Aislaitner G, Bello A, Tan S C, Hutt A J, Marriott C, Gorrod J W
Chelsea Department of Pharmacy, King's College London, University of London, UK.
Eur J Drug Metab Pharmacokinet. 1997 Oct-Dec;22(4):395-402. doi: 10.1007/BF03190976.
The metabolism of (-)-(S)-nicotine has been investigated following intratracheal administration to the recirculating perfused rabbit lung model. The metabolic products present in the perfusate were identified by co-chromatography (HPLC and GC) with authentic standards and quantified by HPLC. After the 180 min perfusion period, nicotine was found to be metabolically transformed to cotinine (33.7%), 3-hydroxycotinine (10.4%), cotinine-1-N-oxide (3.4%) and nicotine-1'-N-oxide (14.4%). Norcotinine, nornicotine, 3-pyridyl-4-oxo-N-methylbutyramide and an uncharacterised metabolite were also detected in low amounts. Following the perfusion experiment, part of the lung tissue was homogenised in the presence of [14C]-sodium cyanide. Subsequent analysis of the homogenates indicated the formation of 2'-cyanonicotine, 1'-cyanomethylnornicotine and the diastereoisomeric 5'-cyanonicotines.
在将(-)-(S)-尼古丁经气管给药至再循环灌注兔肺模型后,对其代谢情况进行了研究。通过与标准品共色谱法(HPLC和GC)鉴定灌注液中存在的代谢产物,并通过HPLC进行定量。在180分钟的灌注期后,发现尼古丁经代谢转化为可替宁(33.7%)、3-羟基可替宁(10.4%)、可替宁-1-N-氧化物(3.4%)和尼古丁-1'-N-氧化物(14.4%)。还检测到少量的去甲可替宁、去甲烟碱、3-吡啶基-4-氧代-N-甲基丁酰胺和一种未鉴定的代谢产物。在灌注实验后,将部分肺组织在[14C]-氰化钠存在下匀浆。随后对匀浆的分析表明形成了2'-氰基尼古丁、1'-氰基甲基去甲烟碱和非对映异构的5'-氰基尼古丁。