Title: Praziquantel
CAS Registry Number: 55268-74-1
CAS Name: 2-(Cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinolin-4-one
Manufacturers' Codes: EMBAY 8440
Trademarks: Biltricide (Bayer); Cesol (Merck KGaA); Droncit (Bayer)
Molecular Formula: C19H24N2O2
Molecular Weight: 312.41
Percent Composition: C 73.05%, H 7.74%, N 8.97%, O 10.24%
Literature References: Prepn: J. Seubert et al., DE 2362539; eidem, US 4001411 (1975, 1977, both to E. Merck, W. Ger.); D. Frehel et al., Heterocycles 20, 1731 (1983). Properties: J. Seubert et al., Experientia 33, 1036 (1977). In vitro study: C. J. Chavasse et al., Z. Parasitenkd. 58, 169 (1979). Effect on ultrastructure of trematodes: H. Mehlhorn et al., Arzneim.-Forsch. 33, 91 (1983). Pharmacodynamics: G. C. Coles, J. Helminthol. 53, 31 (1979). Ovicidal activity in Echinococcus: A. S. Thakur et al., Exp. Parasitol. 47, 131 (1979). Clinical pharmacology: G. Leopold et al., Eur. J. Clin. Pharmacol. 14, 281 (1978). Efficacy in dogs: F. L. Anderson et al., Am. J. Vet. Res. 40, 700 (1979). Mutagenicity study: H. Bartsch et al., Mutat. Res. 58, 133 (1978). Tolerance study: P. Muermann et al., Vet. Med. Rev. 1976 (2), 142. Symposium on African schistosomiasis: Arzneim.-Forsch. 31, 535-618 (1981). Clinical studies (human schistosomiasis): T. E. Nash et al., Am. J. Trop. Med. Hyg. 31, 977 (1982); R. N. H. Pugh, C. H. Teesdale, Br. Med. J. 286, 429 (1983); C. H. Schutte et al., S. Afr. Med. J. 64, 7 (1983). Clinical trial in human parenchymal brain cysticercosis: J. Sotelo et al., N. Engl. J. Med. 310, 1001 (1984).
Properties: Crystals, mp 136-138°. Soly (g/100 ml): ethanol 9.7; chloroform 56.7; water 0.04. LD50 in mice, rats (mg/kg): 2000-3000 orally; >3000 s.c. (Muermann).
Melting point: mp 136-138°
Toxicity data: LD50 in mice, rats (mg/kg): 2000-3000 orally; >3000 s.c. (Muermann)
Therap-Cat: Anthelmintic (Schistosoma).
Therap-Cat-Vet: Anthelmintic.
Keywords: Anthelmintic (Schistosoma). |