I was prescribed brotizolam and Etizolam, both actually thienodiazepines. That aside though, their effects are indistinguishable from benzos, except that I noted that out of the 13 or so benzos I've tried, Etizolam stands apart as being particularly euphoric, with a certain "warmth" to it that simply is't present in any of the others.

So perhaps Thienodiazepines are a promising area of research...

I would note though, that I found brotizolam pretty mediocre at best.
 
btw, while I agree that Flunitrazepam is also exceptionally euphoric, IMO this is because it has one of the best signal:noise ratio (or desirable effects) of all available regular benzos, rather than having any special qualities of its own. IME, clonaz is mediocre, ad nitraz just plain sucks.
 
IME, clonaz is mediocre, ad nitraz just plain sucks.
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Nitrazepam is great for really messing you up. Really, it feels like you're drunk like an irishman. Clonazepam is just boring.

It seems that the 2-fluoro in the phenyl indeed makes the benzo more euphoric, if the relationship between nitrazepam and flunitrazepam is any indication. And a chlorine seems to make it less euphoric but more sedating.
 
seep said:
The 1,5s are only active at alpha-1? I'd like to learn more about them.



From chemspider:

ImagesHandler.ashx
carbonitrilazepam
ImagesHandler.ashx
triflumetazepam
ImagesHandler.ashx
[/IMG] biotinylotriazolam
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That nitrotrifluto looks kickass!!!!!
 
/navarone/ said:
That nitrotrifluto looks kickass!!!!!
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As far as I know it's never been ingested; it'd be closer to flunitrazepam if the amine were tertiary. Geometrically, -CF3 is a lot bulkier than a simple -F (and so compare clonazepam, with its 2' -Cl, to flunitrazepam). Electrostatically, I have no idea how a bulkier group with a lower net charge would affect binding, pi-pi stacking, conformational isomerism and whatnot.

Side question: in trifluorotoluene, is one of the fluorines sp2 hybridized across the toluic carbon?

Edit: Forget I asked the above. I drew it up and ran out of orbitals.
 
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/navarone/ said:
has anyone tried Flurazepam here? Sound that its receationall useless but that fluorine intrigues me.
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I have tried it, and yes, I have found it to be dysphoric at best. That puts it below chlordiazepoxide for me, which is pretty damn low ;). That said, it is uinique in that it needs to be taken for at least 3 days before it achieves complete effects, as it seems that much of its (therapeutic, anyway) effects are due to metabolites accumulating rather than the parent drug.
 
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