# CERC-501



## hennessy (Apr 2, 2008)

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

Elliott mentioned me that and it sounds promising.

Do you think it will be a cure or relief for dp? Do you think it's going to be avaible anytime soon?


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## TDX (Jul 12, 2014)

It's a kappa-opioid antagonist, so it might be useful against depersonalization. The problem is that it might also fail in depression trials like ALKS-5461.

It's investigated for several disorders, but it didn't reach phase 3 in any of them yet. So it might take 2 to 3 years until it becomes available, if it does not fail in phase 3 trials like ALKS-5461.


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## hennessy (Apr 2, 2008)

TDX said:


> It's a kappa-opioid antagonist, so it might be useful against depersonalization. The problem is that it might also fail in depression trials like ALKS-5461.
> 
> It's investigated for several disorders, but it didn't reach phase 3 in any of them yet. So it might take 2 to 3 years until it becomes available, if it does not fail in phase 3 trials like ALKS-5461.


Don't you think it might be avaible before 2 years?


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## utopia (Mar 7, 2016)

It is promising, mainly because it has been generally well tolerated in three human clinical trials.

Computational insights into different inhibition modes of the κ-opioid receptor with antagonists LY2456302 and JDTic:



> Among the κ-OR selective antagonists, JDTic is a failed antidepressant with a short drug-target residence time (RT), whereas LY2456302 exhibits better effects with a longer RT than JDTic.
> 
> Through detailed analyses of the simulations, a strong but single interaction mode was found to be responsible for the adverse effects and short RT of JDTic, which could be considered as an alert for other chemotypes, whereas LY2456302 was more advanced, mainly due to its multiple metastable states.


Unfortunately, it won't be available soon as TDX previously stated.


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## Max XR (Apr 9, 2016)

Possible to source this chemical, no?

I know multiple labs who do custom synths but... it's pricey.


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## hennessy (Apr 2, 2008)

Travis Scott said:


> Possible to source this chemical, no?
> 
> I know multiple labs who do custom synths but... it's pricey.


Are they trustable? How do we know if the thing we get is CERC-501 and not something else?


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## TDX (Jul 12, 2014)

I wouldn't let a lab create CERC-501, because it's a kappa-opioid-antagonist and we can already have this with Buprenorphine. There are other interesting drugs, with unique effects available drugs cannot achieve, where the lab-way might be more reasonable. The high price might be reduced by organizing a group buy. This was done on longecity.org multiple times.



> Are they trustable? How do we know if the thing we get is CERC-501 and not something else?


In a group buy this problem could be reduced to a degree by randomly choosing some participants which act as "food tasters" - which means they take the drug before the others and report the effects.


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## Max XR (Apr 9, 2016)

TDX said:


> I wouldn't let a lab create CERC-501, because it's a kappa-opioid-antagonist and we can already have this with Buprenorphine. There are other interesting drugs, with unique effects available drugs cannot achieve, where the lab-way might be more reasonable. The high price might be reduced by organizing a group buy. This was done on longecity.org multiple times.
> 
> In a group buy this problem could be reduced to a degree by randomly choosing some participants which act as "food tasters" - which means they take the drug before the others and report the effects.


if such a thing was ever organized, i would totally try it despite the risks.


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## hennessy (Apr 2, 2008)

Travis Scott said:


> if such a thing was ever organized, i would totally try it despite the risks.


I'm actually in for CERC-501.

What else can we want them to create?


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## Max XR (Apr 9, 2016)

hennessy said:


> I'm actually in for CERC-501.
> 
> What else can we want them to create?


 Really depends on their labs capabilities.


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## TDX (Jul 12, 2014)

> if such a thing was ever organized, i would totally try it despite the risks.


I would do to, if all conventional treatments fail. If the substance has passed phase I I suppose it's relatively safe.



> I'm actually in for CERC-501.
> 
> What else can we want them to create?


I'm against CERC-501, because you can already have this by using Buprenorphine-Naltrexone. I wouldn't waste money for something you can already have by conventional means. There are other interesting substances like NSI-189, which you cannot get by conventional means, so they are preferred targets for custom synthesis.


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## Max XR (Apr 9, 2016)

TDX said:


> I would do to, if all conventional treatments fail. If the substance has passed phase I I suppose it's relatively safe.
> 
> I'm against CERC-501, because you can already have this by using Buprenorphine-Naltrexone. I wouldn't waste money for something you can already have by conventional means. There are other interesting substances like NSI-189, which you cannot get by conventional means, so they are preferred targets for custom synthesis.


 I don't really like the whole buprenorphine thing because bupe tends to spike my DP and makes it difficult to piss and shit.

Least favorite opiate, recreationally... couldn't bare to stand it as a med for my DP.


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## hennessy (Apr 2, 2008)

TDX said:


> I would do to, if all conventional treatments fail. If the substance has passed phase I I suppose it's relatively safe.
> 
> I'm against CERC-501, because you can already have this by using Buprenorphine-Naltrexone. I wouldn't waste money for something you can already have by conventional means. There are other interesting substances like NSI-189, which you cannot get by conventional means, so they are preferred targets for custom synthesis.


Can you explain us NSI-189 and why do you think it'd work?


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## TDX (Jul 12, 2014)

> Can you explain us NSI-189 and why do you think it'd work?


I stimulates neurogenesis and according to Wikipedia is not only investigated for the usage against depression, but also for traumatic brain injury, Alzheimer's disease, post-traumatic stress disorder, stroke, andnatural cognitive and memory decline in aging.

There also a few anecdotal reports where it helped against depersonalization.


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## hennessy (Apr 2, 2008)

TDX said:


> I stimulates neurogenesis and according to Wikipedia is not only investigated for the usage against depression, but also for traumatic brain injury, Alzheimer's disease, post-traumatic stress disorder, stroke, andnatural cognitive and memory decline in aging.
> 
> There also a few anecdotal reports where it helped against depersonalization.


When do you think it'd be avaible?

The combo of CERC-501/ALKS and NSI-189 might be promising when avaible.


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## TDX (Jul 12, 2014)

> When do you think it'd be avaible?


They are conducting phase II trials by now, so I think in 3 or 4 years if everything goes well.


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