• Neuroscience & Pharmacology Discussion Welcome Guest
    Posting Rules Bluelight Rules
    Recent Journal Articles Chemistry Mega-Thread
    FREE Chemistry Databases! Self-Education Guide

  • N&PD Moderators: Skorpio

Drug designs. (MedicinalUser SAR thread)

Smyth2 said:
Trachsel D, Nichols DE, Kidd S, Hadorn M, Baumberger F. 4-aryl-substituted 2,5-dimethoxyphenethylamines: synthesis and serotonin 5-HT(2A) receptor affinities. Chem Biodivers. 2009 May;6(5):692-704. doi: 10.1002/cbdv.200800235. PMID: 19479848.
Click to expand...

Affinity ≠ effaciacy.

Ralf Helm specifically produced examples of the NBOMes that were antagonists. Specifically he took the 2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one motif of respiridone and simply replaced the simpler ortho anisole motif of the agonists.

I see the logic as it allowed resesearchers so see if a more selective medication would prove to be a safer/better antipsychotic but it appears that one needs to blockade dopamine receptor or possibly reduce extracellular dopamine levels in the brain. It was @MedicinalUser247 who threw down the gauntlet asking for someone to identify a selective dopamine releaser, which was done. While that whole 'message-address' thinking is a simplification, if one has found a novel compound that selectively INCREASES extracellular dopamine levels, one then has the 'address' and that could be valuable.

At least, I assume that is why they asked.
 
You must log in or register to reply here.
Top