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ALKS 5461/CERC-501 kappa antagonists

alks 5461 cerc-501 kappa antagonists

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#1 tolerant

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Posted 27 June 2016 - 04:15 PM


Would anyone be interested in organising a group buy for either of these compounds?

 

https://en.wikipedia...ine/samidorphan

 

https://en.wikipedia.org/wiki/CERC-501



#2 Stinkorninjor

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Posted 27 June 2016 - 09:06 PM

CERC-501 definitely looks interesting! = ) The much lauded Samidorphan seems to have been a bit of a dud though... not even remotely as effective as the true, pure K-antagonists.

 

It's too bad JDtic has that pesky VT side-effect - it would be the ultimate anxiolytic otherwise - complete abolishment of feelings of dread of punishment.

 

It makes you... BRAVE. But without becoming a dumb-ass as well, as so many other compounds do.



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#3 MoreNowAgain

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Posted 27 June 2016 - 10:40 PM

I would be interested in a CERC-501 group buy.



#4 tolerant

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Posted 30 June 2016 - 09:33 PM

I think we should try to revive interest in this thread.



#5 Der Springende Punkt

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Posted 01 July 2016 - 06:45 AM

I would be interested in a CERC-501 group buy.

 

Mee too.



#6 satsumass

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Posted 04 July 2016 - 04:07 AM

I'm in for a group buy of CERC501 as well.



#7 tolerant

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Posted 07 July 2016 - 10:32 PM

So currently we have the following members interested in a CERC-501 group buy:

 

tolerant

Stinkorninjor

MoreNowAgain

Der Springende Punkt

satsumass

 

I am currently in the process of researching and approaching labs. Considering that the dose being researched by the company are 10 mg, my thinking is to offer members quantities of either 300 mg (i.e. one month's supply) or 1 g (three months' supply). If there's positive feedback, we can always arrange another group buy.

 


Edited by tolerant, 07 July 2016 - 10:37 PM.


#8 sentics

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Posted 11 July 2016 - 07:26 PM

any idea how much it will cost?



#9 tolerant

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Posted 11 July 2016 - 07:55 PM

any idea how much it will cost?

 

Not yet, I'm still investigating this by approaching labs. If anyone knows of a suitable lab to approach, please let me know.



#10 gamesguru

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Posted 11 July 2016 - 10:53 PM

If anyone knows of a suitable lab to approach, please let me know.

 

calling out redan



#11 Stinkorninjor

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Posted 12 July 2016 - 10:53 PM

I'm surprised there's so little interest in this one? Considering the highly encouraging results from the trials.

 

Anyways, how many peeps do we need for the group buy to approach critical mass? How many was involved in the NSI-189 group buy, as a reference? And as I recall it, there was more people interested in the JDtic group buy.

 

Shall we have a look at those threads perhaps, and see if we can find suitable group buy -mates to get hooked into the buy? I imagine at least a few of them would be interested.



#12 tolerant

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Posted 12 July 2016 - 11:20 PM

I'm surprised there's so little interest in this one? Considering the highly encouraging results from the trials.

 

Anyways, how many peeps do we need for the group buy to approach critical mass? How many was involved in the NSI-189 group buy, as a reference? And as I recall it, there was more people interested in the JDtic group buy.

 

Shall we have a look at those threads perhaps, and see if we can find suitable group buy -mates to get hooked into the buy? I imagine at least a few of them would be interested.

 

I think part of the reason is that this thread is hidden in the Mental Health subforum, which gets far less traffic than the Brain Health forum. Which is fair enough because KOR antagonists are not known for any cognitive benefits. On the other hand, a lot of people get into NSI-189 (which I think is the most active thread in Brain Health) because of its antidepressant/anxiolytic potential. 

 

Anyway, I registered on dpselfhelp.com to get extra people, because they have a number of threads on KOR antagonists, including a thread on CERC-501 in which they say, why don't we organise a group buy, it's been done on longecity.org many times. So I made a number of very friendly posts and messaged the administrator of the forum, for which I got a ban. Maybe someone who has an account there can recruit people. But your idea of getting group-mates from the JDtic thread is a very bright one!

 

I don't yet know what the critical mass would be. There's an NRX-1074 group buy going on right now (which I'm involved in), which appears to have 15 spots.

 

Yesterday I contacted a Chinese lab (which was kindly suggested to me and endorsed by one of the members here) to get a quote. They said that they already had a CERC-501 project which got halted. They've already got the process figured out (which I enclose), but said the main issue was whether "intermediate 6 can be resolved". Maybe someone with a chemistry background can tell us what that means exactly.

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Edited by tolerant, 12 July 2016 - 11:23 PM.


#13 Stinkorninjor

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Posted 12 July 2016 - 11:36 PM

 

I'm surprised there's so little interest in this one? Considering the highly encouraging results from the trials.

 

Anyways, how many peeps do we need for the group buy to approach critical mass? How many was involved in the NSI-189 group buy, as a reference? And as I recall it, there was more people interested in the JDtic group buy.

 

Shall we have a look at those threads perhaps, and see if we can find suitable group buy -mates to get hooked into the buy? I imagine at least a few of them would be interested.

 

I think part of the reason is that this thread is hidden in the Mental Health subforum, which gets far less traffic than the Brain Health forum. Which is fair enough because KOR antagonists are not known for any cognitive benefits. On the other hand, a lot of people get into NSI-189 (which I think is the most active thread in Brain Health) because of its antidepressant/anxiolytic potential. 

 

Anyway, I registered on dpselfhelp.com to get extra people, because they have a number of threads on KOR antagonists, including a thread on CERC-501 in which they say, why don't we organise a group buy, it's been done on longecity.org many times. So I made a number of very friendly posts and messaged the administrator of the forum, for which I got a ban. Maybe someone who has an account there can recruit people. But your idea of getting group-mates from the JDtic thread is a very bright one!

 

I don't yet know what the critical mass would be. There's an NRX-1074 group buy going on right now (which I'm involved in), which appears to have 15 spots.

 

Yesterday I contacted a Chinese lab (which was kindly suggested to me and endorsed by one of the members here) to get a quote. They said that they already had a CERC-501 project which got halted. They've already got the process figured out (which I enclose), but said the main issue was whether "intermediate 6 can be resolved". Maybe someone with a chemistry background can tell us what that means exactly.

 

 

It sounds like they are trying to figure out how to combine the two different compounds, to the right, in step #6 into the final structure at the bottom left? As you can see they have jotted down letters and numbers on top of the arrows indicating a chemical change in all of the other steps, but not in the last step. The numbers and letters probably indicates what chemicals and treatments they apply to the compound to transform it to the next stage.

 

Eventually you end up with CERC-501.

 

Hmm... what papers are there on CERC-501 synthesis? Even if they are behind paywalls we might be able to have a look... Is there a patent btw? Or perhaps there are synthesis-steps in related compounds, available - which can be used to figure out the final step.

 

You're right about us needing a chemist for some info though, lol! Tricky, tricky... I'd try to learn it, but I'm too burnt out at the moment.



#14 tolerant

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Posted 13 July 2016 - 02:10 AM

By the way, getting back to the JDTic thread, the makeshift selective KOR antagonist in the form of buprenorphine + naltrexone was discussed at length in that thread. I want to try this combination, but so far I haven't been able to find a legitimate source for buprenorphine. If anyone knows of one, please let me know. If someone thinks I'm doing something illegal -- I'm not. Buprenorphine is not a "border controlled drug" under Australian legislation, and so it's not illegal to import it. 



#15 MoreNowAgain

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Posted 13 July 2016 - 12:58 PM

Perhaps we can galvanise an interest for the CERC-501/Hydroxynorketamine/Basimglurant group buy on another medium such as Reddit? Of course only after we have found a reliable lab to synthesize them.


Edited by MoreNowAgain, 13 July 2016 - 01:02 PM.

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#16 Stinkorninjor

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Posted 13 July 2016 - 01:42 PM

Perhaps we can galvanise an interest for the CERC-501/Hydroxynorketamine/Basimglurant group buy on another medium such as Reddit? Of course only after we have found a reliable lab to synthesize them.

 

An excellent suggestion, which I had been considering myself. I am all for it!

 

I believe we actually have the lab though, they just need a little bit more info, so they can complete the manufacturing-process.

 

What other forums are there? Drugsforum? Bluelight? Etc, et c.

 

Let's just stack them here, and then we can start assigning people to start the process of recruitment:

 

1. Longecity (Half-done!)

 

2. Reddit /r nootropics, /r mentalhealth,

 

https://www.reddit.com/r/Nootropics/

https://www.reddit.com/r/mentalhealth/

https://www.reddit.c.../mentalillness/

 

3. Drugs Forum - Health

https://drugs-forum....splay.php?f=308

 

4. Crazyboards - Antidepressants

http://www.crazyboar...nd-you-know-it/

 

5. Crazymeds - miscellaneous antidepressants

https://www.crazymed...ant-miscellany/

 

 

If anybody knows of any more mediums and places, then don't hesitate to list them here, and then we can go to work on them.


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#17 GreenWhite

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Posted 13 July 2016 - 03:11 PM

I would be interested after the NRX 1074 group buy. First i want to see if NRX is helping me if not i would be interested in a spot.



#18 tolerant

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Posted 13 July 2016 - 10:09 PM

I believe we actually have the lab though, they just need a little bit more info, so they can complete the manufacturing-process.

 

It's a big question mark whether we do have a lab. Of course if we explain the last step of the synthesis to them, they will probably do it. But our most recent communication was as follows:

 

I wrote (from my fake corporate email address at my fake corporate domain name, including the name of my fake organisation and my fake corporate signature):

 

Thank you for your prompt reply.

We do not require the substance urgently. I understand it will involve custom synthesis, and if the synthesis could be completed within a six-week period, that would be acceptable. With regards to specifications, we would need the highest purity that could reasonably be achieved without a major escalation in price. With regards to a target price, while we do have a range in mind, at this moment we are soliciting quotes from a number of labs, so I would appreciate it if you could provide me with a quote that would cover your costs and profit margin.

Finally, we had a look at the proposed steps of synthesis, and understand the difficulties, but we would expect to be provided with a firm answer as to whether the synthesis can be achieved, because we cannot proceed on the basis that the synthesis might fail.

I eagerly await your response.

 

They wrote:

 

Thank you very much for your email.
The resolution of intermediate 6 is truly difficult that we cannot guarantee the 100% success. Besides, you require highest purity. And we cannot guarantee 6- week period as well. This is why the project cannot be started quickly.

Moreover, due to G20 held in Hangzhou, we cannot transport chemicals from August 15th to September 15th. You can take a look whether you can find suitable suppliers or not. When our project re-starts in the future and we can provide this compound, we will contact you again.

 

I tried to sound professional but maybe I scared them off a bit.


Edited by tolerant, 13 July 2016 - 10:25 PM.


#19 tolerant

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Posted 14 July 2016 - 04:16 AM

CERC-501 definitely looks interesting! = ) The much lauded Samidorphan seems to have been a bit of a dud though... not even remotely as effective as the true, pure K-antagonists.

 

It's too bad JDtic has that pesky VT side-effect - it would be the ultimate anxiolytic otherwise - complete abolishment of feelings of dread of punishment.

 

It makes you... BRAVE. But without becoming a dumb-ass as well, as so many other compounds do.

 

Could you elaborate on your experience with JDTic? There's precious little anecdotal reports on KOR antagonists out there. As such, yours is definitely one which inspires me to obtain CERC-501 and to try a buprenorphine/naltrexone makeshift KOR antagonist which I referred to above.



#20 Stinkorninjor

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Posted 14 July 2016 - 06:18 PM

 

CERC-501 definitely looks interesting! = ) The much lauded Samidorphan seems to have been a bit of a dud though... not even remotely as effective as the true, pure K-antagonists.

 

It's too bad JDtic has that pesky VT side-effect - it would be the ultimate anxiolytic otherwise - complete abolishment of feelings of dread of punishment.

 

It makes you... BRAVE. But without becoming a dumb-ass as well, as so many other compounds do.

 

Could you elaborate on your experience with JDTic? There's precious little anecdotal reports on KOR antagonists out there. As such, yours is definitely one which inspires me to obtain CERC-501 and to try a buprenorphine/naltrexone makeshift KOR antagonist which I referred to above.

 

 

Sorry mate, but I'm going off of anecdotes and the proposed mode of action too - I don't know any more than you do. : | Sorry if I gave that impression! I'm going off the discussion on ALKS-5461's trial-reports on Reddit when it comes to my doubts about that one - as I understand it, the initial results aren't as dramatic at all as JDtic.

 

Here, check the press-release:

https://www.thestree...th-outlook.html


Edited by Stinkorninjor, 14 July 2016 - 06:37 PM.


#21 tolerant

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Posted 14 July 2016 - 08:46 PM

 

Could you elaborate on your experience with JDTic? There's precious little anecdotal reports on KOR antagonists out there. As such, yours is definitely one which inspires me to obtain CERC-501 and to try a buprenorphine/naltrexone makeshift KOR antagonist which I referred to above.

 

Sorry mate, but I'm going off of anecdotes and the proposed mode of action too - I don't know any more than you do. : | Sorry if I gave that impression! I'm going off the discussion on ALKS-5461's trial-reports on Reddit when it comes to my doubts about that one - as I understand it, the initial results aren't as dramatic at all as JDtic.

 

Here, check the press-release:

https://www.thestree...th-outlook.html

 

 

 

Nah, that's fine. As long as you're going off more than more than one anecdote, that's even more valuable. If you're going off just one, that's OK too.

 

As regards the article, yeah I've come across this info before. Sometimes you get an enormous placebo response and have to do further trials until that placebo response comes down -- apparently that's how MDD trials work. What I would mention is that according to the member Oracle Laboratories here, samidorphan is one of the only drugs strong enough to block buprenorphine's MOR activity. Maybe they overdid the samidorphan dosages. I think that in the previous trials, 0.5mg/0.5mg and 2mg/2mg showed response, while 8mg/8mg didn't. So it may be that you put enough samidorphan in there and it will block not only buprenorphine's MOR activity but natural MOR activity, leaving a person with the symptoms of opiate withdrawal. I mean, one would have thought the researchers are smart enough to figure all of that out, but we know from anecdotes that JDTic works, we know from anecdotes AND studies that buprenorphine on its own works for MDD, we know from anecdotes that buprenorphine/naltrexone works. So why not buprenorphine/samidorphan?

 

Plus, if you look at the stock prices, the stock plummeted from about $60 to $35 on the back of that news, but now it's back up to $50 (though that may well be on the back of other drugs they're developing).


Edited by tolerant, 14 July 2016 - 08:57 PM.


#22 tolerant

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Posted 22 July 2016 - 10:34 AM

I have secured a quote from a Chinese lab of $8200 for 10 grams of CERC-501. This quote is excessive (i.e. it's almost on par with reputable Western European/US suppliers), so I will be negotiating.

 

But I need to know how much people are prepared to pay for this compound and how much they want to buy. Keep in mind that the daily dose is 10 mg. So 300 mg will last a month, and a gram will last three months. Please express your interest by stating the amount of the substance you wish to buy and what price you would be willing to pay for it. Thanks.



#23 satsumass

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Posted 22 July 2016 - 10:45 AM

500mg, willing to pay $250



#24 MoreNowAgain

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Posted 22 July 2016 - 02:59 PM

Willing to spend $250-300



#25 alex921

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Posted 25 July 2016 - 06:31 PM

Interested in this group buy. If the price is right .



#26 Stinkorninjor

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Posted 25 July 2016 - 10:07 PM

500 mg - willing to spend 150 $. :)

With the warning that I am a poor guy these days, so not sure if I'll have the money. : | Still, I'll try!

#27 tolerant

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Posted 25 July 2016 - 10:58 PM

The lab agreed to reduce the price of 10 g synthesis to $7200. Five grams would cost $5000. Five grams is also the smallest amount they are willing to  The lab (DC Chemicals) has previously supplied good quality basimglurant (see this thread) and claim to have experience in making CERC-501. Unfortunately we have not yet generated anywhere close to enough interest for a synthesis. So we wait.



#28 tautomeric

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Posted 28 July 2016 - 09:27 PM

These 2 medications are being researched for fighting against substance abuse. I do not really understand the point of the group buy. Is it for treating conditions such as alcohol abuse to help quitting, or get a legal opioid succedaneum ?

EDIT : I found a bit of answer in another thread :

 

 

I'd Be interested in any people that have used Dihexa and can report on its action etc If anyone has any Advice on taking, I,e quantities etc
I'm also quite interested in looking at brain plasticity, relearning and almost re programming mentally, if anyone can help?


Hmm... I just got an idea here... Kappa Opioid ANtagonists supposedly work by impairing the neural networks that govern learned response to negative stimuli - i.e they make it harder for you to feel punishment - meaning that phobias and anxieties will no longer have the same hold of you, and you can start learning to overcome them.

And dihexa promotes synaptic growth... enhancing learning.

In theory, shouldn't two such compounds be highly synergistic?

There's currently a group buy -thread being organized for Cerc-501 - a compound with such an action - have a look and see what you make of it, yeah?

 


Edited by tautomeric, 28 July 2016 - 10:15 PM.


#29 Stinkorninjor

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Posted 29 July 2016 - 06:19 PM

Yep - Kappa opioid antagonists are being researched as anxiolytics and antidepressants as well - they should be particularly effective in combatting phobias and OCD.

A few days on CERC-501 could, in theory, be the equivalent of YEARS of CBT and DBT.

There is a legendary drug called Jdtic, a kappa-antagonist that had a "half-life" of several weeks...! The few psychonauts that tried it reported incredible results.

So did the clinical trials - however, they also reported a very serious side-effect: ventricular tachycardia.

CERC-501 is one of the latest attempts to recreate this incredible drug - but without this side-effect.

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#30 MoreNowAgain

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Posted 11 August 2016 - 10:06 PM

There's 5 more people interested in this group buy

 

http://www.reddit.co...in_a_group_buy/


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