659 replies to this topic

[VICREP]

@ILikeBeer

Group buys have been organised through chem synthesis companies a numbers of times from memory. NSI-189, JDTic, Dihexa

[Dayfob]

Count me in.

[tintinet]

In as well!

[h2o]

I contacted MrYouAreSoDumb from reddit and he said based on the naming convention, threonyl-prolyl-2R-(2-benzyl)-prolyl-threonine amide this is how NRX-1074 looks like:

 

[jefferson]

Not that I don't trust Ceretropic, but we need to get that verified by multiple authorities.

[h2o]

You are right jefferson. I recieved an update from MrYouAreSoDumb.

 

 

 

I actually think I attached the benzyl inccorectly. It's not at the 2 position.

It's actually probably more like this

 

 

 

I'm just messing around in Chemdoodle, though. Don't tell people that is for sure what the structure looks like yet.

 

So here is just a tentative possibility of how the chemical looks like, but nothing fully verified as of now.

[Adr1n]

I'm in for the group buy

[neuroatypicow]

me too.

[h2o]

MrYouAreSoDumb talked to one of his chemists that he consults, and he said that based on the info we have NRX-1074 can come in two forms.

 

 

There are two possible conformations that the 2-Benzyl-L-Proline amino acid can come in. I made this image to illustrate it. Most should end up being option A, but some will be option B too. So that is what I think NRX-1074 should look like. Again, it is just an estimation.

 

 

 

 

So now I am wondering if there are differences between the two structures with regards to safety and efficacy in vivo.

Edited by h2o, 11 August 2015 - 04:04 PM.

[lifescience]

Both Option A and Option B have right stereochemistry but structures are not acurate(Both have typo). 1,The two unnatural amino acid are actually the same R configuration  2. The "2R" in its name means benzyl group in 2 position and the configuration is R.  I attached the right structures below.

 

MrYouAreSoDumb talked to one of his chemists that he consults, and he said that based on the info we have NRX-1074 can come in two forms.

 

 

There are two possible conformations that the 2-Benzyl-L-Proline amino acid can come in. I made this image to illustrate it. Most should end up being option A, but some will be option B too. So that is what I think NRX-1074 should look like. Again, it is just an estimation.

 

 

 

 

So now I am wondering if there are differences between the two structures with regards to safety and efficacy in vivo.

 

Attached Files

•  untitled.png   23.08KB   10 downloads

Edited by lifescience, 11 August 2015 - 07:32 PM.

[jefferson]

Where is ScienceGuy when you need him?

[MetaMind]

count me in as well.

[Forty Six & 2]

Hi All,

 

We have researched this synthesis extensively, produced a very small first test synthesis, as well as two analogues we feel are even superior.

We can offer a Group Buy situation for this compound, however, kindly note this is quite a challenging and costly molecule (an enantiomeric conjugated tetrapeptide) to produce.

 

We can offer as follows, and interests can be confirmed herein, for those who have serious research in this field:

 

NRX-1074 98%

 

100mg at 300USD + shipping

500mg at 1300USD + shipping

 

Lead Time:  6-8 weeks

 

We will be looking to see a demand of >20 researchers. If greater than 30 researchers we will avail a 10% discount on the given price.

 

Thank you for your consideration.  We indeed would like to make this valuable molecule available.

 

Kindly NOTE:

 

We as well will include FREE GLYX-OX 5G Powder, our proprietary Glycine-Site Antagonist Optimized Xtract, that we feel is very worthwhile for those researching in this area.  https://teamtlr.com/...ocognitive.html

Further, we will include FREE SNRB-OX 20mg, as we feel there is a synergy with very low dose SNRB-OX and Glycine-Site Antagonists for the most pronounced and clean efficacy for neurogenic/nootropic antidepressant efficacy.  As well, the synergy appears to allow for a reduction of the dose of NRX-1074 for comparable/superior efficacy.

 

We feel there is great worth to exploring this area thoroughly and hope research will manifest a superior paradigm of superior antidepressant/neurogenic/synaptogenic efficacy with no adverse effects.

 

Thank you for your kind time and progressive mind.

Forty Six & 2

TeamTLR

[ILIkeBeer]

So... sounds like a group buy then?

[Reformed-Redan]

So... sounds like a group buy then?

TeamTLR sells bunk goods according to 3'rd party lab analysis reports some time ago done on available products that don't even disclose their ingredients. 

[Forty Six & 2]

Actually, that is in reality a blatant lie and wholly disproved, so thanks again redan for spreading lies and hate as you have along with your other chums of CereBrownosery ilk

We can link all the threads so displaying that the actual truth is one of a conflict of interest agenda, incompetency, slander, defamation, and otherwise of that nature. However, we rather not go into all that again. Niner and other Moderators here will be alerted that you and yours are once again spreading 'hate' and lies. As it has been thoroughly dealt with and disproved I will as well request anyone from this point so beating this dead horse and spreading such defamation be banned, as simply it has gone on far long enough and then some.

Best Regards~

 

P.S.  PLEASE NOTE:

After the last atrocity of this nonsense uprising, Mind, a head Moderator, as well supported the position of our integrity at TeamTLR

Edited by Forty Six & 2, 27 August 2015 - 03:10 AM.

[jefferson]

I'm willing to consider this for NRX-1074, as it seems like a good deal. Of course, the product needs to be analyzed by a third party. This should be done no matter the source.

[uptownboy]

I am in for a group buy with this one. From what i can see, we almost have structure and NRX-1074 will be available, right? 

[Izan]

Hi All,

 

We have researched this synthesis extensively, produced a very small first test synthesis, as well as two analogues we feel are even superior.

We can offer a Group Buy situation for this compound, however, kindly note this is quite a challenging and costly molecule (an enantiomeric conjugated tetrapeptide) to produce.

 

We can offer as follows, and interests can be confirmed herein, for those who have serious research in this field:

 

NRX-1074 98%

 

100mg at 300USD + shipping

500mg at 1300USD + shipping

 

Lead Time:  6-8 weeks

 

We will be looking to see a demand of >20 researchers. If greater than 30 researchers we will avail a 10% discount on the given price.

 

Thank you for your consideration.  We indeed would like to make this valuable molecule available.

 

Kindly NOTE:

 

We as well will include FREE GLYX-OX 5G Powder, our proprietary Glycine-Site Antagonist Optimized Xtract, that we feel is very worthwhile for those researching in this area.  https://teamtlr.com/...ocognitive.html

Further, we will include FREE SNRB-OX 20mg, as we feel there is a synergy with very low dose SNRB-OX and Glycine-Site Antagonists for the most pronounced and clean efficacy for neurogenic/nootropic antidepressant efficacy.  As well, the synergy appears to allow for a reduction of the dose of NRX-1074 for comparable/superior efficacy.

 

We feel there is great worth to exploring this area thoroughly and hope research will manifest a superior paradigm of superior antidepressant/neurogenic/synaptogenic efficacy with no adverse effects.

 

Thank you for your kind time and progressive mind.

Forty Six & 2

TeamTLR

i see you sell anti hairloss products. try to synthesize proteasome inhibitor 1 or PS1 @ > 98% purity and i you will have 100000 new customers in a heartbeat. are you be willing to produce PS1? 

[Vitalist]

I'm in for the TeamTLR group buy.

[Forty Six & 2]

TeamTLR

Is Pleased To Announce

The Production and Pre-Order Limited Time Special

of

NRX-1074

 

While the Group Buy dynamic did not manifest in anywhere near as substantial a size as to be remotely garner the requisite interest, through a strong initiative to push to get this valuable compound in motion we have thankfully reached a sufficient amount of pre-orders to make the production of NRX-1074 viable. We are now offering a one-time opportunity to pre-order NRX-1074 at a 20% discount donation off the listed retail price that we will honor for one week through Sunday September 20th.

https://teamtlr.com/...neurogenic.html

 

Therein, if this is of interest to anyone here who is following the thread, we hope you take advantage of this offer and please kindly contact us at TLR@TeamTLR.com to request to order via the special.

 

We have two of our most expert producers that we have a very long relationship with working to produce this and as noted it is estimated to be about 6-8 weeks lead time until completion. As such, we are anticipating to have the material readied to ship by about mid-November. We are really pleased this could go forward and to offer this landmark compound as a first for research intents.

 

Thank you to all who support this effort and TLR and look to support the betterment of one's self and of others.

[Reformed-Redan]

I'm interested in a group buy. If TLR can provide a third party lab analysis of the compound, I'd be down to make a purchase. 

 

Cheers.

[Forty Six & 2]

We're offering it as above, so no need for a group buy for the discount so noted as pre-order. For that, one simply just needs to contact us for placing the special pre-order by next Sunday.

We do have a third party lab that is excellent with peptides and in which we paid for and coordinated testing for the GHK/GHK-Cu 1:1 MIX we supplied the group buy there.

Within third party testing, as was with the above GHK/GHK-Cu Mix testing, we would always wish a random sample from a purchaser be sent in so as for a pure "chain of custody assurance". This is the only means to truly valid quality assurance of any material so supplied, as we have noted many times prior.

Edited by Forty Six & 2, 20 September 2015 - 12:53 AM.

[Reformed-Redan]

If anyone with a chemistry background could help with obtaining/synthesizing the unusual intermediate used to produce NRX-1074, please post here or PM me. Thanks.

[uralsky]

So how many oral doses would 50 mg provide?

10 mg was effective by IV. Perhaps 50 mg would be enough for couple oral doses?

Edited by uralsky, 21 September 2015 - 05:44 PM.

[Reformed-Redan]

So how many oral doses would 50 mg provide?

10 mg was effective by IV. Perhaps 50 mg would be enough for couple oral doses?

We don't really know as bioavailability hasn't been disclosed, afaik. 

[Forty Six & 2]

For purposes of discussion, the doses seen used in oral administration are about 5-10 times that of those used in injection (i.v.) route of administration, of which via i.v. injection has shown to be effective at 5mg and 10mg in a largely dose dependent fashion.  Likely an oral equivalency requiring 10x the dose as given i.v. is the figure that is more true to be of similar efficacy basis, but there is no indication demonstrating full and direct comparisons and such still remains to be more fully determined.  As such this is a guide to understanding an extrapolation of some of the current testing and data so available.

 

Intranasal administration may allow a small, but significant, amount to directly enter the CNS and bypass the inherent poor BBB penetration of such peptides, thus to seem of potential to be of near or equal efficacy and potency to (peripheral) injectible (i.v. or otherwise, such as s.c., i.m.) routes.  

 

Notably, i.v. administration, as would very likely be such with intranasal, shows rapid onset and sustained effects for ~1-2 weeks in general.

 

I hope this aids all in their understanding of these matters.  Any further questions do not hesitate to ask.   Hopefully many will look to research with this landmark compound and as so stated prior we are offering a limited time pre-order 20% discount off the website pricing by request to our e-mail TLR@TeamTLR.com through Sunday 9/27.

https://teamtlr.com/...neurogenic.html

 

[Joe chiavarini]

I AM IN WITH 100 bucks

[cheezburger]

Concerning oral administration, Naurex has only tried two dosages : 25mg and 125mg. This quite broad range seems to indicate that they're still in early stage about oral dosage.

I think it's a self bet to stay around ~75mg.

 

source: https://clinicaltria...NRX-1074&rank=3

Edited by cheezburger, 22 September 2015 - 12:55 PM.

[Forty Six & 2]

To elaborate for purposes of further discussion, indeed the above trial doses of 25mg and 125mg are correct from one trial outlined in 2013, and hence the notation of a what would appear a sound potential for oral dosages at ~10x the i.v. dose to be of some equivalence in efficacy.

As seen herein:  https://clinicaltria...how/NCT01856556

 

However, I should clarify further, that while this is hoped for so as the oral dose is even remotely 'rational', especially as regards the inherent high cost to produce a conjugated, enantiomeric tetrapeptide, such an oral dosage range may well be wishful thinking and oral dosing may not ever be at all realistically tenable (even if approved and released commercially, due to cost, or such that I am not sure what insurance would be willing to cover it).

 

Herein this link we see dosages that are far in excess of 25mg and 125mg at 375mg, 500mg, and 750mg (OUCH!) from a more recent trial outline from 2015: https://clinicaltria...how/NCT02366364

 

So, for the edification of all, this is why we would like to note that routes involving i.v. (or injection otherwise), or intranasal would be likely the only tenable means.

 

 

Edited by Forty Six & 2, 22 September 2015 - 02:08 PM.