The Susceptibility of Plasmodium Falciparum in Vitro To Chlorpromazine and the Stereo‐isomeric Compounds Cis(z)‐ And Trans(E)‐Clopenthixol

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Abstract
New antimalaria drugs are needed on the background of increasing resistance to chloroquine. This study was undertaken to elucidate whether other membrane stabilizers than chloroquine have anti‐malarial activity in vitro. We here report the anti‐plasmodial activity of chlorpromazine (CPZ) and the stereo‐isomeric compounds cis(Z)‐ and trans(E)‐clopenthixol. As a screening method we used a modified Desjardins' 3H‐hypoxanthine assay. The IC50= 50% inhibition of 3H‐hypoxanthine uptake was found at 1.028 ng/ml = 3.2 μM CPZ, 758 ng/ml = 1.6 μM trans(E)‐clopenthixol and 436 ng/ml = 0.9 μM cis(Z)‐clopenthixol. The inhibitory effect of trans(E)‐clopenthixol in these low concentrations on Plasmodium falciparum in vitro seems particularly promising, since it is known that trans(E)‐clopenthixol has no neuroleptic effect.

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