Chemistry:Lucanthone

From HandWiki

Lucanthone is a drug used to treat parasitic diseases such as bilharziasis[1] and schistosomiasis[2] It is a prodrug and is converted to the active metabolite hycanthone.[3]

Mechanism of action

Hycanthone binds to acetylcholine receptors in the worm[4] and results in increased sensitivity to stimulation by 5-HT causing increase in motility, paired worms are separated and reproduction is stopped. It causes damage of the integument and vitelline duct.

References

  1. "Lucanthone hydrochloride; a review". Bulletin of the World Health Organization 18 (5–6): 989–1010. 1958. PMID 13573122. 
  2. "Chemotherapy of Helminthic Infections". Experimental chemotherapy.. 1. New York, New York: Academic Press. 1963. p. 770. ISBN 978-1-4832-7308-2. https://books.google.com/books?id=3C0SBQAAQBAJ&dq=Lucanthone&pg=PA770. 
  3. "Hycanthone, a new active metabolite of lucanthone". Journal of Medicinal Chemistry 10 (5): 867–76. September 1967. doi:10.1021/jm00317a025. PMID 4963368. 
  4. "Anticholinergic properties of the antischistosomal drug hycanthone". The American Journal of Tropical Medicine and Hygiene 24 (5): 827–34. September 1975. doi:10.4269/ajtmh.1975.24.827. PMID 1190369.