4DQSAR
Bluelighter
- Joined
- Feb 3, 2025
- Messages
- 898
Do we have even animal models? The 1961 (?) paper Janssen published that covered hundreds of 3,3-diphenyl heptanone class of opioid appeared to show that primary carboxamides were the most potent. 8-CAC is an example of a phenol being swapped for a primary carboxamide.
I'm almost sure one of those nitazenes has a carboxamide in place of the nitro. But as a class, while interesting, nitazenes seem a dubious group of compounds.
My experience was that more than 90% of the time, even compounds WITH animal testing weren't good products. You have to presume that the odds are against you.
I have pointed them out before but amphetamines begat the diaryl (e.g. pipradrol) class which begat the THIQs (e.g. nomifensine) which begat those crazy high-affinity compounds (e.g. Mcn-5292). But looking at the papers, the ring-substitution patterns seem to match up pretty well. That's why I wondered why the para ethynyl homologue of methadrone might be of interest. I found one ligand supplier who had in the past offered para ethynyl amphetamine but it does seem that at least within the 3-carbon PEAs, a ketone may lower potency but it does appear to be less toxic. But that is just an opinion.
So thanks for doing that stuff - someone has to and you stepped up to the plate and did it. Kudos for that @Smyth2 - it is much appreciated.
BTW many years ago before Sigma and Aldrich combined, some BLer got a sample of nomifensine and wrote a report. They said it was good but a sample size of just 2 isn't great, but it's something.
I'm almost sure one of those nitazenes has a carboxamide in place of the nitro. But as a class, while interesting, nitazenes seem a dubious group of compounds.
My experience was that more than 90% of the time, even compounds WITH animal testing weren't good products. You have to presume that the odds are against you.
I have pointed them out before but amphetamines begat the diaryl (e.g. pipradrol) class which begat the THIQs (e.g. nomifensine) which begat those crazy high-affinity compounds (e.g. Mcn-5292). But looking at the papers, the ring-substitution patterns seem to match up pretty well. That's why I wondered why the para ethynyl homologue of methadrone might be of interest. I found one ligand supplier who had in the past offered para ethynyl amphetamine but it does seem that at least within the 3-carbon PEAs, a ketone may lower potency but it does appear to be less toxic. But that is just an opinion.
So thanks for doing that stuff - someone has to and you stepped up to the plate and did it. Kudos for that @Smyth2 - it is much appreciated.
BTW many years ago before Sigma and Aldrich combined, some BLer got a sample of nomifensine and wrote a report. They said it was good but a sample size of just 2 isn't great, but it's something.
