METABOLISM OF VASODILATOR 4-(3,4,5-TRIMETHOXYCINNA-MOYL)-1-(1-PYRROLIDINYL) CARBONYLMETHYLPIPERAZINE (CINEPAZIDE) : ISOLATION AND IDENTIFICATION OF METABOLITES IN THE RAT AND MAN

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概要

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• Further study on identification of metabolites of cinepazide, 4-(3,4,5-trimethoxycinnamoyl)-1-(1-pyrrolidinyl) carbonylmethylpiperazine, in rats and men was carried out. New metabolites of cinepazide in rat urine were 4-[1-[4-(3,4,5-trimethoxycinnamoyl)-piperazinyl] acetamido]-1-butanol (M-II), 4-(3,4,5-trimethoxycinnamoyl)-1-[1-(hydroxypyrrolidinyl)] carbonylmethylpiperazine (M-IV) and 4-[1-{4-(3,4,5-trimethoxycinnamoyl) piperazinyl} acetamido]-1-butyric acid (M-VI). Structures of two mono-O-demethylated metabolites of cinepazide predicted in the previous paper were assigned as 3-hydroxy-4,5-dimethoxycinnamoyl and 4-hydroxy-3,5-dimethoxycinnamoyl compounds (M-III and M-V) by the FT-NMR spectrometry measured in a mixture of CDCl_3-C_6D_6 (1 : 1,v/v) after methylation with dimethylsulfate-d_6. The corresponding pyrrolidone metabolite of cinepazide was undetectable in rat urine. New metabolites of cinepazide in rat feces were found to be 4-(3,5-dihydroxy-phenethylcarbonyl)-1-(1-pyrrolidinyl) carbonylmethylpiperazine (M-VIII) and 4-(3,5-dihydroxycinnamoyl)-1-(1-pyrrolidinyl) carbonylmethylpiperazine (M-IX). Metabolitcs of cinepazide in human urine were studied by both methods-high performance liquid chromatography and mass spectrometry with ion cluster technique. Unchanged drug was mainly excreted in the urine, and M-VI was the major urinary metabolite. The existence of M-IV and M-V was suggested by high performance liquid chromatography. The corresponding pyrrolidone was also undetectable in human urine.

• 公益社団法人日本薬学会の論文

著者

• Nomura Hisashi

  Drug Metabolism Research Center Research Institute Daiichi Seiyaku Co. Ltd.

• SANO MITSUJI

  Drug Metabolism Research Center, Research Institute, Daiichi Seiyaku Co., Ltd.

• Sano Mitsuji

  Drug Metabolism Research Center Research Institute Daiichi Seiyaku Co. Ltd.

• TSUMURA MITSUYOSHI

  Drug Metabolism Research Center, Research Institute, Daiichi Seiyaku Co., Ltd.

• TAKASUGI NORIO

  Drug Metabolism Research Center, Research Institute, Daiichi Seiyaku Co., Ltd.

• Takasugi Norio

  Drug Delivery Research Center Developmental Research Laboratories Daiichi Pharmaceutical Co. Ltd.

• Takasugi Norio

  Drug Metabolism Research Center Research Institute Daiichi Seiyaku Co. Ltd.

• Tsumura Mitsuyoshi

  Drug Metabolism Research Center Research Institute Daiichi Seiyaku Co. Ltd.

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• METABOLISM OF VASODILATOR 4-(3,4,5-TRIMETHOXYCINNA-MOYL)-1-(1-PYRROLIDINYL) CARBONYLMETHYLPIPERAZINE (CINEPAZIDE) : ISOLATION AND IDENTIFICATION OF METABOLITES IN THE RAT AND MAN

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