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The chemo therapy of rodent malaria part 25 anti malarial activity of wr 122455 a 9 phenanthrenemethanol in vivo and in vitro






Annals of Tropical Medicine and Parasitology 70(3): 259-270

The chemo therapy of rodent malaria part 25 anti malarial activity of wr 122455 a 9 phenanthrenemethanol in vivo and in vitro

WR 122,455, 3,6-bis(trifluoromethyl)-.alpha.-(2-piperidinyl)-9-phenanthrenemethanol HCl, suppresses infection with drug-sensitive Plasmodium berghei N strain in mice. It acts rapidly and affects all the stages of the asexual intraerythrocytic parasites, the effective dose levels being about 3 times those of chloroquine and 1/12-1/15 those of quinine. Under the influence of WR 122,455 hemozoin seems to disappear from the affected parasites following an initial coarsening of the fine pigment granules. These changes are similar to those exerted by quinine. Large doses of WR 122,455 have a residual affect due in part at least to deposition of insoluble material in the tissues. The drug appears to exert an antagonistic action on chloroquine when both drugs are administered simultaneously. It has no casual prophylactic effect. In vitro WR 122,455 is a competitive antogonist of chloroquine in a similar manner to quinine and appears to have a Kd of 2.26 .times. 10-8 M, making it about 18 times as active as quinine. WR 122,455 interacts strongly with calf thymus DNA, but the mechanism of interaction has yet to be defined. Mice tolerate single doses of a saline/Tween 80 suspension up to about 400 mg/kg but s.c. administration induces necrotic changes at the injection site. Up to 30 mg/kg daily p.o. for 7 consecutive days is well tolerated systemically but local tissue reaction may occur if the drug is given by the s.c. or i.p. routes. Systemically up to 60 mg/kg is tolerated s.c. or i.p. The relation of WR 122,455 to drug resistant malaria will be reported later.


Accession: 006614076



Related references

Peters, W.; Porter, M., 1976: The chemo therapy of rodent malaria part 26 the potential value of wr 122455 a 9 phenanthrenemethanol against drug resistant malaria parasites. The phenanthrenemethanol compound WR 122,455 is an effective blood schizontocide against lines of Plasmodium berghei that are highly resistant to primaquine, sulfonamides, pyrimethamine and cycloguanil. It is also active against the NS line that i...

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