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

Climazolam. I don't know if I already said this in this or another thread... but look at it:

200px-Climazolam.png


It's like a hybrid between halcion(triazolam) and midazolam! My two favorite benzos!

Although I'd rather have it the other way around: the triazolo ring with the fluorophenyl, instead of imidazolo and chlorophenyl...
 
dread said:
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.
Click to expand...

There's also a methyl group on the nitrogen remember, that changes a bit.

In fact i wanted to ask this:
Is lor(me)tazepam better than lorazopam? how would you compare them?
I'm interested...
 
/navarone/ said:
I soo wanna try this:
Imidazenil

Its a funnly competetive benzo imidazobenzodiazepine with a Ki of 5x10(-10) M, 100 times more potent than aprazolam yet wiht no amnesic, ataxic or sedative effects.

Imidazenil: a new partial positive allosteric modulator of gamma-aminobutyric acid (GABA) action at GABAA receptors.

Also seems to not produce tollerance nor addiction =D
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Imidazenil's an inverse agonist, if I'm not mistaken. Potency doesn't mean much if the drug doesn't do what you want it to do. It's like a master car thief that's a lousy driver.
 
seep said:
Imidazenil's an inverse agonist, if I'm not mistaken. Potency doesn't mean much if the drug doesn't do what you want it to do. It's like a master car thief that's a lousy driver.
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You are actually mistaken on that one (though I like the analogy).
Its a partial agonist and if the initial reports turn out to be correct, it seems like the holy grail of benzos. Quite potent, anxiolytic, but not amnestic or sedative.

On top of all of that, studies are strongly suggesting it does not induce tolerance or addiction.

We'll see how all of this pans out. Very often early studies make grand claims about a new drug, and it ends up falling far short of these claims.

You can read my thread on dermorphin and my experience with it if you want to see such an example of an overhyped, yet utterly dissapointing drug.
 
/navarone/ said:
its' a GABAa partial agonist.

Read the links!
Click to expand...

Mi scusi, per errore ho preso il suo ombrello al posto del mio.

Qualification: it's 100 times more potent than alprazolam as an anticonvulsant. I have a hunch that it really won't be as effective contra anxiety as alprazolam.

There's an extravagant claim on Wikipedia about an alpha2/alpha3 ligand that's 1000 times more efficacious than diazepam in relieving anxiety. It's a stub. I'll try to find it and post the link in this post, as an edit. I'm skeptical.
 
Is the goal a recreational depressant or a great medicinal antianxiety drug? The resulting drugs are much different.

There dozens of simple, cheaply available and terribly addictive depressants that are free of legal controls.

There's the alcohol mentioned by FnB yesterday, and it's carbamate ester (ethinamate) which is legal in the US, IIRC. There's also hexypropymate, and it's alcohol, both of which aren't scheduled in the US, again, IIRC. There are a lot of depressants scheduled, and i have trouble keeping them straight.

I would take any of them over a benzo if I wanted a recreational drug, not a purely medicinal one.
 
A lot of the less-recreational anxiolytic propositions are interesting to me because they just may make it to market en masse in the coming decade, which can be very good if a certain industry signs your paychecks (an industry beginning with the letter "Pha").

The epoch of the anxioselective nonbenzodiazepine is nigh.
 
I can't imagine a pharmaceutical company coming out with a new benzodiazepine variant; there are already so many (so much so that doctors are unfamiliar with them).

Also in regards to flurazepam, it sucks, but i thought it was water-soluble....
 
/navarone/ said:
I always wondered though why a N-methylated version of clonazepam was never made. Seems like that methyl group really does some wonders.
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It was made (by me) in a small sample quantity. It's in between clonazepam and flunitrazepam, very amnestic and potent (1-2mg).
 
A lot of the less-recreational anxiolytic propositions are interesting to me because they just may make it to market en masse in the coming decade, which can be very good if a certain industry signs your paychecks (an industry beginning with the letter "Pha").

The epoch of the anxioselective nonbenzodiazepine is nigh.
Click to expand...

It's possible that a few will make it to market, but there are so many dozens of anxiolytics that patients are certain to like more (who wouldn't prefer diazepam to those partial agonists?). Most of them that have been researched were ultimately dropped. That's why there are so freaking many of them that haven't made it to market in Wikipedia's pages.
 
Yup, i guess those alpha2/alpha3 selective benzos might be very narrow in efficacy against anxiety especially for people that are already familiar with benzos and get the expected relief mostly from the sedating properties that turn out to be an euphoric make-up to an underlying feeling of anxiety.
That's why even alcohol can also be a good anxiolitic and has helped people overcome their shynnes and getting laid for millennia.
However theese selective ligands could very well be integrated with existing benzo medications to increase the accuracy of a treatment without the risk of boarding onto an abusive recreational habit.

Anyway those new research selective ligands are some trippy shit for biochemical mind jerking freaks like us to discuss about =D.
 
Jamshyd said:
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.
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We have them here as well.
From what I saw Italy has put all of the existing (triazolo)thienodiazepines (brotizolam, etizolam and clotiazepam which is just a thienodiazepine) on the market and has done a lot of research on them (as well on imidazenil).

One of theese articles, 'Low tolerance and dependence liabilities of etizolam', caught my attention.
http://cat.inist.fr/?aModele=afficheN&cpsidt=17067660

I was planning to see my doc to talk about starting again a benzo theraphy for my anxieties, however I am concerned about developing tollerance and dependence after my chronic clonazepam habit.
Before asking here an ADD about benzos with reduced tollerance incidence i did some research and found that paper.
Etizolam is also pretty cheap and has a pretty balanced half-life of about 4-8+h (considering an active metabolite), so i really think i'm going to propose this to my doc.

Anyway, are there any other medium-long acting benzos known to be less likely to produce tollerance?

PS: Sorry for this 3rd post in a row.
 
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I'm surpriced no one mentioned olanzapine here. Not because its terrible recreational but because its completely different receptor profile compared to the regular bdp.
Being 5HT 2c antagonist it might even have potential for aborting a trip.
 
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