新鎮痛剤1,4-Dimethyl-10-hydroxy-2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benzazonine Hydrobromide(ST-2121)の生体内運命(第2報)光学異性体間におけるラット尿中代謝物の比較

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The metabolism of ST-2121 was investigated in rat urine after subcutaneous administration of ^<14>C-labeled and non-labeled compounds. The metabolites were characterized by radio-thin-layer chromatography and gas chromatography-mass spectrometry. ST-2121 (M-I), 9,10-dihydroxy-1,4-dimethyl-2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benzazonine (M-II), 9-hydroxy-10-methoxy (or 9-methoxy-10-hydroxy)-1,4-dimethyl-2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benzazonine (M-III), 10-hydroxy-1-methyl-2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benzazonine (M-IV) and their glucuronides were identified. d-, l- or dl-ST-2121 was administered to rats and M-I, M-II, M-III and M-IV excreted in the urine were determined by mass fragmentography. Remarkable differences were observed between d- and l-isomers with respect to the excretion rate of M-I, M-II and M-III, however, the excretion rate of M-IV was the same among the optical isomers.
1980-04-25