Angevine L S, Nabeshima T, Ho I K, Mehendale H M
Exp Lung Res. 1981 May;2(2):71-84. doi: 10.3109/01902148109052304.
Chlorphentermine (CP) has been noted to cause primary pulmonary hypertension both clinically and experimentally. It was postulated that CP might affect the pulmonary clearance of endogenous vasoactive substances such as norepinephrine (NE). The uptake and metabolism of 14C-NE were followed in artificially ventilated isolated perfused rabbit lung preparations using a constituted perfusate with initial NE concentration of 5 micrograms/100 ml. Perfusate samples were analyzed for total radioactivity, metabolites, and parent compound. Preloading the lungs with 0.25 mM CP significantly increased the concentrations of total radioactivity, deaminated products, and decreased the concentration of normetanephrine in the perfusate. In addition, the accumulation of total radioactivity in the lung tissue after 60 min of perfusion was significantly decreased in CP-treated lungs. The proportion of deaminated metabolites in the lung tissue was slightly decreased while the percent of normetanephrine, and parent compound were significantly increased by the CP treatment. CP (0.1 mM) also inhibited the in vitro metabolism of NE by 79%. These results provide experimental evidence in support of a hindered pulmonary clearance of circulating NE by CP.
氯苯丁胺(CP)在临床和实验中均已被证实可引发原发性肺动脉高压。据推测,CP可能会影响内源性血管活性物质如去甲肾上腺素(NE)的肺清除率。在初始NE浓度为5微克/100毫升的人工配制灌注液的人工通气离体灌注兔肺制备物中,追踪14C-NE的摄取和代谢情况。对灌注液样本进行总放射性、代谢产物和母体化合物分析。用0.25毫摩尔CP对肺进行预负荷显著增加了灌注液中总放射性、脱氨基产物的浓度,并降低了去甲变肾上腺素的浓度。此外,灌注60分钟后,CP处理组肺组织中总放射性的积累显著减少。CP处理使肺组织中脱氨基代谢产物的比例略有下降,而去甲变肾上腺素和母体化合物的百分比则显著增加。CP(0.1毫摩尔)还可使NE的体外代谢抑制79%。这些结果提供了实验证据,支持CP阻碍循环中NE的肺清除。