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犬体内胺碘酮新代谢产物二 - N - 去乙基胺碘酮的高效液相色谱分离与快原子轰击质谱鉴定

High-performance liquid chromatographic isolation and fast atom bombardment mass spectrometric identification of Di-N-desethylamiodarone, a new metabolite of amiodarone in the dog.

作者信息

Latini R, Reginato R, Burlingame A L, Kates R E

出版信息

Biomed Mass Spectrom. 1984 Sep;11(9):466-71. doi: 10.1002/bms.1200110906.

Abstract

Amiodarone is an antiarrhythmic drug which has received considerable attention in recent years. It has been suggested that the unusual pharmacodynamic characteristics of this drug may be due in part to the influence of active metabolites. Using fast atom bombardment (FAB) mass spectrometry we have identified a new metabolite of amiodarone, the di-N-desethyl analog (DDEA). This metabolite was present in the blood of dogs treated with the parent drug, and showed a greater affinity for myocardium than did the parent drug. The unique features of FAB mass spectrometry over electron impact mass spectrometry was an essential element in facilitating the identification of this new metabolite. Whether or not this metabolite has pharmacologic activity or is responsible for some of the side effects occurring during amiodarone administration is not known.

摘要

胺碘酮是一种近年来备受关注的抗心律失常药物。有人提出,这种药物不同寻常的药效学特性可能部分归因于活性代谢产物的影响。我们使用快原子轰击(FAB)质谱法鉴定出了胺碘酮的一种新代谢产物,即二 - N - 去乙基类似物(DDEA)。这种代谢产物存在于用母体药物治疗的犬的血液中,并且对心肌的亲和力比母体药物更高。FAB质谱法相对于电子轰击质谱法的独特特性是有助于鉴定这种新代谢产物的关键因素。这种代谢产物是否具有药理活性或是否导致胺碘酮给药期间出现的某些副作用尚不清楚。

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