Kornhauser D M, Vestal R E, Shand D G
Pharmacology. 1980;20(5):275-83. doi: 10.1159/000137373.
The role of the alveolar macrophage in the uptake of 3H-propranolol by the isolated perfused rabbit lung and displacement of 3H-propranolol from this site has been investigated. Removal of 3H-propranolol (100 microgram) by the lung was characterized by a rapid distribution phase (t1/2 min) and a slower elimination phase with a clearance of 22.4 ml/min (t1/2 = 47 min). Addition of chlorpromazine (1 mg) at 30 min was followed by a twofold increase in perfusate concentrations of 3H-propranolol which was also associated with a reduction of 3H-propranolol in macrophages recovered from lungs at the end of perfusion experiments. Experiments using isolated alveolar macrophages demonstrated uptake of propranolol and marked inhibition by 100-fold higher concentrations of chlorpromazine and imipramine. In the intact dog, injection of imipramine (1 mg/kg) 60-70 min after bolus injection of 3H-propranolol (0.3 mg/kg) was associated with an immediate increase in blood levels of 3H-propranolol consistent with tissue redistribution. It is concluded that chlorpromazine and imipramine can displace propranolol from the lung,and that the alveolar macrophage is involved in this process.
已对肺泡巨噬细胞在离体灌注兔肺摄取3H-普萘洛尔以及从该部位置换3H-普萘洛尔中的作用进行了研究。肺对3H-普萘洛尔（100微克）的清除表现为快速分布期（t1/2分钟）和较慢的消除期，清除率为22.4毫升/分钟（t1/2 = 47分钟）。在30分钟时加入氯丙嗪（1毫克）后，3H-普萘洛尔的灌注液浓度增加了两倍，这也与灌注实验结束时从肺中回收的巨噬细胞中3H-普萘洛尔的减少有关。使用分离的肺泡巨噬细胞进行的实验表明，普萘洛尔被摄取，并且100倍高浓度的氯丙嗪和丙咪嗪对其有明显抑制作用。在完整的狗中，在推注3H-普萘洛尔（0.3毫克/千克）60 - 70分钟后注射丙咪嗪（1毫克/千克），与3H-普萘洛尔血药浓度立即升高有关，这与组织再分布一致。结论是氯丙嗪和丙咪嗪可从肺中置换出普萘洛尔，并且肺泡巨噬细胞参与了这一过程。
