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AH-7921 analogs

tantric

tantric

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Does anyone have a ref that discusses analogs of AH-7921 other than this one.

200px-AH-7921_structure.png


Dibromo? N,N,diethyl? Neither of these is discussed in the above ref.
 
I have a feeling this class of opioids has not been investigated as in-depth as you'd like.

AH7291 always reminded me a bit of tilidine. That Br. J. Pharm. paper sez N-piperidyl or N-piperazinyl substitutions are a no-go so I bet decreasing bulk on the nitrogen would be better. Diethyl might work but don't expect miracles. (and I think diethylamine is more controlled than dimethyl anyway)

The benzoyl group SAR suggests that 3,4 dichloro is already pretty good. Maybe 3,4 methylenedioxy would go too. lots of electronegativity seems to be better. even a di-methoxy substitution would work I bet.

maybe one could replace the dimethylamino group with a mehyl ester? again bringing this cmpd close to tilidine/pethidine.

alternatively, thinking of this as a ketamine-type chemical, one could try adding a 4'-keto on the cyclohexane ring... that apparently bodes well for opi activity (viz. 4-keto-pcp).
 
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It is not merely a matter of MOR affinity though, right? Considering some potent opioids carry little recreational value and euphoria with the potential for analgesia, I take it there are differences between actual opioid action and dopaminergic action. Or is one of those secondary to the other?
Anyway AH-7921 sounds to me like it is good as a painkiller but not a recreational drug.

Is there any SAR info that would inform us about what would constitute wanted effects vs. side-effects?
(When used as recreational drugs I consider analgesia a side-effect of opioids, not sure if you agree that I do that)
 
Solipsis said:
Anyway AH-7921 sounds to me like it is good as a painkiller but not a recreational drug.
Click to expand...

Well I happen to find it quite enjoyable ;) Very little to do with other weak opioids/opiates such as O-DTramadol or codeine. For me it's closer to the "big ones"; maybe there's less euphoria but it has even more anxiolitic and relaxing properties.
 
If you read that very same Br. J. Pharmacol. paper they point out AH-7291 produces dependence like morphine. Bodes well for euphoriant f/x.
 
This thread is old but I know a few AH-7921 analogues mainly potent ĸappa agonist but they might not be as close as AH-7921 as you want.

BRL-52537 , GR-89696 , ICI-199,441 , ICI-204,448 , LPK-26 , U-50488
 
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