Abstract
The inhibitory effect of chlorpromazine on l-methionine transport was studied in the everted sac preparation of the rat intestine. Chlorpromazine inhibits only the sodium-dependent active component of l-methionine transport, without affecting the sodium-independent diffusion component. Inhibition of methionine transport by chlorpromazine is time dependent and concentration dependent. Half-maximal inhibition was observed at 5.2 × 10 −4 M chlorpromazine in the medium. No significant metabolism of chlorpromazine was observed during the experiment, suggesting that the unchanged chlorpromazine was the active inhibitor. Studies on a few chlorpromazine metabolites showed that demethylation in the aminopropyl side chain or ring hydroxylation at the 7-position in the chlorpromazine molecule did not affect the inhibitory activity on methionine transport, while oxidation at the sulfur atom completely abolished it.
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