Praziquantel is an anti-helminthic against parasitic flatworms that causes contractions and paralysis the organism. Research suggests Praziquantel works mostly by increasing cell permeability. Praziquantel was developed in the laboratories for parasitological research of Bayer AG and Merck KGaA (Elberfeld and Darmstadt sites in Germany) in the mid-1970s.
A pyrazinoisoquinoline derivative, Praziquantel increases the tegument permeability in the suceptible worms, resulting in an influx and therefore an increase in intra-tegumental calcium. This leads to contractions and paralysis of the worm's musculature via an increase in calcium in the sarcoplasmic reticulum. Subsequent vacuolization of the tegumental syncytium and blebbing results in disintegration of the tegument, leading to antigen exposure and eliciting host defense responses to the worm. This results in the formation of granulomas and phagocytosis.
Praziquantel is a racemate, composed of two enantiomers: a biologically active enantiomer (R-praziquantel) has greater antiparasitic activity compared to the inactive distomer (S-praziquantel) in both in vitro and in vivo applications.
Praziquantel is used to study schistosomiasis (syn: snail fever), a tropical disease and helminthiasis caused by the parasitic flatform of the genus Schistosoma.
Praziquantel is soluble in ethanol and DMSO.
| Mechanism of Action | Praziquantel increases the permeability of the tegmentum to Ca2+ inducing paralytic muscle contraction and death. Recent studies have indicated that Praziquantel binds to a variant of the β- subunit of the voltage gated Ca2+ channel and to actin, which is a component of some Ca2+ channels. |
| Eukaryotic Cell Culture Applications | Praziquantel is a potent anthelmintic against parasitic flatworms (flukes and tapeworms). |
| Molecular Formula | C19H24N2O2 |
| References |
Cioli D, Pica-Mattoccia L (2003) Praziquantel. Parasitol Res. 90 Supp 1:S3-9. PMID 12811543. Olliaro P, Delgado-Romero P, Keiser J (2014) The little we know about the pharmacokinetics and pharmacodynamics of praziquantel (racemate and R-enantiomer). J Antimicrob Chemother. 69(4):863-870 PMID 24390933 , , , , , , , ChemMedChem 2023, 18, e202300154. |