Benzylpiperazine (Trifluoromethyl-Phenylpiperazine): History notes
Last modified: Thursday, 25. December 2008 - 8:37 am
Piperazines have an interesting history in medical therapeutics, although they often failed to deliver the effects originally promised. As far back as 1919, Finley Ellingwood, M.D., touted their uses as “renal sedatives and correctives” in The American Materia Medica, Therapeutics and Pharmacognosy. Indications for use included “persistent, excessive excretion of uric acid and the urates with constant backache, dry skin and scanty urine, or where there is a brick dust sediment in the urine…It acts more rapidly than other better known agents, and is direct and positive. It is soothing to the irritated passages.” Other conditions said to respond to the piperazines included chronic rheumatic arthritis, gout, acute rheumatism, and rheumatic pericarditis, or inflammation of the coverings of the heart. Although the author claimed that “further experience should broaden its field of usefulness,” none of the indications cited in this treatise have withstood the test of time.
Since the early 1950s, piperazines have been widely used in veterinary medicine and in humans as anthelminthic drugs to rid the lower intestinal tract of parasitic worms. In 1999, Japanese researchers found that an N-benzylpiperidine derivative chemically related to the piperazines improved learning in rats. This eventually led to the discovery of donepezil (Aricept) used to slow down progressive memory loss in Alzheimer’s disease and related conditions. Although other BZP derivatives are being investigated for possible Therapeutic uses in depression, other psychiatric illnesses, epilepsy or seizure disorders, pain, inflammatory diseases, and certain tumors, none were being used for these conditions as of April 2002.