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NRX-1074 topic. (Future group buy)

Nick Kyz's Photo Nick Kyz 28 Aug 2016

After some back and forth with the lab, they feel they can't do it. 

 

Unless we can find an alternative lab at the same price point I'm prepared to refund all the group buyers. I am extremely disappointed. I have spoken to some Chinese labs, including HHDPharm that synthesized NSI-189, but none of them have synthesized this compound before and I'm somewhat skeptical of their ability, given it's such a complicated synthesis. I've spoken to other Western labs but generally their price is much higher. 

 

My suggested course of action would be to refund the money, search for an alternative lab and if we find one with reliable history we can try another group buy. 

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samson75's Photo samson75 28 Aug 2016

Why don't try glyx-13 instead ? It's already available.

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franbird's Photo franbird 28 Aug 2016

Sad news

 

Thanks for trying Nick

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Der Springende Punkt's Photo Der Springende Punkt 28 Aug 2016

Why don't try glyx-13 instead ? It's already available.

 

I second this question. The amount of NRX-1074 with this group buy was too small to take it orally. A lot of people planned to take it intranasally. So Glyx-13 (if the synthesis is actually simpler) could be a good alternative.

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jefferson's Photo jefferson 29 Aug 2016

Thanks for trying. I await the refund.

 

I'm much more hesitant about this "Glyx-13". You'd have to inject it, for one thing. It's also about to enter phase III trials, which means if it works it could be available in 2-3 more years. For some people, waiting for it might be better.

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samson75's Photo samson75 29 Aug 2016

For some other people suffering hell 2-3 more years will be too late.

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Nick Kyz's Photo Nick Kyz 29 Aug 2016

About 75% of the refunds have gone through now, I'm waiting on a bank transfer to process the rest. All refunds should be processed by midweek.

 

There are several labs that say they can synthesize the compound. They're just more expensive and I'm personally too busy to organize that side of things again. I'm still very interested of course. 

 

I would be wary of anyone on Alibaba that says they have the compound or can synthesize it. Particularly if they want upfront payment.

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Azedia's Photo Azedia 29 Aug 2016

Refund received! It is unfortunate this did not work out, at the same time - thank you, Nick, Redan and the others for organizing this and giving it a shot.

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Nick Kyz's Photo Nick Kyz 31 Aug 2016

Everyone should have been fully refunded now. I am sorry we could not deliver. It was possible to shift things to another lab but there were too many unknowns for me to be comfortable holding on to everyone's money. At the very least I have several reports from this lab with which to vet any future route of synthesis.

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samson75's Photo samson75 31 Aug 2016

Got my refund, thanks so much Nick for all your efforts.

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nyckrazy's Photo nyckrazy 01 Sep 2016

thanks for the effort bud.

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Reformed-Redan's Photo Reformed-Redan 02 Sep 2016

We've been thinking with Nick of making a nasal spray solution of the readily available GLYX-13, as to not fall into despair over the unsuccessful NRX-1074 synthesis. 

 

I hope we can get people interested. For this venture we won't need any funding; but, some pre-orders can and might be made by users here at Longecity.

 

I'll mention more details about the product once we get some rough estimate of costs of production. 

 

Eventually, we might further simply things and just offer GLYX-13 for purchase directly for users to solute themselves. Just a thought worth considering. 

 

Best regards.

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Forty Six & 2's Photo Forty Six & 2 02 Sep 2016

Hi All,

 

As I prior noted herein this thread quite a while back, I made the forecast that this would not be able to be synthesized by any group, as to the exceedingly difficult nature of such.

 

We have successfully synthesized NRX-1074, though currently the cost of production is at a loss to the price we have been offering.  This is as it is quite a bit more than initially estimated due to the challenges that are not initially apparent; such as seen with the Polish University synthesis attempts and their failure to achieve a successful method.  This is no slight to the team from Poland.  Indeed, we had to use or extensive network of connections to arrive at a chemist who had the expertise in this area and general skill overall in synthesis to find success, after many failed attempts ourselves with methods that on paper seemed to be quite viable. 

 

As such, we are making final movements to reduce the cost of this production to at least be around a break even, related to the current offering price. We have been willing to take a loss here, as we will be overall, and expend all the cost and efforts (thus far >8 months) as to our valuing the high degree of importance of this compound for research.  

 

Notably, we likely will only run enough of a production to accommodate the present pre-orders, as well as any new pre-orders.  We are still looking at 6-8 weeks to have finished and aliquoted product in hand at a 'small bulk' scale.  

 

This has truly been a nightmarishly challenging synthesis, but thankfully we have means now in hand to execute a synthesis that is viable.  We can discuss further details with any parties who have interest.  We will likely maintain pre-orders open for this upcoming production until the end of the month; though, we encourage those so interested to express such directly to us as soon as possible so as we can best ensure to accommodate.

 

We greatly thank those parties who have placed a pre-order and have been so incredibly patient and understanding within this situation; one that was immensely more challenging than ever anticipated.  As always, we will do our best to ensure the highest quality research materials, particularly those that are of such a nature that are of great importance; further, even and especially those that are of great difficulty to provide.

 

Best Success,

Forty Six & 2 and TeamTLR

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samson75's Photo samson75 02 Sep 2016

We've been thinking with Nick of making a nasal spray solution of the readily available GLYX-13, as to not fall into despair over the unsuccessful NRX-1074 synthesis. 

 

 

 

Many of us would probably be interested by a nasal spray. In my case i don't see myselft injecting Glyx-13 or snorting it like another member did.

But anyway, this group buy began years ago and ended nowhere despite nick and redan's great commitment.

So i'll keep an eye here but without any expectations.
 


Edited by samson75, 02 September 2016 - 09:34 PM.
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The Capybara's Photo The Capybara 03 Sep 2016

I'm still sitting on many 200mg vials of GLYX that's sitting in one of my freezers

Rather than forming a group buy, why not take these off my hands at my cost (really)?

I bought the minimum quantity, which had a price tag of just over $2k

This particular compound is not being sold for human use.

Peptides tend to be unstable in solution. In fact nearly every thermodynamically unfavorable compound tends to degrade much faster in solution.

Then you have bacteria which view many peptides as food, especially in solution.

Here's a good peptide stability primer (or you can just read the first sentence if chemistry is not an interest of yours).

 

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franbird's Photo franbird 03 Sep 2016

Hi All,

 

As I prior noted herein this thread quite a while back, I made the forecast that this would not be able to be synthesized by any group, as to the exceedingly difficult nature of such.

 

We have successfully synthesized NRX-1074, though currently the cost of production is at a loss to the price we have been offering.  This is as it is quite a bit more than initially estimated due to the challenges that are not initially apparent; such as seen with the Polish University synthesis attempts and their failure to achieve a successful method.  This is no slight to the team from Poland.  Indeed, we had to use or extensive network of connections to arrive at a chemist who had the expertise in this area and general skill overall in synthesis to find success, after many failed attempts ourselves with methods that on paper seemed to be quite viable. 

 

As such, we are making final movements to reduce the cost of this production to at least be around a break even, related to the current offering price. We have been willing to take a loss here, as we will be overall, and expend all the cost and efforts (thus far >8 months) as to our valuing the high degree of importance of this compound for research.  

 

Notably, we likely will only run enough of a production to accommodate the present pre-orders, as well as any new pre-orders.  We are still looking at 6-8 weeks to have finished and aliquoted product in hand at a 'small bulk' scale.  

 

This has truly been a nightmarishly challenging synthesis, but thankfully we have means now in hand to execute a synthesis that is viable.  We can discuss further details with any parties who have interest.  We will likely maintain pre-orders open for this upcoming production until the end of the month; though, we encourage those so interested to express such directly to us as soon as possible so as we can best ensure to accommodate.

 

We greatly thank those parties who have placed a pre-order and have been so incredibly patient and understanding within this situation; one that was immensely more challenging than ever anticipated.  As always, we will do our best to ensure the highest quality research materials, particularly those that are of such a nature that are of great importance; further, even and especially those that are of great difficulty to provide.

 

Best Success,

Forty Six & 2 and TeamTLR

 

Maybe you could tell us which lab you used

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plumper76's Photo plumper76 03 Sep 2016

I'm in for this group buy GLYX 13
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The Capybara's Photo The Capybara 04 Sep 2016

Here Here!

It's sitting in a freezer doing absolutely nothing for anyone's projects.

This was the price I paid after putting $2k+ down, so I don't see it getting any cheaper.

Click here to read the Longecity glyx diary. Both compelling and problematic (for me).

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samson75's Photo samson75 04 Sep 2016

How are you going to send a product that needs to be refrigerated (overseas in my case) ?

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citizen81's Photo citizen81 08 Sep 2016

Has anyone looked into: L-4-Chlorokynurenine (4-Cl-KYN; developmental code name AV-101)?

 

It appears to have similar effects to NRX-1074 and GLYX 13. Poking around Longecity, there's not much discussion around it. If it has a similar functionality, perhaps it would be easier to make?

 

http://www.ncbi.nlm....pubmed/26265321

https://en.wikipedia...hlorokynurenine

 

L-4-Chlorokynurenine (4-Cl-KYN; developmental code name AV-101) is an orally active small molecule prodrug candidate that in vivo produces a glycine binding site NMDA receptor antagonist. AV-101 is in clinical development by VistaGen Therapeutics. Inc. as a potential new generation, fast-acting antidepressant,[1][2] and for other central nervous system (CNS) indications. The initial Phase 2 clinical study of AV-101 is expected to begin in 2015 and will be focused on treatment-resistant depression (TRD) and major depressive disorder (MDD).[3]

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Babakk's Photo Babakk 12 Sep 2016

GLX 13 is already in Phase III. So when it comes to safety it is by far a better bet than using the other NMDA receptor antagonist mentioned here.

 

Does the injection have to be inter venous or can it be inter-muscular or even subcutaneous?

 

Also here is a site that is selling it under the name of Rapastinel : https://www.medcheme...Rapastinel.html.

 

Any thoughts?

 

  

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Der Springende Punkt's Photo Der Springende Punkt 12 Sep 2016

GLX 13 is already in Phase III.

 

Any source?

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franbird's Photo franbird 13 Sep 2016

GLX 13 is already in Phase III. So when it comes to safety it is by far a better bet than using the other NMDA receptor antagonist mentioned here.

 

Does the injection have to be inter venous or can it be inter-muscular or even subcutaneous?

 

Also here is a site that is selling it under the name of Rapastinel : https://www.medcheme...Rapastinel.html.

 

Any thoughts?

 

That is beyond excessively expensive

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Babakk's Photo Babakk 13 Sep 2016

 

GLX 13 is already in Phase III. So when it comes to safety it is by far a better bet than using the other NMDA receptor antagonist mentioned here.

 

Does the injection have to be inter venous or can it be inter-muscular or even subcutaneous?

 

Also here is a site that is selling it under the name of Rapastinel : https://www.medcheme...Rapastinel.html.

 

Any thoughts?

 

That is beyond excessively expensive

 

Come on guys.

No one has answered my question about the injection?

Now about the price, we could negotiate if we bought bulk however it does bring me back to one last question: what is the single dose required? The dosages discussed in reddit article seem too wide to be reliable. I can't believe that you could need 1000mg injections.

Why isn't there more information on the matter. BTW the same goes for NRX-1074.

I have only come across one reference to dosage of 3mg but that was on rats from an early experiment.

 

Finally if the Phase III clinical trials have already been started. It should be on the market by 2017, early 2018. In UK sometimes they are available before the phase III is over and I know that there are Trials being taken place in UK. If it works, I wouldn't mind traveling to UK once a month just to have the injection.

 

So I would be grateful for answering all my questions?


Edited by Babakk, 13 September 2016 - 04:19 AM.
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Der Springende Punkt's Photo Der Springende Punkt 14 Sep 2016

 

As of yet no phase 3 registration was published. Thus it's highly likely that there is no phase 3 atm. That means waiting, waiting, waiting...

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opusensemble's Photo opusensemble 12 Oct 2016

Maybe instead of waiting for bandaids to enter the market, we should look for the cure instead. Nemifitide given by IV was arguably the closest to a cure ever found. 

Please check the 3 parts of this article for groundbreaking research:  http://akhutherapeut...ression-part-3/

http://www.huffingto...4b08c46f0e4c639

 

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opusensemble's Photo opusensemble 12 Oct 2016

Tim Ferriss raised money for psilocybin research in a couple days. https://www.crowdrise.com/timferriss
And akhu in 2 months could only get a fraction of that. https://www.indiegog...ty-depression#/
Akhu guys definitely needed a marketing boost. 

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opusensemble's Photo opusensemble 12 Oct 2016

Has anyone looked into: L-4-Chlorokynurenine (4-Cl-KYN; developmental code name AV-101)?

 

It appears to have similar effects to NRX-1074 and GLYX 13. Poking around Longecity, there's not much discussion around it. If it has a similar functionality, perhaps it would be easier to make?

 

http://www.ncbi.nlm....pubmed/26265321

https://en.wikipedia...hlorokynurenine

 

L-4-Chlorokynurenine (4-Cl-KYN; developmental code name AV-101) is an orally active small molecule prodrug candidate that in vivo produces a glycine binding site NMDA receptor antagonist. AV-101 is in clinical development by VistaGen Therapeutics. Inc. as a potential new generation, fast-acting antidepressant,[1][2] and for other central nervous system (CNS) indications. The initial Phase 2 clinical study of AV-101 is expected to begin in 2015 and will be focused on treatment-resistant depression (TRD) and major depressive disorder (MDD).[3]

I personally think this drug will be a total failure for TRD, given the molecule similarity to wellbutrin, meth, ritalin. It even shares the dopaminergic characteristics. All the company announcements from Vistagen around this drug is nothing but a marketing hype to get some moments of profit glory, either in stock price, either in M&As, either in an eventually drug launch in the market. 

Remember the TCAs and how the were all based on Imipramine and worked essentially the same? This is only history repeating. Forget AV-101. Vistagen is not making science, is making speculation with a me-too compound. 

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Cadmium's Photo Cadmium 13 Oct 2016

Maybe instead of waiting for bandaids to enter the market, we should look for the cure instead. Nemifitide given by IV was arguably the closest to a cure ever found. 

Please check the 3 parts of this article for groundbreaking research:  http://akhutherapeut...ression-part-3/

http://www.huffingto...4b08c46f0e4c639

 

 

What do you feel makes this more of a 'cure' than say NSI-189 or NRX-1074?

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