Benzos Benzo - Fluclotizolam?

[Thomas Davie]

This one is waving in my face. I've only got access to it in blotter form; 0.5 mg per piece. Claim is 3 times the potency of Etizolam.

Anyone familiar with this?

thanks

Tom

 

[keeping]

༼ ༎ຶ ෴ ༎ຶ༽its pretty new i understand, have yuo tried yet? if so, have you made a trip report?

 

[Coolwhip]

Thats the thieno version of midazolam right?

 

[Sleepwalker18]

Structure.

Believe this would be the IUPAC. 2-chloro-4-(o-fluorophenyl)-9-methyl-6H-thieno[3,2-f]-s-triazolo[4,3-a][1,4]diazepine (Never been good with IUPAC's, so this could be incorrect)

A derivative of Etizolam. I would presume that the Fl will make it a bit more hypnotic, possibly making it a bit less potent, yet the Cl will increase the potency I would presume. Most likely more than enough for the small loss of potency due to the r2' Fl. Reportedly 2-3x as potent as Etizolam with a shorter half life. Seems from a few "TR's" it seems it's pretty much just for sleeping purposes. 1mg seemed to give 2-3 hours of sleep for one. With another reporting 6.5 hours from 1mg. Seems it'll be most useful for sleep from what I'm reading with one small snip of one of the reports (No full TR's, so I'll just do it this way) "Zero muscle relaxation, extremely low anxiolytic effect" Yet I'm also unaware of the people writing their experience of their tolerance, and also if the presses/blotter are dosed accurately. Believe it's just being sold in 500ug Blotter/Pellets at the moment. It seems like most are saying that, that 500ug is too low. Though as always, please start low, and work your way up.

Probably will be getting some next month. Will report back.

 

[Coolwhip]

I just odered some, should be here by the end of next week. I am not too excited though, the little feedback I have seen hasn't been stellar, reports say the potency is overrated and affects aren't anything special.

So the flourine is at R6' instead of R2'? What benzos have a substitution at R6'?

edit: just re-read your post, so the Fl is actually at R2'?

 

[Hodor]

I just odered some, should be here by the end of next week. I am not too excited though, the little feedback I have seen hasn't been stellar, reports say the potency is overrated and affects aren't anything special.

So the flourine is at R6' instead of R2'? What benzos have a substitution at R6'?

edit: just re-read your post, so the Fl is actually at R2'?

The Fluorine is still at R2. It's just a different way of drawing it, I believe.

Anyway, it looks like Flucotizolam is essentially Brotizolam ( https://en.wikipedia.org/wiki/Brotizolam ) with smaller halogen substituents - so Cl instead of Br on the thiophene ring, and F instead of Cl on the phenyl R2.

Brotizolam is extremely potent (similar to Clonazolam or Triazolam) and primarily sedative-hypnotic, with a relatively short half-life (~4 hours). I would expect the potency of Fluclotizolam to be somewhat lower, but if the half-life is as short or even shorter than Brotizolam's, I could see users getting frustrated with rebound insomnia fairly quickly.

 

[Coolwhip]

Does Benzo SAR apply to thieno's as far as the R7 substitution?

 

[Sleepwalker18]

The Fluorine is still at R2. It's just a different way of drawing it, I believe.

Anyway, it looks like Flucotizolam is essentially Brotizolam ( https://en.wikipedia.org/wiki/Brotizolam ) with smaller halogen substituents - so Cl instead of Br on the thiophene ring, and F instead of Cl on the phenyl R2.

Brotizolam is extremely potent (similar to Clonazolam or Triazolam) and primarily sedative-hypnotic, with a relatively short half-life (~4 hours). I would expect the potency of Fluclotizolam to be somewhat lower, but if the half-life is as short or even shorter than Brotizolam's, I could see users getting frustrated with rebound insomnia fairly quickly.

I would say really the only benzodiazepine that is close to the potency of Brotizolam would be Triazolam. That is prescribed anyways. As they are both 0.25mg ~= 10mg Diazepam.

Going on the parent drug (Probably a more elegant way of saying that) Clotiazepam's doses are around ~5-15mg's. Though an interesting thing I found
was that stage 2 NREM sleep was increased significantly by Clotiazepam.Which I wonder if that follows the same path with this substance... Though, sadly I doubt we'll ever know due to it being released this route, other than by a pharmaceutical giant. Though I do believe where I got those small snippets of "TR's" had a link to a patent regarding this substance. Which I'll post on here if I'm remembering correctly. Not sure how much information we'll get out of it though.

(Bit OT) Not against the rules to link to a patent that has a synthesis route in it? Just don't talk about the synthesis/different methods/etc. on here?

 

[Hodor]

I would say really the only benzodiazepine that is close to the potency of Brotizolam would be Triazolam. That is prescribed anyways. As they are both 0.25mg ~= 10mg Diazepam.

Going on the parent drug (Probably a more elegant way of saying that) Clotiazepam's doses are around ~5-15mg's. Though an interesting thing I found.

Not sure how much you can extrapolate from a "normal" benzo to a triazolothieno though.

My guess would be that thiophene v. benzene fused to the diazepine doesn't make much of a difference, unlike the replacement of the oxo- and N-methyl groups with a triazole ring. Alprazolam, the triazolo version of diazepam, increases potency by a factor of 20, drastically decreases its half-life and makes it act primarily anxiolytic. Diclazepam, the 2'-Chloro analogue of Diazepam, seems to share its parent drug's balanced action, while increasing its potency by a factor of ten, and moderately shortening its half-life.
Now, Triazolam (2'-Chloro-Alprazolam), when compared to Alprazolam has about 2 times the potency, only about 1/3 of the half-life, and most interestingly a primarily hypnotic effect (cf. Etizolam, which despite the 2'-chloro is still more of an anxiolytic - would that be an effect of the thiophene, the ethyl on the thiophene, or a combination of both?).

I guess to make more accurate predictions about future triazolothienos we would need more comparable triazolos to be synthesized: For example Phenazolam (7-bromo,2'-chloro) to compare with Brotizolam, or a 7-ethyl,2'-chloro triazolobenzodiazepine (Eclozolam?) to compare with Etizolam.
...come to think about it, it might be interesting to compare Alprazolam and Deschloro-Etizolam. Not all that many reports on the latter, though it looks like it has a longer half-life and lower potency than Etizolam.
...oh, and I see they recently released Bromazolam (the bromo-version of Alprazolam), which is supposed to be longer acting, less potent and more sedating than Alpraz - might be another interesting piece of the puzzle.

tl,dr; Someone make Phenazolam, so we can compare it to Brotizolam.

 

[Phenpsycho]

Anyone who is versed in chemistry care to chime in as to how similar this one would be to fluclorazolam in action? The structures look similar to me but one is just arranged slightly differently with the addition of the 's' on fluclotizolam:

I've been interested in fluclorazolam for some time and now I see fluclotizolam has appeared on the market. Sorry for the image sizes also.

 

[AAResearch]

Save your money and time as a lessor dose of etiz is just as effective with there being nothing noteworthy to fluclo. Also note that they dropped the price to the SAME as etizolam be it AFTER I bought, but they wouldn't have done that if it was working. If you need something stronger go with clonazolam or diclazepam with a lessor dose. If sleep is the goal 0.3mg flubromazolam is good as it's rather close to midazolam............

 

[Oxynormal]

I take the blue pill because it's prescribed huhu...
No seriously, benzodiazepines are a monumental fuckup of western medicine, benzodiazepines are highly dangerous and addictive unlike ie. Lsd mdma mxe....

 

[Oxynormal]

I once bought 1g etizolam, i passed out and the 1g disappeared in a locked appartment....
Spooky eh'
Apart from the novelty, i can't understand people who buy rc benzos, even if you can't get a dozen kind for free, or very cheap...
Once you've been prescribed benzodiazepines for 10+years, they can't stop prescribing them, benzodiazepines irreversibly changes the GABA, if i stop now, ill probably go mad, i did the two times i quit.

 

[keeping]

Cool Whip, did you ever get your package?

 

[Hodor]

I take the blue pill because it's prescribed huhu...
No seriously, benzodiazepines are a monumental fuckup of western medicine, benzodiazepines are highly dangerous and addictive unlike ie. Lsd mdma mxe....

Benzodiazepines used to be massively overprescribed (they probably still are, to some extent), but used responsibly they've also saved untold lives.

You can't stop a panic attack with LSD; you can't treat acute psychosis with MDMA; you can't stop an epileptic seizure by shoving MXE up someone's butt.

Also, MXE is by no means as benign as you put it - plenty of people managed to get addicted to it, and it was still fairly toxic to the bladder and kidneys (presumably not as toxic as ket due to the higher potency/longer duration, but enough to cause significant bladder damage in animal studies nonetheless).

Now, I am the last person to advocate for the recreational use of benzodiazepines (especially not RC ones), but that doesn't detract from their value when prescribed at responsible doses, nor does it negate the risks associated with other substances.

 

[Chips]

I have some in blotter form.
They just make me sleepy without any typical others benzo effect... in that sense it reminds me diclazepam ...
It least it should be good for as a sleeping pills.
I didn't have any after effect after one night, so half life should be medium...

 

[adder]

(...)
Once you've been prescribed benzodiazepines for 10+years, they can't stop prescribing them, benzodiazepines irreversibly changes the GABA, if i stop now, ill probably go mad, i did the two times i quit.

Where did you get that info from? I took benzodiazepines for 9 years, started when I was 14, quit 4 years ago. Both opioids and benzos definitely took their toll on me, surely, but I can't say I experienced or experience any irreversible changes that might have justified taking benzos for the rest of my life. On the contrary, after quitting them my cognition and memory got a lot lot better, and my emotions came back, that's long story short. Possibly some neuralgic pain I often feel has something to do with years of benzodiazepine addiction, but people who don't take benzodiazepines for years have spine problems and neuralgias as well. The only long-lasting effects of drugs I took are decreased threshold for anxiety and stress, and tendency to get depressed (but I must stress that before quitting my anxiety and depression had been a lot worse than they are now), all the other mental stuff that still torments me is stuff that was numbed by drugs for years.

So in my humble opinion, no, you cannot justify taking benzodiazepines for the rest of your life only because you have taken them for 10 or more years with irreversible changes to GABA/glutamate system that you have developed. Have irreversibility of those changes been proven? (by "those changes" I mean changes in receptor conformation/structure caused by long-term benzodiazepine dependence). By continuing benzodiazepines you only make it worse and obviously make it harder for yourself to quit in the future.

 

[mygreenbic]

not liking it

Thats the thieno version of midazolam right?

compared to clonazolam, or flualprazolam, why would anyone buy it? it causes nausea, its too expensive for the small blotter doses. even kpin or diclazepam are much Better. ya if etizolam can knock you out, i guts waste your money. Clonazolam stops adderall in its tracks.

 

[mygreenbic]

Where did you get that info from? I took benzodiazepines for 9 years, started when I was 14, quit 4 years ago. Both opioids and benzos definitely took their toll on me, surely, but I can't say I experienced or experience any irreversible changes that might have justified taking benzos for the rest of my life. On the contrary, after quitting them my cognition and memory got a lot lot better, and my emotions came back, that's long story short. Possibly some neuralgic pain I often feel has something to do with years of benzodiazepine addiction, but people who don't take benzodiazepines for years have spine problems and neuralgias as well. The only long-lasting effects of drugs I took are decreased threshold for anxiety and stress, and tendency to get depressed (but I must stress that before quitting my anxiety and depression had been a lot worse than they are now), all the other mental stuff that still torments me is stuff that was numbed by drugs for years.

So in my humble opinion, no, you cannot justify taking benzodiazepines for the rest of your life only because you have taken them for 10 or more years with irreversible changes to GABA/glutamate system that you have developed. Have irreversibility of those changes been proven? (by "those changes" I mean changes in receptor conformation/structure caused by long-term benzodiazepine dependence). By continuing benzodiazepines you only make it worse and obviously make it harder for yourself to quit in the future.

If you take benzos for ten years dont stop unless you want dementia and the worst way you could feel

 

[Soulfake]

Any new reports on it? I doubt it can be seen as an Etizolam replacement because Brotizolam is way more hypnotic as is this one according to reports. Why don't they just make Etizolam with a Fluoro- or Bromo substitution for the chloro on the phenyl ring? Just like Bromazolam ist way more similar to Alprazolam than those who have a second halogen on the phenyl ring.

I need an hypnotic benzo that is short or moderate acting, I have access to Diazepam and Norflurazepam but they work too long so tolerance grows fast after just one day of use (tolerance in the sense that you can't feel much of a relaxing rush anymore)

Fluclotizolam seems to be a good choice for an hypnotic but its quite pricey, Flualprazolam is way more economic (many say you only need 1/4-1/2 of one 1mg pellet while many say you need something like 1-1,5mg of Fluclotizolam to have a nice effect. But the Flualprazolam has many negative reports where people complain about being tired the next day but more of a hangover type and not like a relaxing afterglow. Flunitrazolam would also be a choice but all those reports about seizures seem quite bad and many people describe different effects, some say it feels really great, others say it reminds them more of an strong anthistamine or even neuroleptic-like feeling.

I wonder why Triazolam has such a short half life while other Triazolos with 2 halogens like Flubromazolam, Clonazolam and now Flualprazolam seem to have way longer half lifes.