184 replies to this topic

[cetacean]

I also posted in the other CERC-501 purchasing thread but I want to get my name in the mix.  I am willing to go in for a few hundred dollars worth (maybe $200-250 but hopefully less  )

 

 

Edit:  man, I might even go to $300 if got us to the $4500 mark, but from what i saw it would fall short by $400.

Edited by cetacean, 03 April 2017 - 07:33 PM.

[brighterpath]

Hey guys, 

 

Just wanted to give you an update. We are at $2750, involving 7 people including myself. Cetacean and Stink have yet to pay, but they are included in that figure.

 

I am waiting for a message from one member who Tolerant specifically asked me to reach out to. He might potentially be a big buyer willing to put in a substantial amount ($1000+) for resale of the compound, so I am going to give him another 24 hours. 

 

If he doesn't respond, I will likely be beginning the negotiation process after the 24 hours, and hopefully I can bring the synthesis price down to $2500 for 2 grams, which will leave us about $200/$300 for NMR testing. This seems to be about the appropriate price for testing, and I will shop around while we wait for the synthesis to complete. 

 

Tolerant and I think the chance of getting a wrong substance from the lab is very low. He has used the lab before, and from my research they seem to do a lot of legitimate business. In fact, Tolerant mentioned to me that he wants to try the substance before testing is being done, in order to save time. 

 

As always, please feel free to reach out to me if you have any questions or concerns. 

 

 

  

 

 

Edited by brighterpath, 03 April 2017 - 10:40 PM.

[tolerant]

Please see a post I just made in the sister thread on the main Brain Health forum. It's got important information about the compound.

[brighterpath]

Hello everyone, 

 

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

 

I was able to negotiate the price down to $2,400 for 2 grams. We ended up getting 6 people including myself. The other 5 people contributed a total of $1500, but PayPal took a 3% processing fee per every transaction, which left me with $1,455. 

 

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. 

[brighterpath]

I made a mistake - the final price was $2600, down from $2800, not $2400. 

[jaybird10 2]

Thats great to hear. Is the compound cerc 501 or alks-5461?

[Mind_Paralysis]

Thats great to hear. Is the compound cerc 501 or alks-5461?

 

It's Cerc-501 - that was the compound most of us figured seemed the most promising.
 

[jaybird10 2]

Thats great to hear. Is the compound cerc 501 or alks-5461?

It's Cerc-501 - that was the compound most of us figured seemed the most promising.

Okay Thanks. Im still thinking on participating. Ill have to do a little more reading up on it. Im taking pristiq and remeron and feel like Im stable on this combination but dealing with a little anhedonia or lack of positive emotion do you think Im barking up the right tree with trying out this compound?

Edited by jaybird10 2, 06 April 2017 - 01:37 PM.

[Mind_Paralysis]

 

 

Thats great to hear. Is the compound cerc 501 or alks-5461?

It's Cerc-501 - that was the compound most of us figured seemed the most promising.

Okay Thanks. Im still thinking on participating. Ill have to do a little more reading up on it. Im taking pristiq and remeron and feel like Im stable on this combination but dealing with a little anhedonia or lack of positive emotion do you think Im barking up the right tree with trying out this compound?

 

 

It's taking everything I have to reply to this... massive somnolence... atomoxetine asthenia... atypical depression-like symptoms, returning, even though I've kept them at bay for a week with tianeptine...

 

Atomoxetine is a pretty dangerous drug - don't use it, kids - choose Reboxetine instead.

 

 

Anyways, it depends on what you want to treat with Cerc-501? Do you have massive feelings of guilt? Do you punish yourself over certain things? Are you sensitive to critique? And most importantly - have you ever had Depersonalisation/Derealisation?

It might be a treatment for Anhedonia, but that trial is just starting up, there's no telling if it works for that - in theory this compound should make it so that you are LESS BOTHERED by displeasure, (in comparison to traditional opiates which just enhance pleasure) that may or may not work on Anhedonia.

 

You are definitively WELCOME to join the Group Buy! = )

 

But just take in mind, that if you are already stable on Desvenlafaxine (pristiq) and Mirtazapine (remeron) then it's hard to tell how much it could add. It should also be noted that the drug hasn't been trialled as an adjunctive to an SNRI or a NaSSA, only as an adjunct to an SSRI, as far as I know, so the results when combined with two compounds from different classes, with different molecular structures, is completely unknown.

 

Now, considering the MOA, there's unlikely to be any interaction - but you never know, with these here experimental chemicals - could be some kind of pharmacokinetic interaction, with enzymes and metabolism of the different drugs - we don't quite know that yet.

Edited by Stinkorninjor, 06 April 2017 - 02:20 PM.

[jaybird10 2]

Thats great to hear. Is the compound cerc 501 or alks-5461?

It's Cerc-501 - that was the compound most of us figured seemed the most promising.

Okay Thanks. Im still thinking on participating. Ill have to do a little more reading up on it. Im taking pristiq and remeron and feel like Im stable on this combination but dealing with a little anhedonia or lack of positive emotion do you think Im barking up the right tree with trying out this compound?

It's taking everything I have to reply to this... massive somnolence... atomoxetine asthenia... atypical depression-like symptoms, returning, even though I've kept them at bay for a week with tianeptine...

Atomoxetine is a pretty dangerous drug - don't use it, kids - choose Reboxetine instead.


Anyways, it depends on what you want to treat with Cerc-501? Do you have massive feelings of guilt? Do you punish yourself over certain things? Are you sensitive to critique? And most importantly - have you ever had Depersonalisation/Derealisation?
It might be a treatment for Anhedonia, but that trial is just starting up, there's no telling if it works for that - in theory this compound should make it so that you are LESS BOTHERED by displeasure, (in comparison to traditional opiates which just enhance pleasure) that may or may not work on Anhedonia.

You are definitively WELCOME to join the Group Buy! = )

But just take in mind, that if you are already stable on Desvenlafaxine (pristiq) and Mirtazapine (remeron) then it's hard to tell how much it could add. It should also be noted that the drug hasn't been trialled as an adjunctive to an SNRI or a NaSSA, only as an adjunct to an SSRI, as far as I know, so the results when combined with two compounds from different classes, with different molecular structures, is completely unknown.

Now, considering the MOA, there's unlikely to be any interaction - but you never know, with these here experimental chemicals - could be some kind of pharmacokinetic interaction, with enzymes and metabolism of the different drugs - we don't quite know that yet.

Thanks Stink for that detailed response. I have an idea of what it feels like to be so low in mood that it actually hurts to use your brain so I truely appreciate you getting back to me. Im going to think on this compound after going over some of the things you mentioned. I truely hope you and all the members of the group buy get the results,benefits your looking for and get some much needed relief.

[cetacean]

I apologize to Stinkorninjor and brighterpath for not investing into the buy though I showed much initial interest. I have tendencies towards a bad mixture of impulsive and indecisive behavior. I am still seriously considering it though.

I started thinking about things related to the kappa receptor and came up with an observation. I had very positive experiences with hydrocodone. It felt very clean and energizing. And one time I gave morphine orally a try and it was a horrible dysphoric experience. The difference between the two is that morphine hits the kappa receptor while hydrocodone does not (maybe the metabolites do but the first 2 hours of hydrocodone are very clean and uplifting). This may imply that I have oversensitive kappa receptors.

Does this seem like a reasonable conclusion? Has anyone else had similar experiences?

I'd also like to mention that I am on venlafaxine like the above poster. I have had significant improvements in mood and motivation with low dose naltrexone. The only issue I've had is a moderate increase in nervous energy and increased cravings for kratom, opiates, and alcohol. This would hopefully be aleviated by a kappa antagonist.

My bodybuilder supplement freak friend has some (expired) amentoflavone which is a k antagonist. I'm probably getting it tomorrow. I'm going to try it even though I haven't read many positive things. Depending on how that goes I will either try to get more amentoflavone from china or finally commit to the cerc-501 buy...

Edited by cetacean, 06 April 2017 - 06:59 PM.

[satsumass]

Hii cetacean I am super interested in your response to amentoflavone...hope you can report back on your near-term and longer-term results if you're planning on giving this a clean trial. Are there any recent threads or any other content you can help point me to regarding amentoflavone and detail your reasoning? I remember it mentioned just once or twice on this board I believe but don't recall any detail or experiences...positive or negative.

 

I apologize to Stinkorninjor and brighterpath for not investing into the buy though I showed much initial interest. I have tendencies towards a bad mixture of impulsive and indecisive behavior. I am still seriously considering it though.

I started thinking about things related to the kappa receptor and came up with an observation. I had very positive experiences with hydrocodone. It felt very clean and energizing. And one time I gave morphine orally a try and it was a horrible dysphoric experience. The difference between the two is that morphine hits the kappa receptor while hydrocodone does not (maybe the metabolites do but the first 2 hours of hydrocodone are very clean and uplifting). This may imply that I have oversensitive kappa receptors.

Does this seem like a reasonable conclusion? Has anyone else had similar experiences?

I'd also like to mention that I am on venlafaxine like the above poster. I have had significant improvements in mood and motivation with low dose naltrexone. The only issue I've had is a moderate increase in nervous energy and increased cravings for kratom, opiates, and alcohol. This would hopefully be aleviated by a kappa antagonist.

My bodybuilder supplement freak friend has some (expired) amentoflavone which is a k antagonist. I'm probably getting it tomorrow. I'm going to try it even though I haven't read many positive things. Depending on how that goes I will either try to get more amentoflavone from china or finally commit to the cerc-501 buy...

 

[hnk6]

Does anyone want to participate in a Hydroxynorketamine buy group? We are appr. 10 people buying, the lab is about to finish.

If you want to be included, please e-mail me at hnk6 (at) tutanota.com

 

HNK6

[cetacean]

Satsumass, the below article is the best thing I've found so far. It's theoretical and I've seen some people claim it is very poorly absorbed so it would not be orally active. I don't have sources on that yet.

Regarding anecdotes, there are not many. I think part of the problem is that amentoflavone was only commercially available for a short time so not many people tried it for it's kappa antagonist properties. I think most people purchased it for its effect on lipid metabolism.

Here the article:

https://www.ncbi.nlm...les/PMC2265593/

Here is an interesting section of the article about amentoflavone. In the text, (3) refers to amentoflavone because it was listed along with other similar chemicals:

Structures of Naltrexone (1), nor-BNI (2a), GNTI (2b), JDTic (3), Amentoflavone (4), Apigenin (5), Hyperoside (6), 7,4′-Dihydroxyflavone (7), and Naringenin (8)


3 (amentoflavone) was shown to be a more potent κ antagonist than 2a. Biological studies have shown that 3 blocks κ-agonist-induced antinociception in mice and squirrel monkey and antagonizes κ-agonist-induced diuresis in rats. A more recent study illustrated that 3 is effective in decreasing withdrawal signs in rodents, indicating 3 may find some application in the treatment of opiate abuse. Furthemore, 3 significantly reduced foot-shock-induced reinstatement of cocaine responding in rats and decreased immobility and increased swimming time in the forced swim stress test similar to the antidepressant desipramine.3 However, like other κ antagonists mentioned above, 3 has a slow onset and extremely long duration of action.


I will most certainly post my experiences!

Edited by cetacean, 06 April 2017 - 08:06 PM.

[cetacean]

Here's another important part from the posted article showing amentoflavone (now refered to as biflavone 4) is significantly more active at the kappa receptor:

Biflavone 4 was inactive as an antagonist at the μ opioid receptor (Ke > 10 000 nM) and weakly active at the δ opioid receptor (Ke = 6000 nM) (Table 1). In contrast, 4 had good activity at the κ opioid receptor with a Ke of 490 ± 150 nM. Figure 1 shows that amentoflavone at 1000 nM caused nearly a 4-fold shift in the U69,593 concentration–response curve. Moreover, 4 was more than 10-fold selective for the κ over the δ opioid receptor. This is the first report of a flavonoid with κ antagonist activity and opens a new structural scaffold for the development of opioid antagonists.

Edited by cetacean, 06 April 2017 - 07:51 PM.

[Mind_Paralysis]

The below article is the best thing I've found so far. It's theoretical and I've seen some people claim it is very poorly absorbed so it would not be orally active. I don't have sources on that yet.

Regarding anecdotes, there are not many. I think part of the problem is that amentoflavone was only commercially available for a short time so not many people tried it for it's kappa antagonist properties. I think most people purchased it for its effect on lipid metabolism.

Here the article:

https://www.ncbi.nlm...les/PMC2265593/

And this is the interesting part about amentoflavone. In the text, (3) refers to amentoflavone because it was listed along with other similar chemicals:

Structures of Naltrexone (1), nor-BNI (2a), GNTI (2b), JDTic (3), Amentoflavone (4), Apigenin (5), Hyperoside (6), 7,4′-Dihydroxyflavone (7), and Naringenin (8)


3 (amentoflavone) was shown to be a more potent κ antagonist than 2a. Biological studies have shown that 3 blocks κ-agonist-induced antinociception in mice and squirrel monkey and antagonizes κ-agonist-induced diuresis in rats. A more recent study illustrated that 3 is effective in decreasing withdrawal signs in rodents, indicating 3 may find some application in the treatment of opiate abuse. Furthemore, 3 significantly reduced foot-shock-induced reinstatement of cocaine responding in rats and decreased immobility and increased swimming time in the forced swim stress test similar to the antidepressant desipramine.3 However, like other κ antagonists mentioned above, 3 has a slow onset and extremely long duration of action.


I will most certainly post my experiences!

 

Hold on, hold on, hold ON there...!

 

Amentoflavone is a rather dirty chemical, it seems to be one of the compounds within Saint John's Wort which messes with the Cytochrome 450 -system.

 

I would not combine Amentoflavone with Venlafaxine - which is pretty much something you would have to do, since Venlafaxine takes a long time to taper off of - and it's probably not recommended you do so.

 

We know for a fact that it messes with CYP3A4 and CYP2C9, and the active metabolite of Venlafaxine, DesVenlafaxine, is metabolized by CYP3A4, so that's not necessarily a good combo, dude...

 

I would wait with using Amentoflavone until there's actually more info on it's therapeutic effects - at least wait until we have some animal testing on it's potential antidepressant or anxiolytic properties, ok?

 

I'd be a bit bothered about it's effects as a GABA-antagonist as well, if I was you.

[cetacean]

Ok that's something to consider. It's just that so many medications and supplements affect those liver enzymes. I already take modafinil and clonazepam prn plus all my herbs.

What concerns you about the gaba antagonist properties? I never saw it mentioned as being a big part, but I could be wrong. If its mild enough, it would be of benefit to downregulate gaba.

Thanks for the info and I will rethink my experiment.

[tolerant]

Okay Thanks. Im still thinking on participating. Ill have to do a little more reading up on it. Im taking pristiq and remeron and feel like Im stable on this combination but dealing with a little anhedonia or lack of positive emotion do you think Im barking up the right tree with trying out this compound?

 

 

It might be a treatment for Anhedonia, but that trial is just starting up, there's no telling if it works for that - in theory this compound should make it so that you are LESS BOTHERED by displeasure, (in comparison to traditional opiates which just enhance pleasure) that may or may not work on Anhedonia.

 

I have written to Dr. Andy Krystal who is authoring the anhedonia study for any updates and if and when he responds I will post either here or in the new thread, or both.

[Mind_Paralysis]

 

Okay Thanks. Im still thinking on participating. Ill have to do a little more reading up on it. Im taking pristiq and remeron and feel like Im stable on this combination but dealing with a little anhedonia or lack of positive emotion do you think Im barking up the right tree with trying out this compound?

 

 

It might be a treatment for Anhedonia, but that trial is just starting up, there's no telling if it works for that - in theory this compound should make it so that you are LESS BOTHERED by displeasure, (in comparison to traditional opiates which just enhance pleasure) that may or may not work on Anhedonia.

 

I have written to Dr. Andy Krystal who is authoring the anhedonia study for any updates and if and when he responds I will post either here or in the new thread, or both.

 

 

Awesome! = ) I'm looking forward to any potential snippets of knowledge he can pass on concerning this effect - god knows I've got it!

 

Btw... I just got to thinking about up and down -regulation - CERC-501 is probably a drug that needs to be tapered off a bit! We can't afford to be hit with a sudden UPregulation of the kappa-receptors, dude...! o.O Could be down-right catastrophic!

 

So everyone, when you have your dose, plan out how you're going to use it - make sure that you have a certain amount left towards the end of your trial, to properly taper it down.

 

 

What do we know about opioid-antagonism at the Mu and Delta btw? That could probably be a good, reasonable idea about how the kappa-receptor will act when antagonised. Are the effects of Naloxone and Naltrexone persistent even after discontinuation? Or do those receptors then fairly quickly upregulate in response? I believe this is actually what you WANT from those two, as they're used for treating opiate-withdrawal, I believe.

 

Ok that's something to consider. It's just that so many medications and supplements affect those liver enzymes. I already take modafinil and clonazepam prn plus all my herbs.

What concerns you about the gaba antagonist properties? I never saw it mentioned as being a big part, but I could be wrong. If its mild enough, it would be of benefit to downregulate gaba.

Thanks for the info and I will rethink my experiment.

 

GABA-antagonism can cause susceptibility to seizures, especially if you're using another compound which lowers the seizure-threshold - Venlafaxine is one such compound.

It can also cause increased anxiety and disrupt sleep.
 

Basically, it could work in reverse to Benzo's... With that said, you are right that we don't know much about that property - if it's a very weak such effect, then it may not be so bad - it could actually lead to *UP*regulation of the GABA-receptors after a while!

(I'm guessing that's what you meant? because downregulating gaba-receptors leads to benzodiazepine withdrawal-symptoms... you DON'T want that...!)

 

But we don't know much about the compound - so that in itself is a basis for concern - the effect could go either way.

[frenchmoxie]

... I had very positive experiences with hydrocodone. It felt very clean and energizing. And one time I gave morphine orally a try and it was a horrible dysphoric experience. The difference between the two is that morphine hits the kappa receptor while hydrocodone does not (maybe the metabolites do but the first 2 hours of hydrocodone are very clean and uplifting). This may imply that I have oversensitive kappa receptors...

I too have felt quite negative from taking morphine tablet orally. It was a round, small, burgundy pill, I believe 30mg ER morphine sulphate. It was almost like taking a sugar pill. Barely did anything and seemed to take hours to kick in, even though I chewed that sucker up good before downing it.

[HouseElisabeth]

http://ir.cerecor.co...1-phase-2-study

 

Any ideas?

[tolerant]

This comppund sucks. Good on me for orderi g 1.5 months' worth. Anybody wanna buy some off me?

Edited by tolerant, 21 April 2017 - 02:13 PM.

[Der Springende Punkt]

http://ir.cerecor.co...1-phase-2-study

 

Any ideas?

 

CERC-301 (NMDA related) has nothing to do with CERC-501 (kappa opioid related).
 

[HouseElisabeth]

Thank god,you're wright!
How stupid of me...

[Der Springende Punkt]

Thank god,you're wright!
How stupid of me...

 

No problem. It's easy to confuse.

[Mind_Paralysis]

This compound sucks. Good on me for ordering 1.5 months' worth. Anybody wanna buy some off me?

 

Care to elaborate a bit more? What do you feel when you take the drug? Do you get QT-interval prolonging or something?

 

Btw... I was unaware that our group buy synthesis was actually complete?? And even if it was, we still haven't done NMR-testing on it, or any other testing for that matter - hence, we have no idea we've actually got CERC-501 yet!

 

And finally, there's the question if this truly has any acute antidepressant or anxiolytic properties - regular opioids has such effects, but it's not an absolute given that Cerc-501 has immediate effects - maybe it takes a week or two before you truly suppress kappa-activity enough to actually notice the magic.

 

I think you truly need to take these things into account before you pass judgement on the compound.
 

[tolerant]

Sorry, I was far too drunk to differentiate the two compounds. I haven't tried CERC-501 (or CERC-301 for that matter). Obviously waiting like everyone else for the synthesis to be completed. So ignore my previous post please! Also ignore the previous post in the other thread where I said I thought I might be getting better!

Edited by tolerant, 21 April 2017 - 04:46 PM.

[brighterpath]

Hey everyone, I have a few updates. 

 

Firstly, I got the news on Monday from the lab that our synthesis is complete. They are currently running their internal quality control, and will be shipping out the compound this week if the quality is acceptable. 

 

Secondly, I have been speaking with two labs about NMR testing on our end, and they've quoted me $560 and $700 respectively. They use different processes, and I've been learning that NMR is incredibly complicated, so it is difficult to tell as of right now which one might be a better value, but I am working on it. But it does seem like the pricer one is more accurate at this point. They both require about 100mg of the material as well, which will have to be factored into the cost. 

 

On that note, we need a way to pay for the NMR testing. Tolerant had the idea of dividing the price by the number of people who participated in the buy, but I know people paid different amounts, so I'm not sure it would make sense to just divide $560 or $700 + 100mg worth of material by 7 or 8 people. So I think the better solution might be to just add on the cost of the NMR testing to the total cost, and calculate the new price per 100mg. 

 

The buy went through at $2600 for 2 grams, so the pricing was $130 for 100mg. But this would have to become $2600 (synthesis cost) + $560 (lower end NMR cost example) + $130 (100mg material lost cost). Paypal also took a 3% cut from everything you sent me, and while I was just going to cover this cost at first, when we are dealing with 2-3K this fee became up to $100. So this will need to be factored in. There is also shipping cost that was not factored into collection for a lot of people, which we will have to figure out when we are at the stage. 

 

The tentative total right now is either $3290 or $3430, which brings the price to $164.5 or $176.5 per 100mg of the compound. You could either pay a little extra for the same amount of compound or get less for the amount you paid. 

 

Does this seem fair to everyone who participated in the buy? I apologize for the slight change in the pricing post synthesis, but it was difficult to anticipate the pricing for NMR, given that they charge different amounts for different compounds. 

 

Please feel free to message me with any questions or concerns. 

[Laurus]

Hello everyone, 

 

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

 

I was able to negotiate the price down to $2,400 for 2 grams. We ended up getting 6 people including myself. The other 5 people contributed a total of $1500, but PayPal took a 3% processing fee per every transaction, which left me with $1,455. 

 

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. 

 

Hi brighterpath, 

 

I stumbled upon your thread yesterday and registered to the forum today. 

I suffer from DP/DR since almost 10 years and - as many of us - did a lot of research on possible medications. What is known about KOR antagonists sounds promising, but it's upsetting that none are available at the moment.

 

It's amazing that you, tolerant, and others put so much effort in organizing this group buy! 

 

Is it still possible to join you? You said, that you "personally fronted a large sum, and would be happy to part with some shares" - is that still the case?

 

best wishes

[brighterpath]

Hi Laurus,

You are definitely welcome to join our buy! I will send you a message right now.