New SERT Modulators?

[Moldy Plates]

I found this synthesis paper to be interesting: the quaternary ammonium tryptamine salts 4-HO-DMET, 4-HO-DMPT, and 4-HO-DMiPT apparently lose 5HT2A binding (in comparison to the tertiary analogues) while inhibiting 5HT reuptake via SERT. Seems like a viable start to some SAR work for new empathogenic drugs that are probably pretty safe. (though the 5HT2B binding is somewhat concerning)

 

[cosmosmariner]

I’m interested in your thoughts, but it went over my head. SAR?

 

[Moldy Plates]

I’m interested in your thoughts, but it went over my head. SAR?

Structure-Activity Relationship. The 4-substituted tryptamines are generally pretty safe molecules to ingest. Several things that mess with SERT (the serotonin channel that MDMA reverses) are not the safest molecules to ingest. I don't necessarily think any of these 4 substituted quaternary amines are going to directly end up being empathogens, but the basic skeleton is a decent place to start looking.

 

[cosmosmariner]

Structure-Activity Relationship. The 4-substituted tryptamines are generally pretty safe molecules to ingest. Several things that mess with SERT (the serotonin channel that MDMA reverses) are not the safest molecules to ingest. I don't necessarily think any of these 4 substituted quaternary amines are going to directly end up being empathogens, but the basic skeleton is a decent place to start looking.

Thanks for the further explanation. And thanks for this line of thinking. I believe empathogens could be a tremendous force for good in society, but we need more of them, and we need them to be safer and less prone to abuse.