184 replies to this topic

[Yuri Ericson]

Will pay up to $250 for 500 mg

 

[tolerant]

Guys, 

 

Thanks for your interest. With the quotes I've got, the minimum for a 500 mg amount will be $350 if we get about 20 people involved, and $500 if we get 10 involved. Please up your bidding!

 

Note that a dose of 10 mg will result in 94% saturation of your kappa-opioid receptors post-dose and the half-life of the substance is 30-40 hours: https://en.wikipedia.org/wiki/CERC-501

 

 

Edited by tolerant, 13 August 2016 - 10:15 AM.

[samson75]

But this substance has failed it third tests procedure hasn't it ?

It did not have significant advantage against placebo except in high doses, and even there

the impact on depression was not extraordinary.

[Mind_Paralysis]

But this substance has failed it third tests procedure hasn't it ?

It did not have significant advantage against placebo except in high doses, and even there

the impact on depression was not extraordinary.

 

Ah, but that was depression! A degenerative disease, requiring neurogenesis to be healed.

 

Me personally, I think it would help with PTSD, anxiety and learned helplessness - because the kappa opioid receptors control punishment, instead of reward.

 

I've got a genetic neuro-malformative disease called CDD - Concentration Deficit Disorder - this disease, because of environmental pressure, leads to aquired anxiety, something even akin to PTSD (but not quite), a form of situational shyness, which is triggered by activities which are difficult to perform when you have the disease - i.e, learned helplessness.

 

We become PUNISHMENT-sensitive!

(in contrast to adhd-ers who become reward-sensitive, always seeking new thrills, we instead seek to avoid punishment)
 

 

CERC-501 should blunt punishment sufficiently to allow a person such as me, when medicated with a norepinephrinergic like Atomoxetine, to go through previous failures, disarm their paralysing effect, and become a new, more dynamic person.

 

 

I think the testing on Anxiety and PTSD, perhaps even OCD (as those who have it, feels something truly bad will happen if they don't do their OCD-rituals - but if they feel less punishment...) will go much better than with Depression.

[samson75]

thanks for the clarification. I've had a terrible daily anxiety/social anxiety/stress for years. This is what lead to depression for me, which is now installed and not properly cured by SSRI's.

Do you think this substance could be useful for my condition ?

 

 

Edited by samson75, 13 August 2016 - 02:02 PM.

[Mind_Paralysis]

thanks for the clarification. I've had a terrible daily anxiety/social anxiety/stress for years. This is what lead to depression for me, which is now installed and not properly cured by SSRI's.

Do you think this substance could be useful for my condition ?

 

It's possible - it is supposed to be used as an adjunct to SSRI's as well, I believe? I guess it depends on what you would say causes your anxiety? Have you always been anxious, or is it something that started happening in recent years?
 

I think, theoretically, that what CERC-501 will do, is to start removing any feelings of guilt or shame, which you may have unjustly been burdened with.

 

Now, if you have ADHD, SCT, ASD, maybe even low-level impairing Neuropsychiatric disorders such as pure Dyslexia, Dyscalculia or DCD, it will probably help with those feelings of guilt - of not being able to live up to your own or someone elses expectations.

 

Might be able to help with certain other traumas as well.

 

The anxiety just have to stem from punishment, guilt, or learned helplessness. (they're all sort of the same thing)

Edited by Stinkorninjor, 13 August 2016 - 04:52 PM.

[samson75]

It's a very ancient anxiety that always worsens. Mainly caused by social inadequacy/awkardness. The depression that followed has been there for almost a decade. I might try this; i have nothing to loose...

Edited by samson75, 13 August 2016 - 05:35 PM.

[satsumass]

Will up my bid for 500mg to $350!! Hope we can make this happen

[Yuri Ericson]

Would this inhibit effects of adderal? I can't seem to find any info on this. With my cursory knowledge of pscyopharmacology it doesn't seem like it would inhibit nor potentate. If this is correct, I'm in for $350 for 500 mg.

[samson75]

I'm in too. 350$ for 500mg.

[Mind_Paralysis]

Would this inhibit effects of adderal? I can't seem to find any info on this. With my cursory knowledge of pscyopharmacology it doesn't seem like it would inhibit nor potentate. If this is correct, I'm in for $350 for 500 mg.

 

This is a good question.

 

@Tolerant: do we have ANY metabolism data? I can't find anything on the metabolism of CERC-501 at all - but it does seem to play along well with a few SSRI's.

Wait... that might be it! Which SSRI's is it intended to be used with? We can then check out their metabolism, and then perhaps draw some conclusions regarding CERC-501 in relation to Amphetamine.

 

Also, for those more chemically trained than I, the molecular structure should shine some light on the metabolism as well, yes?
 

EDIT: Here we go... the two SSRI's are supposed to be Citalopram and Imipramine, according to wikipedia... : \

 

Antagonists of the kappa opioid receptor

http://www.sciencedi...960894X14002674

 

LY2456302 is the old name for CERC-501. REALLY good paper btw...! Really goes into depth, and all available in free full-text! : D

I can't find jack sh*t about what it's supposed to be augmented with either. The paper mentions reference #28.

 

https://clinicaltria...Y2456302&rank=1

 

However, there's NOTHING in there about combinations either. Can someone with a less burnt-out mind check the links and see if I've simply missed it?

 

 

Edited by Stinkorninjor, 14 August 2016 - 09:19 AM.

[Yuri Ericson]

I don't have time to find/post the reference now, but I read last night, after this post, that Kappa activation inhibits Amphetamine. It is possible then that a Kappa antagonist (CERC-501) would either be neutral or potentiate. I will try to post reference later today. In a bit of a rush.

I meant to write: Kappa activation inhibits dopamine. Reference pending.

Edited by Yuri Ericson, 14 August 2016 - 01:22 PM.

[tolerant]

But this substance has failed it third tests procedure hasn't it ?

It did not have significant advantage against placebo except in high doses, and even there

the impact on depression was not extraordinary.

 

I think you're confusing CERC-501 and ALKS 5461. CERC-501 hasn't failed anything because there hasn't yet been a trial for it other than to establish safety and pharmacological parameters. Clinicaltrials.gov shows that there was one TRD trial which was terminated.

[samson75]

Thanks for the clarification.

Edited by samson75, 14 August 2016 - 01:57 PM.

[Yuri Ericson]

Here is the reference affirming that kappa agonists inhibit dopamine.

"Stimulation of kappa-opioid receptors, the endogenous receptor for the dynorphin-like peptides, inhibits dopamine release in the striatum (nucleus accumbens and caudate putamen) and induces a negative mood state in humans and animals."

http://www.ncbi.nlm....les/PMC2787673/

[GreenWhite]

in for 350 dollars.

[John Felipe]

I would be willing to pay $200. A small price for giving me life after anhedonia.

[Mind_Paralysis]

RIGHT then! =) I'm feeling a bit better from the burnout, but I do notice that any sorts of setbacks or punishment still cause severe, *severe* anhedonia and demoralisation.

 

KOR-antagonism is the key there - kicking its arse should sort me out.

 

So, where we at when it comes to this experiment? I'm willing to start spreading the word and getting people interested.

 

 

Checking the peeps in this thread, as well as other forums, these are the folks so far:

 

Those who are IN:

1. satsumass - $350

 

2. MoreNowAgain - $250

3. Stinkorninjor - $150

 

4. tolerant - $250

5. Yuri Ericson - $250

 

6. samson75 - $350

 

7. GreenWhite -  $350

 

8. John Felipe - $200

 

 

Those who are interested:

9. Der Springende Punkt

 

10. alex921

 

11. OceanFixNow99 (Reddit)

 

12. thagodjbone (Reddit)

 

13. gabeavers (Reddit)

 

14. scoobyafinil (Reddit)

 

15. sunflower162 (Reddit)

 

16. HarryDerHaarige (Reddit)

 

 

List of other forums with participators:
 

Reddit

https://www.reddit.c...in_a_group_buy/

 

 

I'm going to try and drum up some interest on Drugs forum myself, and will try and report back with any new interested parties. Meanwhile, maybe MoreNowAgain can try and message some people and give an update on Reddit? To let them know that this isn't dead, and that we're recruiting participants.

 

On another note: It's great to see the list swelling! = ) Already we've potentially got 16 peeps willing to pay for a synthesis and testing - it should be noted though, that I think a group buy needs about 30 people to truly get running - so we're only halfway there. Preferrably I'd say something akin to 50...! people, to truly get a good amount of the chemical at an affordable price.

Edited by Stinkorninjor, 09 October 2016 - 07:20 PM.

[Strangelove]

Kappa antagonism is the next "big thing" I want to try, for stress that other compounds cannot touch, and indirect mood boost... Very exciting! Hopefully this group buy will happen and I ll have the extra money to chip in soon.

[Severious]

I'm interested in this as well

[Der Springende Punkt]

Alkermes plc (ALKS) Announces Third ALKS 5461 Phase 3 Met Primary Endpoint in Major Depressive Disorder

[YoungSchizo]

Alkermes plc (ALKS) Announces Third ALKS 5461 Phase 3 Met Primary Endpoint in Major Depressive Disorder

Finally, great news! Almost lost hope with the other two studies "failing"!

[Mind_Paralysis]

 

Alkermes plc (ALKS) Announces Third ALKS 5461 Phase 3 Met Primary Endpoint in Major Depressive Disorder

Finally, great news! Almost lost hope with the other two studies "failing"!

 

 

Hmm, interesting note here, btw - I just realized that maybe Kappa-antagonism can help with an aspect of schizotypy which is a bit unexpected...

 

If you have hard to treat positive symptoms - voices telling you that you suck, et c, then, perhaps... Kappa antagonism can change them - or at least the way you respond to the hallucinations, and then in turn their nature.

 

In places like Africa and India, where family-structure, society and beliefs, differ from the West, many schizo's actually report a DIFFERENT quality to their delusions: they are actually more benign.

 

Some of the angst and pain and depression that comes from schizo, is apparently cultural... Christianity really did a number on our civilization.
 

In Africa at least, there is a faith in spirits, natural and familial, which then extends to the schizos: they believe the voices are their deceased loved ones, trying to help them in their life - telling them jokes and giving advice in tricky situations.

 

Now, I probably shouldn't be saying this, because, HELL, it probably won't work, but maaaaybe, maaybe... Kappa-antagonism will change the way you respond to the voices? (if you have them) - living with Schizo wouldn't be half as hard if the voices were actually COOL for once, instead of being DICKS, like they are here in the West.

 

There might be something to it though - if you feel no punishment, then how can you fear the voices? How can they hurt you? The answer is, perhaps, in no fucking way whatsoever.

[YoungSchizo]

I'm schizoaffective, who knows, I'm at least glad ALKS is a whole different substance than available now for depression.

Funny you mention that voices can change, mine changed three times, each time my psychosis changed. It turned from evil, to healing, to helpful. (Not putting a meaning to it, it's still confusing as fuck)

[William Finch]

I would go in on this. What's the status?

[Mind_Paralysis]

I would go in on this. What's the status?

 

Still recruiting! = )

 

Tolerant hasn't been on for a while, so I'm guessing he might not be feeling well enough to deal with the particulars of the group buy, but I'm getting better so I'm up for continuing the struggle to get this on.

 

I'll see if I can get a hold of him through e-mail, and let him know the recent developments.

[tolerant]

Indeed I haven't been well enough to handle the logistics of a group buy. There's not enough people anyway. Also, my attempts to recreate the effects of ALKS-5461 with buprenorphine and naltrexone have largely been unsuccessful, although I have given up completely yet. I don't advise anyone try and do this unless you've researched this very thoroughly. And start with the smallest dosage. If my experiments with buprenorphine/naltrexone went better, I would have fronted the cost of the group buy, but that hasn't happened. Sorry guys.

[William Finch]

That combination is just called suboxone in the states. Having been on it for over a year about ten years ago the withdrawals sucked, and were prolonged.  It's a K antagonist, but also a partial U-agonist, which I believe is where the painful withdrawals come from. How long have you been on it? What dose? I have no interest in any compound similar to suboxone, but I think (perhaps wrongfully) the k antagonists like Jdtic don't lead to withdrawal. Having used buprenorphine under the care of a doctor when suboxone was somewhat new 10 years ago be aware that if you use buprenorphine regularly you will get dope sick when you quit. It's not as intense as heroin, but it lasts much, much longer. 

Edited by William Finch, 09 November 2016 - 03:36 AM.

[tolerant]

That combination is just called suboxone in the states. Having been on it for over a year about ten years ago the withdrawals sucked, and were prolonged.  It's a K antagonist, but also a partial U-agonist, which I believe is where the painful withdrawals come from. How long have you been on it? What dose? I have no interest in any compound similar to suboxone, but I think (perhaps wrongfully) the k antagonists like Jdtic don't lead to withdrawal. Having used buprenorphine under the care of a doctor when suboxone was somewhat new 10 years ago be aware that if you use buprenorphine regularly you will get dope sick when you quit. It's not as intense as heroin, but it lasts much, much longer. 

 

Suboxone is actually a combination of buprenorphine and naloxone, with naloxone being inactive when taken orally. I've been using buprenorphine and naltrexone sparingly, I'm not continuously on any dose, but I haven't gone higher than 0.5 mg buprenorphine and 5 mg naltrexone. Although it alleviates anxiety to a degree, I get this unusual effect of a really unpleasant stupor which can come on at random times and last for a few hours. I also cannot tell the difference between taking buprenorphine alone and taking it with naltrexone. That tells me that perhaps naltrexone is not really good at blocking u-opioid receptors and the relief I get is mainly from buprenorphine acting on those receptors, which is not something I want because of the issues of tolerance and withdrawal.

 

Unfortunately, there is no data of which I'm aware that would suggest that kappa-opioid antagonists like CERC-501 will not itself cause tolerance and withdrawal, but at least it's worth a shot.

[hnk6]

Anyone interested in a Hydroxynorketamine group buy? Then click here:

http://www.longecity...e-2#entry794605