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CERC-501 Kappa Opioid Antagonist Groupbuy

kappa opioid

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#1 brighterpath

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Posted 02 April 2017 - 11:21 AM


We are going ahead with the groupbuy of CERC-501, a kappa opioid antagonist, and wanted to see if there was any last minute interest from the Brain Health forum. 

 

A few members of the Mental Health forum have been organizing this group buy for a while (http://www.longecity...e-3#entry810988), and we are finally pushing through with the synthesis after this weekend. The original poster, Tolerant, has been recovering from an illness for a while, and has entrusted the organizational duties to me. We have currently raised over $2200, but was hoping to get a few more people involved to bring down the synthesis price further and leave room for NMR testing once the compound arrives. 

 

The lab has quoted us the following prices:

Price: 500 USD/100mg, 900 USD/500mg,  1800 USD/1gram,  2800 USD/2grams,  3700 USD/3grams,  4000 USD/4grams, 4500 USD/5grams.

 

During clinical trials, researchers used 10mg for daily dose, so 300mg should be about a month's supply of the drug. 

 

You can find more information about the compound here. https://en.wikipedia.org/wiki/CERC-501

If anyone is familiar with jdTic, CERC-501 should be similar to being a heart friendly and shorter acting version of the drug. 

 

Please let me know if there are any questions or concerns. 

Brighter

 

 


Edited by brighterpath, 02 April 2017 - 11:22 AM.

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#2 Ben

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Posted 02 April 2017 - 06:05 PM

Hi There,

 

Is my math correct: $420 for a month's supply?



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#3 brighterpath

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Posted 02 April 2017 - 06:51 PM

At the current buy level, yes, that would be correct Ben.

#4 Junipersun

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Posted 02 April 2017 - 07:21 PM

Why would you pay $420 for a month of relief? What part am I missing here? Do you all battle addiction problems? That would make sense to me. But other than that? Are there any long term benefits for depression/anxiety/ocd/phobias?



#5 brighterpath

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Posted 02 April 2017 - 07:44 PM

Kappa opioid antagonists are the long sought after gold standard for people suffering from derealization/depersonalization,and is being looked at as a novel and extremely promising drug for treatment refractory depression. It is also thought to have nootropic and anixiolic properties as well by increasing the dopamine levels in the limbic system.

Many people participating in the buy probably have exhausted all other options, or want to try a new mechanism, and since this buy has never been done before, we are willing to pay some premium to be the first. If it is successful, I'm sure we will be organizing larger buys in the future where the price is lower as well.
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#6 tolerant

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Posted 03 April 2017 - 03:54 AM

Hi everyone,

 

If anybody has any lingering doubts about this group buy, I can confirm that I have personally entrusted the organisation of this group buy to brightpath. I started the group buy thread way back in about July last year and my goal was to raise $7000 which would give people 50 days' supply for $350. However, that required the participation of 20 people each giving $350, and it turned out that this way never going to happen. Since the lab's minimum quantity for a synthesis at that time was 5 g, even a smaller group buy required the participation of 10 people each giving $500, which was also not going to happen. A number of people expressed their interest last year, however the amounts they were willing to contribute were too low to make the group buy happen in the way I envisaged it.

 

In about October last year I wrote in the thread that I had no energy to continue as the organiser in any event because of the current status of my health condition. At that point, everything that I collected to to make the group buy happen was public knowledge, including information about the compound, the identity of the lab and the pricing which I had negotiated. However, the thread lingered until late last month, with new people occasionally expressing their interest, but nothing else happening.

 

That was until brightpath came along virtually a week ago and stated in a personal message to me and in the thread that he would like to see this group buy happen ASAP and to that end he was willing to put in a large amount of money (several times that of the next highest contributor, which is myself). He also resumed negotiations with the lab and we found out that their pricing policy had changed in that the compound became a little cheaper and the minimum amount the lab was willing to produce went down drastically from 5 grams to about 500 mg, which made a small group buy possible. I told him that since at this point in time he's got the most drive and is putting in the greatest financial contribution (by far) to see this happen in the quickest time possible, he should be organising the group buy. We thought about the idea that I should collect the money as the more senior member with documented history of ordering an testing compounds synthesised by labs, including this particular lab, but I said that I was not currently able to do organising duties and anyway that would create an unnecessary logistical step in the process. So he has my full blessing to be the new organiser of this group buy.

 

At the moment, brightpath has collected about $2250 from about five people, including myself. We have decided that we will set a very tight deadline on the collection of funds, which is this weekend (if you still have doubts, if brightpath's intentions were not genuine, he would let this group buy linger to collect more money). I have exchanged about 20 emails with brightpath and have no doubts about his integrity and motivation for this. The motivation for both him and myself is that we have tried everything possible for our respective conditions and CERC-501 is a promising compound that we would like to try, but we can't wait forever. So as I said we decided to set a very tight deadline and go ahead with the group order by that deadline irrespective of the amount raised. Because the group buy will be smaller than envisaged, unfortunately the cost of participating will be greater than that I first envisaged way back last year. This is obviously how lab pricing works. The CERC-501 buy thread has been active on the Brain Health forum for about 9 months. As brighpath said in this thread, if at the end it turns out that we are only a small group of people willing to be the first to get this done, we will have to settle on ordering a smaller overall quantity and thus pay a premium on the price.

 

I have given brightpath little pieces of advice here and there (although he is an intelligent university student perfectly capable of organising the group buy himself). It was my suggestion that he start a thread in the Mental Health forum, because it would generate more attention than the current thread in the Brain Health subforum. The purpose of this thread is to hopefully get some people interested at the last minute, because if more funds can be raised, the price of the synthesis will be cheaper and people will get more of the substance for their respective contributions. I also think that if not for this thread, people interested in the compound who don't monitor that Brain Health forum would have missed the thread there and then be "kicking themselves" once they found out that the group buy went ahead.

 

So all I can say is "jump on board". Brighpath has my trust along with the trust of about five other people who have already contributed funds. At any rate, as far as I understand it, PayPal has a charge back system which would allow people to recoup their money if this group buy was in any way not genuine. I understand the concerns of people over contributing money in such haste to a newcomer to the forum (I would no doubt have the same concerns had I not the chance to get to know brighpath over email during the past week or so), but I'm happy to advise everyone that to my judgment everything here is above board.


Edited by tolerant, 03 April 2017 - 04:33 AM.

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#7 cetacean

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Posted 03 April 2017 - 06:26 PM

Hi there.  I have been learning about the kappa receptor and believe I may benefit from this.   I would like to join the group buy.  



#8 cetacean

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Posted 03 April 2017 - 07:55 PM

So...if it is not too late, I will definitely go in for $200-250.  And would even go to $300 if got us a larger quantity purchase.


Edited by cetacean, 03 April 2017 - 07:57 PM.


#9 brighterpath

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Posted 03 April 2017 - 08:41 PM

Just responded to your message cetacean! I will likely be going through the negotiation process with the lab tonight. 



#10 Mind_Paralysis

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Posted 03 April 2017 - 11:04 PM

I am currently in deep contact with BrighterPath as well! = ) I am, so far, of the same opinion as Tolerant - Bright' actually seems to be a legit and sincere guy.



#11 tolerant

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Posted 05 April 2017 - 02:18 AM

I have a duty to inform everyone that when I looked up clinical trials involving CERC-501 today, I was reminded that the proof-of-concept treatment treatment-resistant depression study of CERC-501 has been terminated. I guess the reason for termination can range from lack of funds to the inability by researchers to proof the usefulness of the intervention which manifests itself early and the study is abandoned to avoid the spending of further funds. I posted about this as far back as August of last year, but it might have been lost in the fine print and forgotten by now. However, there is a CERC-501 anhedonia trial currently recruiting, along with one on smoking. Today I wanted to contact Maurizio Fava, MD, who was responsible for the depression trial to find out the reason for termination, however one peculiarity of American universities and I guess other organisations is that they don't give out emails of their staff. I don't feel comfortable contacting him by phone about this matter, not to mention vast time zone differences between Australia and the US.

 

However, the positive results of animal trials referenced on its Wikipedia page do suggest this drug's antidepressant efficacy. We also know from a previous nicotine withdrawal trial that the drugs is safe: "CERC-501 was generally well-tolerated with no serious adverse events reported and no discontinuations due to adverse events with CERC-501. The most commonly reported adverse events, over 5% and greater than placebo in the study, were diarrhea and decreased appetite."

 

I have also come across several anecdotal reports of people being able to achieve attenuation/complete remission of their DP/DR symptoms using a combination of buprenorphine and naltrexone to mimic KOR antagonist activity. My own attempts to achieve relief from anxiety/depression by these means largely failed, which information I have also posted earlier, but feel obliged to repeat. 

 

On the plus side, however, we've got Stinkorninojor's conviction that this drug will end all ills, which is as far as I can gather based on anecdotal reports of people who managed to try JDTic.


Edited by tolerant, 05 April 2017 - 02:27 AM.

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#12 brighterpath

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Posted 05 April 2017 - 04:10 AM

I have actually been able to obtain the Dr. Fava's email, so I'll send that your way Tolerant. However, looking at the way the terminated study was designed, I immediately notice that the study was only supposed to give drugs to people for three days, which seems like a critical flaw for studying treatment refractory depression, for which you would normally expect weeks for effects of any drug to manifest. Inappropriate trial designs are often grounds for early termination of trials. All of the other studies look at the effect of CERC 501 over at least 2 weeks, up to 8 weeks. 

 

As another promising sign, the ALKS 5461 trial showed efficacy in the depression trial. For those unfamiliar, this drug was the samidorphan/buprenorphine mix, which is an improved version of naltrexone/buprenorphine mix. The main problem with Naltrexone/buprenorphine combo is that buprenorphine has a higher MOR affinity than Naltrexone, so it can't effectively stop buprenorphine binding to the site. Samidorphan fixed this problem. They had some trouble in the first two trials, so there are some lingering doubts, but they claim it was due to trial design errors and higher than expected placebo effect. 

 

Moreover, with MOR and KOR being extremely closely related in function, I would venture to guess that strict KOR antagonism may have a different effect then also having MOR antagonism/agonism involved. I am still very hopeful!


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#13 tolerant

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Posted 05 April 2017 - 04:53 AM

I knew I could have been more persistent in searching for M. Fava's email. I've already written to him. Can't see any good reason he'll disclose any further information to an ordinary guy, not to mention he may well be subject to confidentiality duties. But it's worth a shot.

 

Yes, M. Fava's study was designed to last only 3-6 days. On the other hand, given M. Fava has authored heaps of studies, why would his design turn out so poor?

 

I agree with brighterpath that buprenorphine has a higher affinity for MOR than naltrexone, so it will displace/stop naltrexone at MOR binding sites. I remember coming across this information.

 

I think a source of additional hope comes from what we know about KOR agonists. According to this article, they cause "dysphoria, hallucinations and psychotomimetic effects" (first paragraph of section 4). So it would only make sense that KOR antagonists would cause the opposite effects.

 

Edit: grammatical/typing error.


Edited by tolerant, 05 April 2017 - 04:59 AM.


#14 brighterpath

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Posted 06 April 2017 - 04:28 AM

Hello everyone, 

 

Just wanted to let you know that the order has been placed with the lab! This group buy has officially gone through!

 

The lab has guaranteed 98% purity of the compound, and an internal quality control report on the substance from their end, which should include an NMR testing report. We will do our separate NMR testing as well, and I will start looking into that soon. The cost of the lab test will likely be added onto the total, but should run no more than $300 to $400. Synthesis should take between 3 to 4 weeks. 

 

If anyone else would still like to participate, please let me know. I have personally fronted a large sum, and would be happy to part with some shares. 

Thank you everyone for coming together! I will let you know if there are any important updates. 


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#15 brighterpath

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Posted 06 April 2017 - 08:30 AM

And please let me know if there are any questions.


Edited by brighterpath, 06 April 2017 - 08:38 AM.


#16 tolerant

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Posted 08 April 2017 - 12:25 AM

I knew I could have been more persistent in searching for M. Fava's email. I've already written to him. Can't see any good reason he'll disclose any further information to an ordinary guy, not to mention he may well be subject to confidentiality duties. But it's worth a shot.

 

I wrote to Professor Fava and his only response was to contact Andy Krystal to ask him whether there are any news with regards to his CERC-501 study. I have now written to Dr. Krystal and will post here once he answers.



#17 Mind_Paralysis

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Posted 08 April 2017 - 01:44 PM

Hello everyone, 

 

Just wanted to let you know that the order has been placed with the lab! This group buy has officially gone through!

 

The lab has guaranteed 98% purity of the compound, and an internal quality control report on the substance from their end, which should include an NMR testing report. We will do our separate NMR testing as well, and I will start looking into that soon. The cost of the lab test will likely be added onto the total, but should run no more than $300 to $400. Synthesis should take between 3 to 4 weeks. 

 

If anyone else would still like to participate, please let me know. I have personally fronted a large sum, and would be happy to part with some shares. 

Thank you everyone for coming together! I will let you know if there are any important updates. 

 

Awesooome! : D

 

Oh man, I really, really hope this works out! This could mean so much... Well, if the compounds works, lol! But, unless we do this, we might never ever know...
 



#18 Mind_Paralysis

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Posted 12 April 2017 - 02:38 PM

YO! Brighterpath - have you started looking into NMR-testing? And does the lab have any updates regarding their progress on synthesis?



#19 brighterpath

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Posted 13 April 2017 - 08:27 AM

Hey Stink,

Yes, I've been scoping out a few places but nothing definitive yet. Should have something within a week though.

The lab has said everything is coming along as scheduled. I will let you know I'd there are updates.

#20 brighterpath

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Posted 19 April 2017 - 02:44 PM

Hello everyone,

 

I contacted that lab and they said they have two steps left in the synthesis, and if all goes well, we should have our compound by next week. I am also currently in talks with several labs about NMR testing. I will keep you updated if anything else comes up. 



#21 Mind_Paralysis

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Posted 19 April 2017 - 06:39 PM

Hello everyone,

 

I contacted that lab and they said they have two steps left in the synthesis, and if all goes well, we should have our compound by next week. I am also currently in talks with several labs about NMR testing. I will keep you updated if anything else comes up. 

 

Good to hear, good to hear.
I am very pleased to hear that all is progressing according to plan. = ) Keep us updated!

 

Hmm... this gets me thinking - how is everyone doing? I'm currently in a bit of a fluctuating state - about a week ago, I was active and functional for a few days on my drugs (atomoxetine and tianeptine), but then I went up to the max dosage and since then it's rather peculiar... not quite depressed any more, but mostly just passive and sedated, some OCD, some anxiety, some negative thoughts, but not that many.

 

Mostly ok, just truly tired of being under the rule of Atomoxetine, but not near-suicidal any more (atx's side-effects were really pushing me towards the edge there for a while - but I've stuck through most of it)

 

 

I'm especially worried about Tolerant actually! : O He seems to be in a really, really bad place, and it seems as if he's been there for a long while now - I hope he can hold out for just a little while longer! Soon, Tolerant... Soon...


Edited by Stinkorninjor, 19 April 2017 - 06:41 PM.


#22 tolerant

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Posted 19 April 2017 - 07:26 PM

I hesitate to say how I am. I would like to think I'm better, but it's too early to say. Thinking about trying Nardil...



#23 brighterpath

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Posted 28 April 2017 - 01:06 AM

Please see the following update:

 

http://www.longecity...e-4#entry813886



#24 Hip

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Posted 28 April 2017 - 01:40 AM

Kappa opioid antagonists are the long sought after gold standard for people suffering from derealization/depersonalization,and is being looked at as a novel and extremely promising drug for treatment refractory depression.

 

Have you looked into amentoflavone, which is a kappa opioid antagonist? It is available as a supplement.



#25 tolerant

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Posted 28 April 2017 - 02:01 AM

 

Kappa opioid antagonists are the long sought after gold standard for people suffering from derealization/depersonalization,and is being looked at as a novel and extremely promising drug for treatment refractory depression.

 

Have you looked into amentoflavone, which is a kappa opioid antagonist? It is available as a supplement.

 

 

I remember reading something negative about amentoflavone; I think it might have been this.



#26 gamesguru

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Posted 28 April 2017 - 02:17 AM

On the plus side, however, we've got Stinkorninojor's conviction that this drug will end all ills, which is as far as I can gather based on anecdotal reports of people who managed to try JDTic.

 

he says that about a lot of upcomers thou

 

 

Have you looked into amentoflavone, which is a kappa opioid antagonist? It is available as a supplement.

 

yes funny you should mention it.  with a Ki of over 1000nM and a plasma-to-brain ratio of 2%[2] i'm afraid it's pretty hopeless.  if you're looking for something with more activity at the kappa site, (+) catechin[3] is just 320nM.  still a pretty bad P-B ratio, around 6% maybe


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#27 Mind_Paralysis

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Posted 28 April 2017 - 07:37 AM

 

On the plus side, however, we've got Stinkorninojor's conviction that this drug will end all ills, which is as far as I can gather based on anecdotal reports of people who managed to try JDTic.

 

he says that about a lot of upcomers thou

 

 

Alas, yes - my enthusiasm seems to get the better of me a lot of the times. : [

I do feel I have improved a bit with this though - but sure, I've still got a long way to go with this - sometimes I've spread actual disinformation, like when I suggested 23andme for genetic testing for ADHD - turns out I knew too little about the gene-variants and the sort of data specific testing-facilities can actually produce.

 

I rather regret some of these things now - a healthy dose of skepticism is a good thing to always have at the ready in the back of your minds, gentle-folks!
 


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#28 brighterpath

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Posted 01 May 2017 - 08:54 PM

Great news:

 

http://ir.cerecor.co...eases/detail/36



#29 brighterpath

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Posted 19 May 2017 - 04:54 AM

Hey everyone,

 

I got the news from the lab last night that all of the testing is finally complete, and the compound is ready for shipping. I'm sorry about the weeks of delays. The lab kept having to repurify the compound and retest the compound, but from the results they have sent me, we have a 99+% pure product. 

 

I will let you know when it finally gets here. Hopefully it will be by Monday or Tuesday at the latest. Once I have it, the compound will be shipped for NMR testing immediately for verification, and I will send them out to you at the same time. 

 

If you have not done so, please send me your shipping address, and the exact amount of the compound you want given the new pricing (http://www.longecity...e-4#entry813886)

 

Let me know if you have any questions or concerns,

Brighter


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#30 brighterpath

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Posted 26 May 2017 - 03:40 AM

I received the compound earlier this week. The compound has been sent for NMR testing and all of the US orders have been shipped and should be arriving tomorrow. The international orders will be shipping tomorrow morning and hopefully you will be receiving it next week. I will provide tracking information when I can. 

 

Good luck everyone.


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