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Pagoclone - Human dosages used in studies?

flynn54

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Oct 8, 2015
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Hello,

The chemical fairy has put a couple hundred milligrams of Pagoclone under my pillow. Having read research studies on humans, doses of 1.8mg to 4mg were used, but only to achieve an anti-stuttering effect and the papers would claim that the anxiolytic effects only showed up in some of the subjects in doses of 3mg and more. The fact it is a partial BZD agonist does not mean this is a useless chemical, isn't flurazepam a partial BZD agonist too, and the one time I had it, I can say it was far from weak and hyper long lasting. I also wonder about the length of the effects of pagoclone. I wonder what dose I should try to attempt using it for GAD and the information is sparse, I only know it is an anxiolytic drug.

Anyone with first-hand experience or just good old speculation is welcome in giving me info about this compound, because if it is effective, and lasts a decent 6 to 8 hours at least, I'm going to be pretty happy and not touch my Lectopam script and stockpile it for a while. I did a lot of research but it seems like the anti-stuttering effects are monopolizing research at the higher levels of, well, research.

Thanks a lot!
 
Hi flynn,

Would you mind to describe your pagoclone (color, consistency, etc)? I've been interested in this compound too (also as an anxiolytic agent, as it's related to the Z-drugs but not sedating) and once I got my hands onto a little bag which claimed to contain pagoclone. It was a fluffy, weirdly reddish-pink-somewhat substance, with next to no taste (not bitter at all like zopiclone) ... and it had no effects at all, neither ingested nor intranasally. Think I've titrated up to at least 5mg but stopped when I felt really nothing at all. Didn't want to take more of something potentially containing heavy metals or whatnot.

With zolpidem or zopiclone I get a definitive reaction from even 3.75mg.

Since I didn't have the chance to get a proper GC/MS analysis, I don't know whether it was legit or not.
 
Hi dopamimetic,

The pagoclone is an uniformely pink powder, no other colour. The fairy....well, I'll drop this, the vendor whom I got this from is very well regarded. Right now I'm just going to buy a new scale because the studies here : http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2515892/ claim that 0.6mg is large dose, and my best scale is very precise but only down to 10mg and the local headshop doesn't have milligram scales and pagoclone is barely soluble in either water and ethanol. I doubt it'll turn out inactive though, but I'll keep you on the loop when I decide to have some, most likely a weighted 10mg split in 10 tiny piles...I have the tools to do this, but I can't guarantee a 1mg dose, I know. I have access to a mass spectrometer, it might not be enough to be 100% sure and I'll most likely end up trying it before getting to the lab which I'm authorized to use but since it is not mine and I only work there as a subcontractor here and there, it might take a while.
 
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They have a .com domain, sell some SARMs and changed their name / domain somewhen to the beginning of this year? ;) Then it's the same stuff.

I've read about the potency too, that was why I really thought to have been scammed when it had no effect at a multiple of a 'large' dose - although they stopped the trials for stuttering afaik because it didn't work as well, and the anxiolytic dosage may be somewhat higher...

Do you think the insolubility could be the reason for my failure? That I should have used some solvent or oil...?

Yeah, please keep us informed! I'm truly curious about your experiences (am having higher hopes about GABA reuptake inhibitors like that one though - they seem to be free of any relevant tolerance or dependence / withdrawal....)
 
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Well, now that's a downer (or is it?).

I've had another product from that place and it was def active, the only mescaline analogue other vendors in my country did not stock, well that one had none of them except that one,methallyescaline and it was excellent. I hope the product's not a scam, because otherwise I'd just buy more etizolam powder.
 
I've tried and α5 selective benzos and 3mg equated to 1 unit of alcohol. 3 of us took 25mg and we were drunk in a good way - not so much bouncing off walls, no nausea, no rebound anxiety. Would make an ideal drug to dry out alcoholics as it's so much less harmful. I think an admixture with 1,amino cyclopentanol (the active in Tippler's Bane) mushrooms. It's much less toxic than disulfuram and someone isolated and patented the active. Coprine is found in the plant but was proved to be a prodrug. I know it was tested on a guy who drank 1l of gin per day (40 units) and he swapped to the pills for a day - he used 30, had no desire for alcohol and said that if the price were the same, he would switch to the pills.
Mixed WITH ethanol would be dangerous hence the afmixture.

I also found a benzo with really potent anti-depressant effects. I think it would be VERY useful for doctors to give a 2-week course as the SSRI began working. As you may know, the VAST majority of suicides are committed not in the depths of unipolar depression but going in or coming out. If we had something to cover the spot between first presentation and the SSRIs working, it would save a LOT of lives.

Both of the above are VERY difficult to make so it would cost £100,000 to produce efficient routes to them, then cellular studies, then animal studies. I truly believe that both would save many lives (although the alcohol pill is HR BUT since it's only acting at 1 site, the BAD effects of alcohol are removed and the patient could first be dried out then given a reduction using the pills. My mother is an alcoholic so I have good reason to want them to be successful.

Oh yes - and both of them are unmetabolized - they leave the body as the same compound that goes in.

My other idea is for a long-acting nicotine agonist. Not to replace cigarettes for healthy people, but to make psychiatric wards smoke 3. My wife worked on such a unit for 8 years and over 90% of patients smoked. I can guess why - it's to get SOME dopamine into brain-cells. Neuroleptics cause anhedonia so they 'exist' rather than just live. Hence my interest in schizophrenia medication. The refractive patents (10%) don't have a dopamine issue, they have too little NMDA. 2 metabolic disturbances that produce the same results. No study has been carried out using JUST patients with low-NMDA, just general population hence it appears to help just a few. If 10% of patients were treated with NMDA agonists, the horrible, toxic clozapine would not be in use. That last one is my life's work. Loosing a close friend in his early 20s (he would be 50 now and is still in an RSU) and also knowing a true genius who is on clozapine makes me want to develop stronger affirmations than 'hypothesis'.

If any of them take off, I'm planning to have sofosbuvir made in India (where it was refused a patent because it's just too similar to the first generation of HIV medications) so that EVERY PERSON with Hepatitis C gets treatment. I see big pharma as inherently evil and if the dose-units carry a language-appropriate livery, NICE could buy them. As I understand it, the legal side is between the maker and the.... non-patent in India. I don't think it's a crime to import the drug itself.

FREEDOM OF SPEECH
 
It's possible that I just did not respond like the majority of people do to this certain compound ... my previous experiences with them (before the name change) were always excellent, a bit expensive but qualitatively top.

Or it's really about the solubility. Maybe some workup is required before the body can absorb it in this certain form they deliver it.

clubcard said:
I also found a benzo with really potent anti-depressant effects. I think it would be VERY useful for doctors to give a 2-week course as the SSRI began working. As you may know, the VAST majority of suicides are committed not in the depths of unipolar depression but going in or coming out. If we had something to cover the spot between first presentation and the SSRIs working, it would save a LOT of lives.
I don't get it why nobody sees the need to taper psych meds unless they have life-threatening side effects like with lamotrigine. Maybe the onset of SSRIs would be much less disturbing if they'd increase the dose every day by 5mg on the example of venlafaxine.. and do the same when discontinuing, but even slower.

And to your other statements I do much agree.. NMDA antagonists should be used more widely for a certain subgroup of patients too.. mainly these with impulse control disorder, emotional oversensitivity (which can exacerbate as 'psychosis like' or psychotic / agitated / etc depression or personality disorder but is just oversensitivity, as in my case).. sometimes co-morbid with AD(H)D..
 
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We tried them all on a full stomach but the drinker didn't really eat... and YES, it DOES make you want to drink. I've never tried just 3 or 6 mg - we quickly found 25mg to be fantastic for getting silly drunk with no payback.

If you tried the other, did you get the strong antidepressant effects we all got. Would have to make 12 hour sustained release, QID aministration is too many chances to forget. We found 3mg to be the perfect number.
 
Would you mind to share the chemical names of these compounds (or are you talking about pagoclone- was yours then pink as well)? They sound interesting for sure. :)

A better alcohol replacement would be NICE to have (even more so than a better caffeine, because we already have things like that). Pagoclone has been proposed as such one, this was with what raised my interest for it. I hate drinking, or rather half of the effects and the side and after effects of it.. the cognitive impairment, AMPA negative allosteric modulation, etc.. and what it makes people to do, act and look like.. Sometimes I thought of dissociatives to be the better ethanol, but well.. it's a different beast and definitely not for the masses.

(I feel utterly snubbed that one of the most 'developed' countries in Europe wants to put me in jail just because of my interest and curiosity and thinking different than the mainstream.. I did not hurt anyone nor did I ever sell or hand a chemical to anyone. But that's off-topic ranting and I could fill pages with all that shit.)
 
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Would love to, but cannot patent common knowledge. The closest is QH-II-66 for alcohol (same effect but longer duration whereas this lasts 6 hours. Unlike pagoclone, this one is dirt-cheap to make. There ARE patents US 7119196 is the patent for QH-II-66. Tip - '2 substitution still keeps selectivity.
 
Well, I want info on pagoclone, not these compounds. Thinking it couldn't be worse than snorting 12mg of zaleplon, I weighted 7.5mg of Pagoclone. 30 minutes later and I am feeling a kind of heavy feeling like gravity is pushing on my body downwards. I still have diazepam in my blood and brain for sure as I had my usual 20mg daily dose yesterday in the evening. I read about a related compound called bretazenil and how it dislodged full agonists causing people to experience withdrawal...so after a dust-sized allergy test, 2 hours later I had that 7.5mg. I seem to have this light-headed feeling, a kind of carefree, unable to listen to the extremely serious geopolitical podcast playing in my headphones, it's all noise to me. My arms feel heavy and typing this is kind of tiring. So I guess it works, but 7.5mg might be a larger dose than the anti-anxiety only effects spoken of in the 5 or so studies I have read. Although, I do not feel any impossible to resist feeling of going to bed, yawning or what would fall into the "sedative" effect. It kind of feels like when you force yourself to stay up on zopiclone, but, at least, in my case, without the alien (no hallucinations) nature of the environment even if I am in my own house, which also happens if I wake up after taking zopiclone for sleep to pee, I can't help but sit back in the bed thinking that everything feels...unfamiliar, alien, even if I recognize objects in my head, that feeling is really peculiar to zopiclone. Nothing of the sort happening right now with pagoclone. I will not be taking more today, I want to see how long this lasts.
 
So, did you find it a good replacement 'social lubricant' that Dr. Nutt suggested it would be useful for? QH-II-66 feels JUST like all of the good points of alcohol with none of the bad. Your drunk for 12 hours with this one but it doesn't affect your balance too much, you don't do stupid things, you don't get nausea or vomiting and no hangover. You just gently sober up. I took it with 2 others, One 25, one 45 & one 51 Years old. We were ALL amazed about how accurate it's effects were. One hadn't touched alcohol for 25 years and while they enjoyed it, they said they wouldn't take it again because it would lead them back to alcohol.

I AM surprised none of the RC crowd haven't made it. HALEX, anyone?
 
If this carries the same visual hallucinations as zopiclone than its use would be very limited.
 
Have to revise my old posting here, either I took too less (regarding its potency, this shouldn't have been the case. It's been too long since to remember though.) or that batch was indeed sketchy. But recently another sample of pagoclone managed its way into my lab. It indeed is an interesting chemical, even when I wasn't really sure what to expect as to me somehow significant anxiolysis is usually inseparatable from intoxication or negative effects as losing inhibitions too much, drowsiness/sedation etc. and the claims for pagoclone say it does not share these, but also failed as an anxiolytic if I remember correctly.

What remains is indeed something along that description and hard to put in words. Would say it will have its use as an anxiolytic for some, and for these to be superior to benzodiazepines. About sedation I remained unsure. It has the signature of a downer, and probably the potential to cause "drunk" behaviour when dosed high enough, but there was no tiredness or urgency to sleep as I get with any and all benzos, severly limiting their use. At first I found it underwhelming, just to finish the bag in two weeks or so. Yeah, it's a recreational, and I'd call it safer than ethanol (ok, that one's easy).

@muie: It appears not to (indeed I was somehow hoping to get them, as zopiclone was very interesting in this respect but at the required dosage or combined with ethanol much too sedating to remember anything besides the obvious 'whoa, that would have been interesting ... if I only could remember anything real'). Zolpidem strangely doesn't work at all for me. It causes an interesting rush at just 5mg but that's it. No sleep, nothing. Pagoclone is unlike either one.

Oh, I'd love to get some of that QH-II-66 ... :/
 
Probably effects related to Serax (yet with more a1 selectivity and less detrimental effect on cognition). But that's weird that it produces less sedation given it's a1 affinity.

But it's not well-researched, so there's that looming risk. Better to stick with classic benzos.
 
I took what I believe to be 6mg 1 hr ago and 6mg 30 min ago for a total of 12mg.

Subjective effects:

Strange drug. It’s unlike zopiclone and Ambien in that it doesn’t produce unusual thoughts or logical implications which wouldn’t occur while sober. It has some of zopiclone's effect (to a lesser extent) where you’ll feel sober for a minute and impaired the next. No metallic taste in mouth whatsoever. Moderate immediate forgetfulness—where you’ll think of something and forget what you were thinking about a few seconds later. Way more muscle relaxing than zopiclone (not sure if its actually muscle relaxing or just body parts feeling heavier), maybe at the level of a benzo or even more. More of a “high” feeling. Probably good for sleeping but not pushing you to sleep in the way zopiclone can. So more of a physical impairment and less of a mental impairment. More emotionally blunting than euphoric.

A good comparison I think would be a shorter acting flualprazolam (similar anxiolytic and hypnotic effects) with more of a physical high feeling.

Pharmacokinetics:

t_max seems to be similar to zopiclone, maybe a bit less (so 1–1.5 hours), therefore I think elimination half life is probably also around 5 hours (I’ll probably sleep soon so I can’t really comment on that). I would say 3mg is about equivalent to 7.5mg zopiclone but they’re hard to compare, I think comparing it to benzos would be more appropriate, which would be about 6mg = 0.75mg Xanax (I have a mild to moderate tolerance).

Also regarding the title, I didn’t read the rest of the thread but in one study for anti-stutter effects I saw they used 0.3/0.6mg and in a Pfizer study for cognitive impairment 1–4mg.

Thanks,
scriptchaser

Edit: It's been about 3 hours since the first dose and the effects have markedly decreased, so I want to revise the elimination half life to 2 hours or potentially even lower. t_max seems to have been overestimated as well, based on my gut feeling, so let's say 1 hour for t_max, possibly also lower. These parameters align more closely with Zaleplon, which itself has unusual pharmacokinetics with the half life being lower than the time to maximum plasma concentration (1.01h vs 1.1h). This is unfortunate, I was really hoping for a longer duration of action.
 
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