INFO NEEDED: Metabolism, Pharmacodynamics and Half-life of Aminorex

[LaGaFàNi]

Hy 'all
All the fuzz about levamisole becoming aminorex in the human's metabolising process has led me to look into this drug.
I've been looking on ncbi, pub.chem and my Uni's library for papers on aminorex's metabolism and if it has active metabolites, for it's half-life and elimination rate (presence of the drug in blood/brain after administration - lets call it elimination/time ratio), and what it's precise binding activity is at DA/NE/SE etc.

All that came up was a paper from 64 that brielfy approaches its similarity with other anorectic drugs (the actual synthesis procedure for McNeil's labs), lots of garbage about horses turning levamisole into aminorex (plus humans - related to coke cut w/leva) even though there are no reports of PH deaths from cocain abuse..), papers approaching its similarity w/ fenfluramine and other anorectics, and its action on 5-HT(s) - which causes the PH, and some other non-exploitable stuff.
I've read one report (not trustworthy) that its half-life was close to 30 hours!?

 

[aced126]

It has a long half life, probably over 10 hours. I'm not too sure whether it releases DA or blocks reuptake, and similarly for 5HT. It agonises 5HT2b receptors, which can cause cardiac valvulopathy which is a real risk.

One thing for sure is that I don't think any biological organism is capable of transforming levamisole into aminorex, or vice versa.

 

[LaGaFàNi]

Any sources? I've kept searching, and the results are contradictory all over.. Some studies found "traces" of aminorex in OD'd cocain users, other surveys didn't find any in a review of 42 users. More info about the cardiac valvulopathic risks? All I found was pulmonary hypertension and some smooth muscle related symptoms.

 

[aced126]

http://www.ncbi.nlm.nih.gov/pubmed/23972547