Norfenfluramine Explained

Norfenfluramine, or 3-trifluoromethylamphetamine, is a never-marketed drug of the amphetamine family that behaves as a serotonin and norepinephrine releasing agent and potent 5-HT_2A, 5-HT_2B, and 5-HT_2C agonist. The action of norfenfluramine on 5-HT_2B receptors on heart valves leads to a characteristic pattern of heart failure following proliferation of cardiac fibroblasts on the tricuspid valve, known as cardiac fibrosis.^[1] This side effect led to the withdrawal of fenfluramine as an anorectic agent worldwide, and to the withdrawal of benfluorex in Europe,^[2] as both fenfluramine and benfluorex form norfenfluramine as an active metabolite. It is a human TAAR1 agonist.^[3]

See also

• Fenfluramine
• Benfluorex
• Norfenfluramine is the precursor to flucetorex

Notes and References

1. Setola . V. . Dukat . M. . Glennon . R. A. . Roth . B. L. . Molecular Determinants for the Interaction of the Valvulopathic Anorexigen Norfenfluramine with the 5-HT_2B Receptor . Molecular Pharmacology . 2005 . 68 . 1 . 20–33 . 15831837 . 10.1124/mol.104.009266 . 30906680 .
2. Web site: European Medicines Agency recommends withdrawal of benfluorex from the market in European Union . European Medicines Agency . 2009-12-18 . dead . https://web.archive.org/web/20091222213737/http://www.emea.europa.eu/pdfs/human/referral/benfluorex/Benfluorex_81503309en.pdf . 2009-12-22 .
3. Lewin AH, Miller GM, Gilmour B . Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class . Bioorg. Med. Chem. . 19 . 23 . 7044–8 . December 2011 . 22037049 . 3236098 . 10.1016/j.bmc.2011.10.007 .