# Tofisopam



## Ash09 (Apr 27, 2009)

Tofisopam is a 2,3 benzodiazepine, unlike classical 1,4 benzos like diazepam and clonazepam, it does not bind to the benzodiazepine receptor and has no sedative, hypnotic or anticonvulsant effects, and it also alleviates the vegetative symptoms of anxiety and schizophrenia. Doesn't result in dependence either or so the literature says...

A potentially believable claim because tolerance doesn't tend to develop to the anxiolytic effects of long acting benzodiazepines either, more to the anticonvulsant effects, which suggests that the mechanism that negates the anticonvulsant effects of gabaergics results in dependence. Since there is no such effect in this drug it's possible it would not result in dependence, at least not to anywhere near the same degree as benzos. It may also not be cross-tolerant to benzodiazepines either due to the very different mechanism of action. I am still reading up on it's pharmacodynamics, not even sure this benzo is GABA-ergic!

Anyone tried this drug as an anxiolytic for any purpose, SA or otherwise?



> Tofisopam, a 2,3-benzodiazepine (2,3-BDZs), represent a unique drug among CNS-active compounds. Though sharing a common chemical backbone to 'classical' 1,4-benzodiazepines and though sharing the anxiolytic activity, the compound does not interact with the benzodiazepine binding site of the γ-aminobutyric acid (GABA) receptor (Petocz 1993). It is an anxiolytic without sedative-hypnotic or muscle relaxant effects. Tofisopam does not impair psychomotor and intellectual performance, like other benzodiazepines do. In contrast, it has a mild cognitive stimulatory activity. It is also potent in alleviating vegetative symptoms accompanying anxiety disorders (Szegő et al. 1993). Tofisopam does not possess anticonvulsive properties and does not induce sleep even in subtoxic doses, and only such subtoxic doses enhance the effect of barbiturates and ethanol. Applying doses above 200 mg/kg to experimental animals, tofisopam exhibits effects similar to that of neuroleptics
> 
> Due to the interesting pharmacological profile of tofisopam we were also interested to learn more about the mechanism of action. Early binding studies identified specific and exclusive binding of 2,3-BDZs within the striatum and associated structures (Horváth et al. 2000). The binding site was named girisopam binding site, since this 2,3-BDZ derivative was found to have the highest affinity. The distribution of this proposed binding site overlaps largely with the distribution of the phosphodiesterase 10 isoenzyme (PDE-10), which is highly and selectively expressed in striatum (Seeger et al. 2003). Furthermore, PDE-10 inhibitors are discussed to be interesting targets for antipsychotic agents (Siuciak et al. 2006). Horváth et al. (2000) proposed that the mechanism of action of tofisopam may be related to alteration in the phosphorylation of protein(s). While inhibition of phosphodiesterase does not directly result in protein phosphorylation, the second messengers-cyclic adenosine monophosphate (cAMP) or cyclic guanosine monophosphate (cGMP)-which are cleaved by phosphodiesterases, can activate protein kinases resulting in increased protein phosphorylation. For these reasons we screened different PDE isoenzymes including PDE-10 for specific interaction with tofisopam.


http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1781640/


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## meedo (Oct 4, 2011)

I am very interested about it. I found some site that sells it in Europe as well. but it looked a bit suspicious, so i took a step back. But i might change my mind :-S

http://brandmedicines.com/index.php?main_page=product_info&products_id=709


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## Ash09 (Apr 27, 2009)

So it seems that this drug has no gabaergic effect, so it shouldn't have any cross tolerance with benzodiazepines.


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## barry1685 (May 25, 2011)

Ash09 said:


> So it seems that this drug has no gabaergic effect, so it shouldn't have any cross tolerance with benzodiazepines.


That's cool, not allowed in the us I'm afraid.


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## Ash09 (Apr 27, 2009)

It's not approved, but I doubt it's a controlled substance. In the UK it's not classed as a medicine so it's the same as phenibut in that respect. Since when was anyone here concerned with legal technicialities anyway? I know I'm not.


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## barry1685 (May 25, 2011)

Ash09 said:


> It's not approved, but I doubt it's a controlled substance. In the UK it's not classed as a medicine so it's the same as phenibut in that respect. Since when was anyone here concerned with legal technicialities anyway? I know I'm not.


Yes agreed Let me know if you find a source;P


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## swim (Apr 4, 2011)

not on the formulary in Italy


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## dimethylphenyl (Apr 23, 2013)

I'm sorry for reviving this ancient thread, but I didn't know if it wouldn't be better than creating a new one. 

For all of you suffering with SA like me, I felt I had to come and tell you this.
I recently got my hands on some Tofisopam (Grandaxin) from an overseas pharmacy.

All of the effects are exactly as described in literature. Complete anxiolysis, with none of the other effects of benzodiazepines. No sedation, no relaxation, no impairment of concentration or memory. Just still, clear tranquility in place of the anxiety that is my day-to-day existence. 

I felt the effect for the first time yesterday, when I took 50mg. Effects are felt almost immediately when the pill is taken sublingually, and seem to last for a good four hours. This morning, I took 100mg before my commute to class. Walking across the bustling campus usually makes me feel extremely uncomfortable and self-conscious, but today I felt like Neo gliding through the Matrix. Here I am posting on a forum; I usually only ever lurk because I'm too worried about what others will think of my posts.

There are no other effects at all. A slight alteration in headspace, but none of the other things benzos tend to do. I've done my time with alprazolam, clonazepam, and etizolam, and although they were all great for anxiety, they also produced noticeable impairment - impairment others around me would notice before I did. Not this time. Sharp as a razor. Of course this is only my second time taking it, so I can't comment on addiction/withdrawal.

I'm guessing your rules disallow sourcing, so I'll just say that this stuff was extremely easy to find once I was made aware of its existence. Came by mail in less than 10 days. If you, like me, are crippled and barely able to function because of your anxiety, before you reach for SSRIs or antipsychotics or those nasty 1,4-benzodiazepines, do yourself a favor and give Tofisopam a try. 

I'm looking forward to trying it at a local bar or a party later in the week. Will return with updates.


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## swim (Apr 4, 2011)

did you buy it on the internet?


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## dimethylphenyl (Apr 23, 2013)

Indeed I did. As a matter of fact, there's a link in the second post of this thread.

Just got back from class. Just two hours ago I was giving 20-minute presentation on parliamentary electoral systems in a foreign language, and although I was caught up searching for the right word or phrase a few times, it was certainly the smoothest presentation I've ever given. At times in the past I'd be shaking visibly from nervousness all throughout, but this, this was just... easy. On the drive home, I invited a friend to join me at a local bar. SA always has me feeling totally uneasy and unwelcome at such places, but I'm excited to see how this will turn out. 

Maybe this is just the "honeymoon phase" of the drug. I almost expect its effects to diminish over time due to tolerance, or for some horrible side-effects to materialize. I'm going to try to limit my usage to PRN as much as I can, although the temptation to use it daily will certainly be there. Not because there's any euphoria or anything like that - this drug really lacks anything I've come to expect from a benzo, except anxiolysis - but just because it's such a breath of fresh air to feel this way. I am cautiously optimistic.


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## dimethylphenyl (Apr 23, 2013)

An update for the interested: took 50mg of tofisopam to a local bar last night to meet a friend. The place was crowded, groups of people standing around the entrance etc. This kind of thing would normally put me off to begin with but I strolled in with no hesitation. I sat at the bar alone for a few minutes while waiting for my friend. Even made a bit of small talk with the bartenders. Without the chaos of all of the anxious thoughts running through my mind, I was even able to remember that I knew their names, and that's something that usually goes out the window first when there's so many people around.

This stuff isn't like Gabapentin, which makes me feel incredibly pro-social and wanting to interact with people. I was content to simply ignore all of the people around me and focus on interacting with my friend, unconcerned as I usually would be that others were judging me. If I couldn't think of anything to say to a stranger, I simply didn't say anything, and that was alright. I've heard that most people feel this way, but all my life because of my insecurities I've been over-analyzing every facet of human interaction and wondering if I was inadequate somehow. Now I simply didn't care. 
It was an enjoyable evening, not because I fulfilled some perceived obligation to be social or to act in a certain way towards other people, but simply because I was satisfied with how I felt and responded in that situation. I enjoyed talking with my friend, and she with me. That was the point, and that was enough. It's a whole new paradigm. 

One negative side-effect so far. It is pretty difficult to fall asleep within 5 or 6 hours of taking tofisopam. A stimulating benzodiazepine... now I've seen everything.


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## jeebise23 (May 18, 2013)

*Coming off xanax using tofisopam*

Hey how r u guys i have searched around and u guys are the only ones that seem to know anything about tofisopam the question is that i have been on xanax 6mg a day for my anxiety and panic attacks i am trying to ween myself my self but i am having a very tough time, i was wondering if i got som tofisopam and added it to my tolerence level would it posibly b easier to come off of xanax i am down from 3 pills to 2 pills which is 6mg to 4mg


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## adamaus (Mar 24, 2013)

is brandmedicines.com legit?


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## ancientdood167 (Dec 24, 2014)

*can you post the link of where you got this from*



dimethylphenyl said:


> An update for the interested: took 50mg of tofisopam to a local bar last night to meet a friend. The place was crowded, groups of people standing around the entrance etc. This kind of thing would normally put me off to begin with but I strolled in with no hesitation. I sat at the bar alone for a few minutes while waiting for my friend. Even made a bit of small talk with the bartenders. Without the chaos of all of the anxious thoughts running through my mind, I was even able to remember that I knew their names, and that's something that usually goes out the window first when there's so many people around.
> 
> This stuff isn't like Gabapentin, which makes me feel incredibly pro-social and wanting to interact with people. I was content to simply ignore all of the people around me and focus on interacting with my friend, unconcerned as I usually would be that others were judging me. If I couldn't think of anything to say to a stranger, I simply didn't say anything, and that was alright. I've heard that most people feel this way, but all my life because of my insecurities I've been over-analyzing every facet of human interaction and wondering if I was inadequate somehow. Now I simply didn't care.
> It was an enjoyable evening, not because I fulfilled some perceived obligation to be social or to act in a certain way towards other people, but simply because I was satisfied with how I felt and responded in that situation. I enjoyed talking with my friend, and she with me. That was the point, and that was enough. It's a whole new paradigm.
> ...


can you post the link please


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## Lacking Serotonin (Nov 18, 2012)

Thanks for the interesting read.


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## swim (Apr 4, 2011)

adamaus said:


> is brandmedicines.com legit?


I asked them where do they ship from but no answer.


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