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Caracemide was found to inhibit choline acetyltransferase (CAT) from rat brain. A concentration of 0.5 mM caracemide inhibited the enzyme by 93%, whereas a degradation product from caracemide, N-(methylcarbamoyloxy)acetamide, produced only a 50% inhibition. Two other degradation products, N-(methyl-carbamoyloxy)-N'-methylurea and N-hydroxy-N'-methylurea, lacked any inhibitory activity. With bovine brain CAT, caracemide showed noncompetitive inhibition with the substrate choline, Km 337 microM, Ki240 microM, Vmax 2.83 nmol acetylcholine formed/min/mg protein and mixed inhibition with the substrate acetyl-CoA, Km 21 microM, Ki 146 microM, Vmax 3.85 nmol acetylcholine formed/min/mg protein.

Methyl-CCNU (NSC-95441) was administered to patients with malignant melanoma in a split dose schedule. Nausea and vomiting were eliminated as clinical problems during therapy. Response rate to the drug seemed somewhat lower than the average of three previously reported disease-oriented phase II trials, though the difference was not significant statistically. The time course of myelosuppression seemed comparable to that seen with a single dose schedule of administration.

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