James M I, Midgley J M, Williams C M
J Pharm Pharmacol. 1983 Sep;35(9):559-65. doi: 10.1111/j.2042-7158.1983.tb04333.x.
The metabolism of (+/-)-o-octopamine and (+/-)-o-synephrine by rats was studied quantitatively by a gas chromatography-mass spectrometry-selected ion monitoring (g.c.-m.s.-s.i.m.) method using deuterated internal standards. When o-octopamine was injected intraperitoneally into rats four metabolites were excreted in the urine: (i) unconjugated o-hydroxymandelic acid (OHMA) (16%), (ii) unconjugated o-hydroxyphenylglycol (OHPG) (4.5%), (iii) an acid-hydrolysable conjugate of OHPG (28%) and (iv) unconjugated o-octopamine (10%). When o-synephrine benzoate was similarly administered six metabolites were excreted in urine: (i) unconjugated OHMA (13.5%), (ii) unconjugated OHPG (3.3%), (iii) an acid-hydrolysable conjugate of OHPG (15.6%), (iv) unconjugated o-synephrine (10%), (v) an acid-hydrolysable conjugate of o-synephrine (8.5%) and (vi) unconjugated o-octopamine (0.3%). Adult rats normally excreted OHMA (1.0 micrograms day-1) but OHPG, o-octopamine and o-synephrine could not be detected in urine. After the administration of a monoamine oxidase inhibitor, unconjugated o-octopamine (0.3 micrograms day-1) was excreted in urine but OHPG and o-synephrine could not be detected. o-Tyramine given to rats afforded urinary o-octopamine (75 ng day-1) and this was increased 10-fold upon co-administration of a monoamine oxidase inhibitor and o-tyramine.
采用气相色谱 - 质谱 - 选择离子监测（g.c.-m.s.-s.i.m.）法并使用氘代内标，对大鼠体内（±）-邻去甲肾上腺素和（±）-邻辛弗林的代谢进行了定量研究。当向大鼠腹腔注射邻去甲肾上腺素时，有四种代谢产物经尿液排出：（i）未结合的邻羟基扁桃酸（OHMA）（16%），（ii）未结合的邻羟基苯乙二醇（OHPG）（4.5%），（iii）OHPG的酸可水解共轭物（28%），以及（iv）未结合的邻去甲肾上腺素（10%）。当以类似方式给予辛弗林苯甲酸酯时，有六种代谢产物经尿液排出：（i）未结合的OHMA（13.5%），（ii）未结合的OHPG（3.3%），（iii）OHPG的酸可水解共轭物（15.6%），（iv）未结合的邻辛弗林（10%），（v）邻辛弗林的酸可水解共轭物（8.5%），以及（vi）未结合的邻去甲肾上腺素（0.3%）。成年大鼠正常情况下经尿液排出OHMA（1.0微克/天），但尿液中未检测到OHPG、邻去甲肾上腺素和邻辛弗林。给予单胺氧化酶抑制剂后，尿液中排出了未结合的邻去甲肾上腺素（0.3微克/天），但未检测到OHPG和邻辛弗林。给大鼠注射酪胺后，尿液中出现了邻去甲肾上腺素（75纳克/天），在同时给予单胺氧化酶抑制剂和酪胺后，其含量增加了10倍。
