Lucanthone
Chemical compound
- none
- 1-{[2-(diethylamino)ethyl]amino}-4-methyl-9H-thioxanthen-9-one
- 479-50-5 Y
- 10180
- DB04967 Y
- 9772 N
- FC6D57000M
- CHEBI:51052 N
- DTXSID6023230
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
- ^ Blair DM (1958). "Lucanthone hydrochloride; a review". Bulletin of the World Health Organization. 18 (5–6): 989–1010. PMC 2537946. PMID 13573122.
- ^ Standen O (1963). "Chemotherapy of Helminthic Infections". In Schnitzer RJ, Hawking F (eds.). Experimental chemotherapy. Vol. 1. New York, New York: Academic Press. p. 770. ISBN 978-1-4832-7308-2.
- ^ Rosi D, Peruzzotti G, Dennis EW, Berberian DA, Freele H, Tullar BF, Archer S (September 1967). "Hycanthone, a new active metabolite of lucanthone". Journal of Medicinal Chemistry. 10 (5): 867–76. doi:10.1021/jm00317a025. PMID 4963368.
- ^ Hillman GR, Senft AW (September 1975). "Anticholinergic properties of the antischistosomal drug hycanthone". The American Journal of Tropical Medicine and Hygiene. 24 (5): 827–34. doi:10.4269/ajtmh.1975.24.827. PMID 1190369.
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Antitrematodals (schistosomicides) |
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Anticestodals (taeniacides) |
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(including
macrofilaricides)
Binds tubulin | |
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Glutamate-gated chloride channel, GABA receptor | |
NMDA |
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Other/unknown |
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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