Lung uptake of 131I-metaiodobenzylguanidine in sheep
Lung uptake of 131I-metaiodobenzylguanidine in sheep
复制标题
绵羊肺吸收 131I-间碘苄基胍
DOI：
10.1007/bf00253443
复制
发表时间：
1988
期刊：
影响因子：
--
通讯作者：
A. Donath
中科院分区：
文献类型：
--
作者：
D. Slosman;D. Morel;P. M. Mo Costabella;A. Donath
已知循环生物胺由哺乳动物肺清除。它们的肺摄取被认为是肺内皮完整性的指标。不幸的是，由于它们的生物学效应和放射性标记的类型（3 H和14 C），它们在人类病理学中作为肺代谢功能的标志物的用途被排除在外，这使得它们对重复注射有害，并且不适合肺动脉造影。间碘苄基胍（MIBG）在结构上与神经元阻断剂乙啶相关，没有显著的生物学效应，并且已显示在体外灌注的大鼠肺中通过与去甲肾上腺素相同的活性钠依赖性饱和转运被提取。我们研究了在5只清醒和5只麻醉的绵羊中，使用标准的双指示剂稀释技术，以99 mTc-人血清白蛋白（HSA）作为血管内参考示踪剂，单次通过肺提取131 I-MIBG。静脉推注剂量增加至400 nmol的MIBG导致清醒和麻醉绵羊中MIBG提取的显著（F比=7.778，P<0.0001）剂量依赖性降低，两组之间的提取值无显著差异。对于10只绵羊，稀释曲线峰值处MIBG的平均单次肺摄取百分比从20 nmol的32%±3%（平均值±SE，n=27次测量）降至400 nmol的18%±2%（n=32）。表观米氏常数（Km）的估计值平均为2±1.2 μM（n=7），而表观最大清除速度（Vmax）的估计值为1.1±0.5 μmol/min（n=7）。与一些受试者间变异性相反，药代动力学参数显示受试者内变异很小。未发现MIBG提取、Km或Vmax值与血液动力学或气体交换参数之间存在相关性。这些数据表明，使用标准的双重稀释技术，可以在体内测定MIBG的肺提取。其肺清除是剂量有限的，其特征可能是米氏动力学常数，表明一个饱和的过程。与去甲肾上腺素相反，γ发射体标记的MIBG因此可能是使用非侵入性闪烁照相方法在体内监测肺内皮细胞功能的合适化合物。
Circulating biogenic amines are known to be cleared by the mammalian lung. Their lung uptake is considered as an indicator of pulmonary endothelial integrity. Unfortunately, their use as markers of pulmonary metabolic function in human pathology is precluded by their biological effects and by the type of radiolabeling (3H and 14C), making them harmful for repeat injections and unfit for scintigraphy. Metaiodobenzylguanidine (MIBG) is structurally related to the neuron blocking agent guanethidine, devoid of significant biological effects, and has been shown to be extracted by the same active sodium dependent, saturable transport as norepinephrine in perfused rat lungs in vitro. We studied the single pass lung extraction of 131I-MIBG in five awake and five anaesthetised sheep using the standard double indicator dilution technique with 99mTc-human serum albumin (HSA) as an intravascular reference tracer. Intravenous bolus injection of increasing doses of MIBG up to 400 nmol resulted in a significant (F ratio=7.778, P<0.0001) dose dependent decrease of MIBG extraction in both awake and anaesthetised sheep, without significant differences of extraction values between the two groups. For the 10 sheep, the averaged percentage single pass pulmonary uptake of MIBG at the peak of the dilution curve decreased from 32%±3% (mean±SE, n=27 measurements) with 20 nmol to 18%±2% (n=32) with 400 nmol. Estimates of the apparent Michaelis-Menten constant (Km) averaged 2±1.2 μM (n=7), whereas estimates of the apparent maximum velocity of removal (Vmax) was 1.1±0.5 μmol/min (n=7). In contrast to some intersubject variability, the pharmacokinetic parameters showed little intra subject variation. No correlation was found between MIBG extraction, Km or Vmax values and haemodynamic or gas exchange parameters. These data indicate that using a standard double dilution technique, lung extraction of MIBG may be determined in vivo. Its lung removal is dose limited and may be characterised by the Michaelis-Menten kinetic constants suggesting a saturable process. In contrast to norepinephrine, the gamma emitter labeled MIBG could therefore be a suitable compound to monitor pulmonary endothelial cell function in vivo using a non invasive scintigraphic method.
培养的牛肾上腺髓质细胞摄取间碘苄基胍和去甲肾上腺素的钠依赖性的比较。
影响因子：
3.6
作者：
JaquesJr,S;Tobes,MC;Sisson,JC;Baker,JA;Wieland,DM
通讯作者：
Wieland,DM
狗肺中血清素摄取的动力学。
DOI：
10.1152/jappl.1981.51.2.405
发表时间：
1981
期刊：
Journal of applied physiology: respiratory, environmental and exercise physiology
影响因子：
--
作者：
Rickaby,DA;Linehan,JH;Bronikowski,TA;Dawson,CA
通讯作者：
Dawson,CA
血液和血浆流速对肺部吸收血清素动力学的影响。
DOI：
10.1152/jappl.1982.53.3.677
发表时间：
1982
期刊：
Journal of applied physiology: respiratory, environmental and exercise physiology
影响因子：
--
作者：
Rickaby,DA;Dawson,CA;Linehan,JH
通讯作者：
Linehan,JH