Fezolamine Explained

Fezolamine (Win-41,528-2) is a drug which was investigated by Sterling Drug as an antidepressant in the 1980s.[1] The isomeric N,N-dimethyl-4,5-diphenyl-1H-pyrazole-1-propanamine was completely inactive in the primary antidepressant screens.

It acts as a serotonin, norepinephrine, and dopamine reuptake inhibitor, with 3- to 4-fold preference for the former neurotransmitter.[2] It was found to be effective and well tolerated in clinical trials but was never marketed.[3]

See also

Notes and References

  1. Bailey DM, Hansen PE, Hlavac AG, Baizman ER, Pearl J, DeFelice AF, Feigenson ME . 3,4-Diphenyl-1H-pyrazole-1-propanamine antidepressants . Journal of Medicinal Chemistry . 28 . 2 . 256–60 . February 1985 . 3968690 . 10.1021/jm00380a020 .
  2. Baizman ER, Ezrin AM, Ferrari RA, Luttinger D . Pharmacologic profile of fezolamine fumarate: a nontricyclic antidepressant in animal models . The Journal of Pharmacology and Experimental Therapeutics . 243 . 1 . 40–54 . October 1987 . 3668867 .
  3. Zisook S, Mendels J, Janowsky D, Feighner J, Lee JC, Fritz A . Efficacy and safety of fezolamine in depressed patients . Neuropsychobiology . 17 . 3 . 133–8 . 1987 . 3683802 . 10.1159/000118353 .

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