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- W1990443314 abstract "SUMMARY The mechanism whereby praziquantel produces a contraction and subsequent flaccid paralysis (a loss of sensitivity to subsequent stimuli) of Schistosoma mansoni in a medium containing an elevated Mg 2+ :Ca 2+ ratio was investigated. In RPMI, praziquantel produced a concentration-dependent tonic contraction of the parasite with an EC 50 of 200 nM. Magnesium inhibited the contraction in such a manner as to convert the tonic contraction to a phasic one without altering the peak force generated. The Mg 2+ -dependent block was non-competitive with praziquantel but was competitive with extracellular Ca 2+ , ratios of 7·5:1; Mg 2+ : Ca 2+ being needed to inhibit the tonic contraction and to induce flaccid paralysis. Flaccid paralysis was associated with a reduced ability of the parasite to take up 45 Ca 2+ from the bath compared to parasites that had not entered into flaccid paralysis and flaccid paralysis was reversible. Recovery from flaccid paralysis was accelerated by treatments that are expected to increase Ca 2+ uptake by the parasite. At a concentration of 500 nM, praziquantel produced 2 distinct phasic contractions in intact parasites incubated in an elevated [Mg 2+ ] medium but only 1 phasic contraction in parasites lacking their surface tegumental membranes. In zero Ca 2+ I-RPMI, 10 μM praziquantel produced a phasic contraction of intact parasites but did not stimulate contraction of detegumented parasites until Ca 2+ was reintroduced into the bath. These results indicate that praziquantel interacts with specific Ca 2+ -permeable sites in the tegumental and sarcoplasmic membranes of the parasite and that under these conditions of elevated Mg 2+ :Ca 2+ ratios, these sites become blocked by Mg 2+ , leading to flaccid paralysis of the parasite." @default.
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- W1990443314 date "1992-02-01" @default.
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- W1990443314 title "Praziquantel: physiological evidence for its site(s) of action in magnesium-paralysed <i>Schistosoma mansoni</i>" @default.
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- W1990443314 doi "https://doi.org/10.1017/s0031182000060807" @default.
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