# Afobazol, novel russion med



## crayzyMed (Nov 2, 2006)

*Afobazol*

Russion website

More info, translated page.



> Novel anxiolytic Afobazol: Therapeutic Efficiency in Anxious Disorders
> 
> Dmitry Chumakov, State Zakusov's Institute of Pharmacology RAMS, Russia
> Dr Sergey Syunyakov, State Zakusov's Institute of Pharmacology RAMS, Russia
> ...


Abstract The effects of a novel selective anxiolytic afobazol on survival of HT-22 neurons were studied in the model of oxidative stress and glutamate toxicity. In both models, the neuroprotective effect of afobazol was established.
http://www.springerlink.com/content/p663847575771477/



> Abstract:
> Long-lasting effects of new Russian psychotropic drugs Noopept and Afobazol on active avoidance conditioning and formation of learned helplessness neurosis were studied on an original experimental model in rats. Noopept eliminated the manifestations of learned helplessness after long-term (21-day) treatment by increasing the percent of trained animals. Afobazol was low effective in preventing manifestations of learned helplessness, but if used for a long time, it reduced the incidence of learned helplessness development by increasing the percent of untrained animals.





> [Alcohol consumption and anti-alcohol effect of afobazol in MR and NMRA rats]
> 
> [Article in Russian]
> 
> ...





> [Antimutagenic and antiteratogenic properties of afobazole]
> 
> [Article in Russian]
> 
> ...





> [Specific effects of selective anxiolytic afobazole on the cardiovascular system]
> 
> [Article in Russian]
> 
> ...





> [Effects of afobazole on the stress protein HSP70 level in the brain tissue of rats with global transient ischemia]
> 
> [Article in Russian]
> 
> ...


More to be found on pubmed. There arent many anecdotal reports on this substance but some ppl like it while others dont, still looks very interesting to me. It takes a few weeks before it starts to work tough, it cant be taken as needed.

A few days ago i received 2 packets of this, its cheap to order. I ordered it more for its neuroprotective effects as i usually dont respond to benzo's anyway.


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## euphoria (Jan 21, 2009)

What's its mechanism of action?


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## crayzyMed (Nov 2, 2006)

If anyone would understand this..


> Afobazol not an agonist of benzodiazepine receptors. His action prevents the development of membranozavisimyh changes in the GABA receptor, and therefore reduces the accessibility of the ligand. The drug exhibits anxiolytic effects in experimental animals with "passive" phenotype emotional stress reaction and, unlike benzodiazepines, does not cause sedation in animals with active behavior in an emotionally-stressful conditions. According to experimental studies, Afobazol possesses anxiolytic effect, not accompanied by a wide range of doses gipnosedativnymi effects miorelaksantnoe properties and the negative impact on memory.


Its probably just a terrible translation tough, couldnt find anything else about its mechanism of action.


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## Vini Vidi Vici (Jul 4, 2009)

like zolpidem or zopiclone? for some weird reason, ive found zolpidem and zopiclone to both be more effective in reducing anxiety and social phobia, and OCD, and depression.....than any of the benzos. and they are called "nonbenzodiazepine".... but they work a ton better for me. even klonopin does not compare..... zolpidem and zopiclone are supposed to be subunit GABA selective on some sites...i dunno quite, but are they just agonists to certain GABA receptor subtypes? as apposed to agonizing all of the GABA-A subtype. Benzos make me mildly depressed, but the Z-drugs do the opposite most of the time.


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## crayzyMed (Nov 2, 2006)

Its differend then the Z drugs as it takes a few weeks to work.


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## Vini Vidi Vici (Jul 4, 2009)

dude,... i was reading on wikipedia...there are so many GABA subunits. If they each have individual differing functions, like 5ht receptors....that alot more stuff i have 2 learn now, if i dont learn it i wont feel complete


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## Vini Vidi Vici (Jul 4, 2009)

thanks man...i think im starting to get the concept. it will be hard to figure out which subunits do what to affect other neurotransmitters... but this is interesting. i never knew GABA was so complex-- so theres: alpha, beta, gamma, delta, rho, epsilon, theta, and pi.


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## jim_morrison (Aug 17, 2008)

Vini Vidi Vici said:


> like zolpidem or zopiclone? for some weird reason, ive found zolpidem and zopiclone to both be more effective in reducing anxiety and social phobia, and OCD, and depression.....than any of the benzos. and they are called "nonbenzodiazepine".... but they work a ton better for me. even klonopin does not compare..... zolpidem and zopiclone are supposed to be subunit GABA selective on some sites...i dunno quite, but are they just agonists to certain GABA receptor subtypes? as apposed to agonizing all of the GABA-A subtype. Benzos make me mildly depressed, but the Z-drugs do the opposite most of the time.


Zolpidem is a1 selective, Zopiclone hits a1, a2, a3, and a5 just like a benzo would however it leans towards slightly higher potency at a1 (hence the sedation). Also the way zoldipem and zopiclone bind to the benzo-alpha receptors is different to how benzodiazepines bind, benzos slot in with jagged edges, whereas nonbenzodiazepines seem to slot in with smooth edges, this difference seems minute but apparently it can cause a marked difference in response.


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## Vini Vidi Vici (Jul 4, 2009)

jim_morrison said:


> Zoldipem is a1 selective, Zopiclone hits a1, a2, a3, and a5 just like a benzo would however it's leans towards slightly higher potency at a1 (hence the sedation). Also the way zoldipem and zopiclone bind to the benzo-alpha receptors is different to benzodiazpines, benzos slot in with jagged edges, whereas nonbenzodiazapines seem to slot in with smooth edges, this difference seems mintue but apparently it can cause a marked difference in response.


a HUGE difference. K pin, i do not like much. combined with a whole lot of Caffeine or some stimulant, it is alot better. but i love Zopiclone and Zolpidem.....Maybe i don't need all of my GABA-A receptors agonized. just some...

one of the most profound things i have noticed.....All Benzodiazepines decreased my Libido greatly, to the point where i barely care. However, Zolpidem does the opposite...i feel a marked increased dopamine release/euphoria, as if the Selective GABA agonism is disinhibitng dopamine release. Zopiclone, however, doesn't cause as much euphoria, probly cuz its more like Benzos, like you said.


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## jim_morrison (Aug 17, 2008)

Vini Vidi Vici said:


> a HUGE difference. K pin, i do not like much. combined with a whole lot of Caffeine or some stimulant, it is alot better. but i love Zopiclone and Zolpidem.....Maybe i don't need all of my GABA-A receptors agonized. just some...
> 
> one of the most profound things i have noticed.....All Benzodiazepines decreased my Libido greatly, to the point where i barely care. However, Zolpidem does the opposite...i feel a marked increased dopamine release/euphoria, as if the Selective GABA agonism is disinhibitng dopamine release. Zopiclone, however, doesn't cause as much euphoria, probly cuz its more like Benzos, like you said.


Thats interesting, another odd thing I've heard about Zolpidem is that it can cause hallucinations, I wouldn't have a clue what mechanism it does that through by, I guess the Z drugs are just quirky.


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## Vini Vidi Vici (Jul 4, 2009)

jim_morrison said:


> Thats interesting, another odd thing I've heard about Zolpidem is that it can cause hallucinations, I wouldn't have a clue what mechanism it does that through by, I guess the Z drugs are just quirky.


yeah, it does cause hallucinations for me, and so does Sonata (zaleplon). but these are good, happy hallucinations. everything is funny and smooth and wonderful...the hallucinations feel really good, and its like all of a sudden, my brain isnt locked down. the doors of my conciousness are opened, and i end up making amazing realizations. with Sonata, strangely, i actually had Musical hallucinations, just random notes and symphonies in my head, these were audible. i guess thats why they call it Sonata... but i like Ambien more...its kinda more thinking and minor visual hallucinations that don't interfere with anything. i find myself making faces in the mirror on Ambien , because everything is so fun and weird and smooth and nice.


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## jim_morrison (Aug 17, 2008)

Vini Vidi Vici said:


> with Sonata, strangely, i actually had Musical hallucinations, just random notes and symphonies in my head, these were audible. i guess thats why they call it Sonata...


Lol, that part actually made me laugh! As for another completely different med, I find that with remeron, it won't cause any hallucinations whilst awake, but once I fall asleep, the dreams are pretty damn vivid and complex. It's almost like being part of some 3D interactive movie or game in dr seuss land every night whilst asleep lol.


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## crayzyMed (Nov 2, 2006)

They also make me hallucinate, the Z drugs are the only "benzo's" i respdong too, not in anxiety kind of way but they sedate me and make me see stuff.


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## crayzyMed (Nov 2, 2006)

More info about its action.



> In Russia, this kind of research conducted in the State Research Institute of Pharmacology RAMS im.V.V.Zakusova scientists from the pharmaceutical department of genetics under the guidance of academician P. Seredenin.
> Based on the concept of genetic predisposition to anxiety, staff set up an experimental model, allowing to study neurochemical changes in the emotional-stress effects in "bold" mice are prone to severe reactions to fear. It turned out that the latter stress caused violations of GABA A receptor-mediated neuromediator system, essential for the regulation of anxiety. Long-term study of mechanisms to identify the changes led to the conclusion that their prevention can provide a selective anxiolytic effect. At the State Research Institute of Pharmacology im.V.V.Zakusova was held required complex chemical, pharmacological, pharmaceutical and toxicological work, led to the emergence of afobazola.
> Of particular importance were the clinical studies performed under the guidance prof.G.G.Neznamova, in which selective anxiolytic effect afobazola shown in patients with anxiety disorders. The results of subsequent clinical trials conducted in the most prestigious institutions of the country: the Center for Mental Health, RAMS, Institute of Forensic and Social Psychology im.V.P.Serbskogo, in the Institute of Psychiatry and in the mental institute im.V.M.Behtereva St. Petersburg have confirmed the experimental and clinical data established in the State Research Institute of Pharmacology RAMS im.V.V.Zakusova.


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## crayzyMed (Nov 2, 2006)

Wow great post man.

I would try it, but as i'm pretty treatment resistant YMMV. It definatly has many interesting properties tough.

I do think its possible this stuff is untherdoses and could have acute results in high doses, i will definatly try some megadoses:yes.


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## Vini Vidi Vici (Jul 4, 2009)

has anyone started or done a thread on Dimebolin? http://www.ncbi.nlm.nih.gov/pubmed/18939977

if Dimebolin was combined with Amisulprude, one could get 5ht2c antagonism, and also 5ht6 and 5ht7 antagonism, presumably. and also GHB agonism, and weak D2/3 antagonism.

http://www.springerlink.com/content/515j16481x05557v/

Dimebolin = 5ht2c, 5ht5a and 5ht6 antagonism, and Amisulpride = 5ht7 antagonism. If these were taken with Tandospirone/Flexinosan for 5ht1a agonism, and weak 5ht4 agonism (Flexinosan) .....this might be the ultimate serotonergic/antidepressant combo, especially combined with any other random Stimulant, opiate, or benzo.

only thing youd have to do is counteract the Histamine agonism, which woudln't be very hard to do, and besides, Histamine agonism isnt that bad.

--another potentially interesting compound is Deramiclane....but i don't think ill be trying it due to its 5ht2a antagonism and GABA reuptake inhibition. but it might work well for some people.


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## crayzyMed (Nov 2, 2006)

Dimebolin looks great, unfortionally i havent found it anywere on the net. If it was availible id make a thread about it.


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## Vini Vidi Vici (Jul 4, 2009)

i found it online.... but its 
$ 197 for 30 pills of 10mg. so i might as well have not found it...but i guess if one was rich enough to invest in it....but its even more than agomelatine! it seems all the 5ht2c antagonists that actually look good cost ...alot for some reason


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## Payn (Sep 15, 2008)

sounds very promising... has anyone tried it for social anxiety ?
I had to order it online, its very cheap, 20 dollars for 50 pills.


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## Vini Vidi Vici (Jul 4, 2009)

Payn said:


> sounds very promising... has anyone tried it for social anxiety ?
> I had to order it online, its very cheap, 20 dollars for 50 pills.


WHat?? Dimebolin? thats awesome! that you could find it


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## crayzyMed (Nov 2, 2006)

Vini Vidi Vici said:


> WHat?? Dimebolin? 20$ for 50 pills....i thought it was all expensive


I think he's talking about afobazol.


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## Vini Vidi Vici (Jul 4, 2009)

crayzyMed said:


> I think he's talking about afobazol.


awwww...im sad now


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## crayzyMed (Nov 2, 2006)

Vini Vidi Vici said:


> awwww...im sad now


Yeah..
I found that dimobolin source, its a damn ripoff. It was used as an antihistamine in russia, it was probably dirt cheap there.


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## Vini Vidi Vici (Jul 4, 2009)

crayzyMed said:


> Yeah..
> I found that dimobolin source, its a damn ripoff. It was used as an antihistamine in russia, it was probably dirt cheap there.


.......until they found out that it might help some people other than those looking for an antihistmine. then it became expensive..... it is frustrating. i wish all the good medications would be like 10 cents a pill, like a single regulated price...and like if the whole world could have 1 FDA, instead of multiple ones.

if one looks at the statistics for depression/anxiety/SA....one can find that millions of dollars in disabilty are spent on such individuals. why not spend those millions of dollars making better drugs (or just simply marketing the good ones that are just sitting around as research chemicals) ......and actually help the people?

if i live past the age of 25, i am seriously gonna start my own pharmeceutical company.


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## crayzyMed (Nov 2, 2006)

Just found this experience regarding afabazol online:


> I have been taking Afobazol 10mg/day for a week. On that dose I don't
> feel a buzz nor I feel stimulating effects but there is definitely a
> noticeable effect on anxiety and social anxiety. I took double dose on
> the day of my PhD defense and it helped me give a more relaxed
> ...


http://groups.google.ca/group/agomelatine-psychonauts/browse_thread/thread/223c99ef3a2065d7?hl=en#

I still have all my afo around, i kinda lost my intrest in it but this report makes me interested in trying it again.

Now my question is, how significant is the MAOA inhibition?? Would it lead to serotonin syndrome in combination with other serotogenics?


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## crayzyMed (Nov 2, 2006)

Bump.
I started afobazole yesterday in combination with memantine, well see how it goes.


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## billyho (Apr 12, 2010)

crayzyMed said:


> Bump.
> I started afobazole yesterday in combination with memantine, well see how it goes.


very interested in your experience with this combo as i am on memantine now and was looking for something to kinda take the edge off..


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## crayzyMed (Nov 2, 2006)

billyho said:


> very interested in your experience with this combo as i am on memantine now and was looking for something to kinda take the edge off..


Dunno wheter it can take the edge of as memantine has no edge for me, yesterday took 20mg 3 times a day but this seemed to make me tired, back to 10mg wich seems to be energizing with memantine.
It needs some time to work, according to the russian study it gets more effective then benzo's for anxiety after a few weeks.


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## crayzyMed (Nov 2, 2006)

http://www.imminst.org/forum/index.php?showtopic=38982
He also tried afobazole for anxiety.

On the agomelatine psychonauts group there are also several reports regarding it, altough rather mixed.


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## billyho (Apr 12, 2010)

crayzyMed said:


> http://www.imminst.org/forum/index.php?showtopic=38982
> He also tried afobazole for anxiety.
> 
> On the agomelatine psychonauts group there are also several reports regarding it, altough rather mixed.


thanks for the info.. is the 'edge' i'm feeling on memantine transient? i've felt an increased drive with a slight agitation but no real effect on ocd for 4 days since upping my dose, then today i kinda crashed a lilttle.


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## martyboi (Sep 18, 2009)

Anyone know what the half-life of afobazol is? i'm wondering what would be the best way to dose it.


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## crayzyMed (Nov 2, 2006)

martyboi said:


> Anyone know what the half-life of afobazol is? i'm wondering what would be the best way to dose it.


No idea, but its recommend to take 10 or 20mg 3 times a day.

I felt exhausted after work today but after taking memantine+EGCG+afobazole full of energy again, other meds could have contributed too tough, but i think i notice a anxiolytic response from it.

Also seems to be a very good neuroprotectant, anti mutanergic, also check this interesting study.



> Effect of afobazole on DNA damage in patients with systemic lupus erythematosus.
> Zhanataev AK, Lisitsyna TA, Durnev AD, Nasonov EL, Seredenin SB.
> 
> V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences, Moscow, Russia. [email protected]
> ...


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## crayzyMed (Nov 2, 2006)

billyho said:


> thanks for the info.. is the 'edge' i'm feeling on memantine transient? i've felt an increased drive with a slight agitation but no real effect on ocd for 4 days since upping my dose, then today i kinda crashed a lilttle.


It should go away, i felt agitated from memantine too the first few days.


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## billyho (Apr 12, 2010)

hey crayzyMed, how's the afo/mem trial going?


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## crayzyMed (Nov 2, 2006)

billyho said:


> hey crayzyMed, how's the afo/mem trial going?


Memantine still working solid for OCD, afobazole not sure, it gives me more energy sometimes and other times i seem to get tired.


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## crayzyMed (Nov 2, 2006)

It may as well be placebo but i think my meds are kicking in, feel lots of energy today even tough i barely slept 4 hours, getting out of bed seemed really easy (had to get up early for work) my mood is more stable too. I dont feel as ****ty right now, and am quite enjoying listening to some music, i'm still a bit bored, but my anhedonia seems alot better.


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## lit (Feb 9, 2010)

Hey, this is for Crazymeds mainly I wanted to ask how the afobazole is going, have you given up on it for now?. 

I was thinking of ordering a little as its so cheap. could you give us an update if you don't mind.


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## crayzyMed (Nov 2, 2006)

lit said:


> Hey, this is for Crazymeds mainly I wanted to ask how the afobazole is going, have you given up on it for now?.
> 
> I was thinking of ordering a little as its so cheap. could you give us an update if you don't mind.


Just gave an update the post above you, i think its starting to kick in, feel more energie, anxiety is reduced too. I'm taking it with 20mg of memantine, so that may also play a role.


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## chrono (Feb 10, 2010)

Great thread, thanks for keeping us updated, crayzyMed.

I'll be interested to see if you run into any problems like Thorsten did (over on ImmInst; see post #39 in that thread).


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## crayzyMed (Nov 2, 2006)

chrono said:


> Great thread, thanks for keeping us updated, crazyMed.
> 
> I'll be interested to see if you run into any problems like Thorsten did (over on ImmInst; see post #39 in that thread).


Hello chrono, we know eachother from imminst, my name there is MeDieViL.

Yeah ive read that thread, i will keep you updated.


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## lit (Feb 9, 2010)

crayzyMed said:


> Just gave an update the post above you, i think its starting to kick in, feel more energie, anxiety is reduced too. I'm taking it with 20mg of memantine, so that may also play a role.


I must of just missed that, well that sounds positive, will order some, have been thinking of trying memantine too but for now I'll just try afobazole on it's own.

Thanks for the update.


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## martyboi (Sep 18, 2009)

I just started this **** a couple days ago. I havent noticed anything yet, not even side effects. Assuming this stuff works, i'm gonna experiment with a few combinations:

Afobazol + Kava (daily)
Afobazol + Mulungu extract
Afobazol + Suntheanine
Afobazol + Picamilon
Afobazol + All of the above

Has anyone tried any of these combos before? maybe i'll be the first. Normally these OTC substances are useless but perhaps they might synergize with afobazol and have a much more pronounced effect.


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## chrono (Feb 10, 2010)

crayzyMed said:


> Hello chrono, we know eachother from imminst, my name there is MeDieViL.
> 
> Yeah ive read that thread, i will keep you updated.


Well, what a small world! 

Afobazol sounded very exciting to me, partly because I have a lingering (and admittedly irrational) preference for medications which don't take a month or two to manifest results, and which you can take a break from.

Unfortunately, afobazol seems to have some MAOI-A activity, which I'm not willing to risk with my tramadol. Getting pretty sick of that constraint -_-


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## enfield (Sep 4, 2010)

bump


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## socialpiranha (Dec 9, 2012)

I tried it, didnt really notice any effect. still have it...


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## enfield (Sep 4, 2010)

socialprisoner said:


> I tried it, didnt really notice any effect. still have it...


how long did you try it for. a lot of people say you have to take it for awhile before you can start to notice anything. do you remember how much you took? 10mg? 20mg?


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## socialpiranha (Dec 9, 2012)

enfield said:


> how long did you try it for. a lot of people say you have to take it for awhile before you can start to notice anything. do you remember how much you took? 10mg? 20mg?


i ony took it for four or five days at 10mg i've tried so many that are "supposed" to work a month later and didnt that i couldnt stick with it. god knows whats counterfeit and whats legit ordering off the internet though the packaging looked genuine and the tabs were air sealed but who knows. i figured i'd feel some positive effect within the first few days if it was going to have any effect but i prob should have given it longer just hard to keep motivated when youve had so many similar failures. I try to stick to drugs that will show effects within a day or two unless im really excited about them. I don't know what the laws are but if its legal to send it to you and you wanna try it let me know.


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## enfield (Sep 4, 2010)

socialprisoner said:


> i ony took it for four or five days at 10mg i've tried so many that are "supposed" to work a month later and didnt that i couldnt stick with it. god knows whats counterfeit and whats legit ordering off the internet though the packaging looked genuine and the tabs were air sealed but who knows. i figured i'd feel some positive effect within the first few days if it was going to have any effect but i prob should have given it longer just hard to keep motivated when youve had so many similar failures. I try to stick to drugs that will show effects within a day or two unless im really excited about them. I don't know what the laws are but if its legal to send it to you and you wanna try it let me know.


thanks for the reply! okay i see. yeah the source on ebay looks official. all the sources i looked at, in fact, looked like they were manufactured the same way. it's kind of you to offer me yours (as far as i know that would be legal, yeah). but since it's not terribly expensive, and since you have to try it for a long time to see if it works possibly, if i do decide to try i, i think i'll just buy the 60 10mg pills for the $.60 or whatever they cost, each.


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## socialpiranha (Dec 9, 2012)

k


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## tygiag (May 29, 2012)

Anybody getting any results yet with this stuff? I'm thinking about buying some, but not really into waiting 3 weeks to get it. 

Also, I don't really respond well to GABA, so I am wondering if this will be a waste or not.


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