PHARMACOLOGICAL STUDIES ON DL-PIPERONYLMETHYLAMINOPROPANE : II TOXICITY AND CENTRAL ACTION

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The toxicity and central action of dl-piperonyl-methylaminopropane (dl-PMAP) were investigated in mice and rabbits.1) After 24 hr the LD<SUB>50</SUB> of the dl-PMAP which was injected in mice subcutaneously was 56.2μg/g. It was clearly greater than that of methamphetamine (25.5μg/g).2) With dl-PMAP 1- 2μg/g injected in mice subcutaneously, symptoms of sedation were noted. The stimulant actions were, however, elicited after the administration of 5μg/g and over.3) Decrease of norepinephrine content in mouse brain occurred 5 min after the administration of dl-PMAP, and a transient recovery of norepinephrine content was observed after 10 min of the drug. However, it then decreased again gradually to less than the control level 3 hr later.4) The sleeping time with hexobarbital, thiopental and pentobarbital was reduced by the administration of dl-PMAP 10μg/g. Furthermore, with the administration of dl-PMAP the sleeping time produced by the combined administration of reserpine and hexobarbital was reduced markedly, while that produced by the chlorpromazine and hexobarbital was hardly shortened. In the experiments with reserpine and hexobarbital, dl-PMAP caused the lowering of norepinephrine content in mouse brain. But in. that with chlorpromazine and hexobarbital it produced almost no change in norepinephrine content.5) The high voltage and large waves appeared, and small waves diminished in the encephalogram immediately after the administration of 1 mg/kg of dl-PMAP in rabbit ear vein.From these experimental results, the toxicity and central excitation caused by dl-PMAP were found to be weaker than that of methamphetamine. In addition the mechanism of action on the central nervous system excitement caused by the drugs was discussed freely.dl-PMAP might be useful as a mild “wake amine” or as a phenylalkylamine giving priority to peripheral action over central action.

PHARMACOLOGICAL STUDIES ON DL-PIPERONYLMETHYLAMINOPROPANE : II TOXICITY AND CENTRAL ACTION

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