Fertile
Bluelighter
- Joined
- Mar 31, 2022
- Messages
- 1,627
I have noted that the Chinese (or wholesalers of RCs) have made a few feeble attempts to produce variants on the AH-7921 and U-47700 scaffolds. They very minor changes and I notice that they are all found in the patent referring the U-47700. Interesting that NOBODY has attempted to make U-77891 which on one hand I can understand (it's significantly more potent) but on the other hand it's an order of magnitude more potent and so one would assume it's worth x10 more.
Now, the interesting thing in the patent for U-77891 is that they produced compounds that were even more potent than the parent compound but contained a structural feature that is clearly intended to prevent beta arrestin II recruitment i.e. it will not lead to physical dependence. I think this is a very important concept. While I regret that we will still hear of people poisoning themselves by taking 'heroic' doses of such compounds, one dose does not invariably lead to another - yes psychological dependence will still be a big problem but I guess that for every death we see thousands who become slaves to opioids.
I've never produced, supplied or even possessed an illegal drug but I am interested to know if any of the AH-7921 & U-47700 derivatives are better, worse or the same as the parent drug. I presume some people here live in nations where U-47700 or at least it's derivatives are not controlled and so they can discuss their activity with impunity. You see, I am very keen to build up a QSAR of this class.
So if any of you have sampled any of this class (even the parents) then I would very much appreciate a trip report. I was recently given a new copy of Chem Office by my wife (she's the romantic type ;-) ) and I have been (trying to) perform a series of overlays. I say trying because between Chem Office 16 and the new version, the way overlays are performed has changed and so I have been forced to build physical models measuring bond-angles and using paper markers to represent hydrogen bonding.... the way we did it until the 1980s.
Oh, for any chemists reading, the Upjohn team that developed this class discovered that while the benzimides were selective to the mu receptor, adding a methylene spacer so that the compounds were the amides of phenylacetic acid produced compounds selective for the sigma receptor which produces dysphoria. It's worth looking at all of the patents of THIS class because removing a methylene suddenly gives rise to a whole new set of mu agonists.
But if it works, I do intend to publish and of course your name will appear as a secondary source (or whatever name you choose to use). I've always been keen to reference as many people as possible in papers so that in the future, said person can honestly tell any interviewer that they worked on LOTS of papers. It's no skin off my nose to reference whatever name you wish (as long as it's decent).
Now, the interesting thing in the patent for U-77891 is that they produced compounds that were even more potent than the parent compound but contained a structural feature that is clearly intended to prevent beta arrestin II recruitment i.e. it will not lead to physical dependence. I think this is a very important concept. While I regret that we will still hear of people poisoning themselves by taking 'heroic' doses of such compounds, one dose does not invariably lead to another - yes psychological dependence will still be a big problem but I guess that for every death we see thousands who become slaves to opioids.
I've never produced, supplied or even possessed an illegal drug but I am interested to know if any of the AH-7921 & U-47700 derivatives are better, worse or the same as the parent drug. I presume some people here live in nations where U-47700 or at least it's derivatives are not controlled and so they can discuss their activity with impunity. You see, I am very keen to build up a QSAR of this class.
So if any of you have sampled any of this class (even the parents) then I would very much appreciate a trip report. I was recently given a new copy of Chem Office by my wife (she's the romantic type ;-) ) and I have been (trying to) perform a series of overlays. I say trying because between Chem Office 16 and the new version, the way overlays are performed has changed and so I have been forced to build physical models measuring bond-angles and using paper markers to represent hydrogen bonding.... the way we did it until the 1980s.
Oh, for any chemists reading, the Upjohn team that developed this class discovered that while the benzimides were selective to the mu receptor, adding a methylene spacer so that the compounds were the amides of phenylacetic acid produced compounds selective for the sigma receptor which produces dysphoria. It's worth looking at all of the patents of THIS class because removing a methylene suddenly gives rise to a whole new set of mu agonists.
But if it works, I do intend to publish and of course your name will appear as a secondary source (or whatever name you choose to use). I've always been keen to reference as many people as possible in papers so that in the future, said person can honestly tell any interviewer that they worked on LOTS of papers. It's no skin off my nose to reference whatever name you wish (as long as it's decent).
