ビペリジンN-誘導体のマウスにおける急性毒性と自発運動量抑制効果

概要

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Acute toxicity and depressive effect on spontaneous motor activity were examined on N-derivatives of piperidine as a model compound for piperidine and peperazine series analgesics, using untreated mice and mice pretreated with phenobarbital or SKF-525A. Acute toxicity of the derivatives with facile N-C cleavage by liver monooxygenase due to enzyme induction became weak but the depressive action became stronger, approaching close to that of piperidine, while acute toxicity and depressive action inversely changed into other direction on enzyme inhibition. Derivatives with difficult N-C cleavage showed hardly any change by derivation and inhibition. These results suggest that N-C cleavage is related to the depressive action of the derivatives, and this was also supported by the results of quantitative assay of piperidine in the blood and brain of mice given the derivatives. These results also suggest a correlation between acute toxicity and N-C cleavage but the toxicity is rapid-acting and central, so that this correlation cannot be definitely concluded.
公益社団法人日本薬学会の論文
1979-12-25