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  • N&PD Moderators: Skorpio | someguyontheinternet

Ketamine salts solubility

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Kaden_Nite said:
220px-TCB-2.png

TCB-2. Psychedelic, apparently very potent. Not that potency is necessarily a sign of quality goods (25-n-boXX and bromo-dragonfly), but this structure intrigues me. Makes me wonder about the potential of other substitutions.

Any guesses?
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I would like to sample TCN-2 (i.e. -Br replaced with -NO2). I reread the Pihkal piece on 2CN in which Shulgin states that it's almost as good as MDMA. I also note that DON is not psychedelic but a potent, long acting stimulant so I would like to try the (S) isomer of that.
 
Feretile said:
I'm asking for some help. I had a paper called something like '3D QSAR of mu kappa & delta opioids'. It used CoMFA to show the 3D relationship of key moieties and had a training-set for each type of opiate ligand. 20 of each if memory serves.

It WAS on the Eunoia disc but my HD died and I lost it.

I have searched extensively but not only is it without a doubt the best paper on learning CoMFA & training-sets, but it had a couple of totally novel ligands. I mean ones that do not show up on any searches but had a very high affinity. The order of training-set was from high to low affinity and one of these had the second or third highest.

I've found 1 Janssen paper from the 1960s that mentions related compounds BUT related compounds were neuroleptics so it covers a huge number of compounds and it's not very clear on the examples with opioid activity.

The REALLY odd thing is that it has a piperidine ring but instead of a 2 or 3 carbon chain linking it to a second aromatic, it has just 1 carbon BUT also a -CH3 side-chain which is apparently a requirement....

I've spent weeks looking and so far, nada. If anyone has the Eunoia Disc, it should be easy to find in 5 minutes. I just need the DOI.

Many thanks
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This? https://pubmed.ncbi.nlm.nih.gov/15743203/

 
Skorpio said:
This? https://pubmed.ncbi.nlm.nih.gov/15743203/

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Many thanks - I did look at that paper. It's a particular ligand that I am really searching for. I can usually spot the relative 3D positions & orientations of key moieties (2 aromatics, basic nitrogen with direction of lone-pair, oxygen with direction of lone-pairs & the steric hinderance to obtain said relative 3D) but this one was unusual.

Janssen briefly mentioned a similar compound in a 1960s patent but it mostly covered neuroleptics. As I'm sure you know, a lot of open-chain opioids are related to neuroleptics (haloperidol/phenoperidine, pimozide/piritamide and so on). The patent is very confusingly written and doesn't specify WHICH examples are opioids and which neuroleptics.

It's just bugging me because, as you know, most opioids don't actually have ALL the features and those that do are very potent (e.g. etorphine/carfentanil/14-phenylpropoxymetopon).

Obviously I've read hundreds if not thousands of Janssen papers but this one was evidently trying to cover as many compounds as possible. Generally, if a compound is further investigated, a more specific patent is issued, but in this case it seems not. SOMEONE took it further, but I've read all of the patents that cite the Janssen patent, but no luck. I suspect that the derivative was developed more than 20 years later and so they did not NEED to cite. After all, they would want to suggest that it was novel.
 
Feretile said:
DOI: 10.2174/157340605774598207

If nobody can obtain it, I will pay to get it next month. That's MY treat for the month :cool:
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I'll post a request for it on the mutual aid scientific community. Somebody may have it there.

Mutual Aid-Science Community Convention - Notice-Science hub Mutual Aid community

video tutorial：https://www.youtube.com/watch?v=tXUfJ62E25oStep 1: You need to register a Community account （Register）Step 2: After the account regist ... Mutual Aid-Science Community Convention
www.wosonhj.com
 
Skorpio said:
I'll post a request for it on the mutual aid scientific community. Somebody may have it there.

Mutual Aid-Science Community Convention - Notice-Science hub Mutual Aid community

video tutorial：https://www.youtube.com/watch?v=tXUfJ62E25oStep 1: You need to register a Community account （Register）Step 2: After the account regist ... Mutual Aid-Science Community Convention
www.wosonhj.com
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Nery kind of you. I'm severely disabled so I cannot work. $60 is more than I spend on food in a month.... so next month would be LEAN.

BTW it's SOMEWHERE in US 2006/0178390 '1,3,8-TRIAZASPIRO4.5DECAN-4-ONE DERVATIVES USEFUL FOR THE TREATMENT OF ORL-1 RECEPTOR
MEDIATED DISORDERS'.

The paper I saw used compound 9 but I suspect that it's compounds with a 4-substitution on the pendent benzene. Oh, and the earlier Janssen patent is US 3,155,670 '1-0XO-2,4,8 TRAZA-SPARO[4,5])PECANES.

It's mentioned on page 298 of 'Opiate Chemistry and Receptors'.

I mean, the Janssen paper has a compound x450 pethidine BUT that'd in animal models so who knows. It's NEVER going to be practical because it's too complex but it is interesting. The first patent I mentioned also seems to suggest that if the N of the lactam is substituted in the same manner as the 4 position of fentanyl analogues, potency is similarly increased.

Now, adding a methoxymethyl (or whatever) to the N of an amide is going to be interesting ;-)
 
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Feretile said:
Nery kind of you. I'm severely disabled so I cannot work. $60 is more than I spend on food in a month.... so next month would be LEAN.

BTW it's SOMEWHERE in US 2006/0178390 '1,3,8-TRIAZASPIRO4.5DECAN-4-ONE DERVATIVES USEFUL FOR THE TREATMENT OF ORL-1 RECEPTOR
MEDIATED DISORDERS'.

The paper I saw used compound 9 but I suspect that it's compounds with a 4-substitution on the pendent benzene. Oh, and the earlier Janssen patent is US 3,155,670 '1-0XO-2,4,8 TRAZA-SPARO[4,5])PECANES.

It's mentioned on page 298 of 'Opiate Chemistry and Receptors'.

I mean, the Janssen paper has a compound x450 pethidine BUT that'd in animal models so who knows. It's NEVER going to be practical because it's too complex but it is interesting. The first patent I mentioned also seems to suggest that if the N of the lactam is substituted in the same manner as the 4 position of fentanyl analogues, potency is similarly increased.

Now, adding a methoxymethyl (or whatever) to the N of an amide is going to be interesting ;-)
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Finally got around for posting it. If anybody is good for it they will reply to this request. http://www.wosonhj.com/scholar/26395xs.html
 
Feretile said:
Nery kind of you. I'm severely disabled so I cannot work. $60 is more than I spend on food in a month.... so next month would be LEAN.

BTW it's SOMEWHERE in US 2006/0178390 '1,3,8-TRIAZASPIRO4.5DECAN-4-ONE DERVATIVES USEFUL FOR THE TREATMENT OF ORL-1 RECEPTOR
MEDIATED DISORDERS'.

The paper I saw used compound 9 but I suspect that it's compounds with a 4-substitution on the pendent benzene. Oh, and the earlier Janssen patent is US 3,155,670 '1-0XO-2,4,8 TRAZA-SPARO[4,5])PECANES.

It's mentioned on page 298 of 'Opiate Chemistry and Receptors'.

I mean, the Janssen paper has a compound x450 pethidine BUT that'd in animal models so who knows. It's NEVER going to be practical because it's too complex but it is interesting. The first patent I mentioned also seems to suggest that if the N of the lactam is substituted in the same manner as the 4 position of fentanyl analogues, potency is similarly increased.

Now, adding a methoxymethyl (or whatever) to the N of an amide is going to be interesting ;-)
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So, i was looking at the article and i do have access through open athens, but i keep getting an error after the thing logs in. I'll try again to see if this is gonna get fixed.
(error is a redirect to www.eurekaselect.net/node/500 idk if that means anything to you)
I'm so quick to scihub that i sometimes forget to check through my legit channels.

I'll keep you updated tho
 
Skorpio said:
So, i was looking at the article and i do have access through open athens, but i keep getting an error after the thing logs in. I'll try again to see if this is gonna get fixed.
(error is a redirect to www.eurekaselect.net/node/500 idk if that means anything to you)
I'm so quick to scihub that i sometimes forget to check through my legit channels.

I'll keep you updated tho
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Well - I do appreciate you efforts. I had a suspicion that it would be hard to acquire.
 
Skorpio said:
So, i was looking at the article and i do have access through open athens, but i keep getting an error after the thing logs in. I'll try again to see if this is gonna get fixed.
(error is a redirect to www.eurekaselect.net/node/500 idk if that means anything to you)
I'm so quick to scihub that i sometimes forget to check through my legit channels.

I'll keep you updated tho
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Ah - only YOU can download it. Dang!
 
Many thanks. It was compound 10 that was in the paper I saw. I'm tired now, but I will read it properly tomorrow. It does closely match up with the Janssen patent and the later patent I cited. It is well worth reading both patents with this paper in front of you.
 
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