Chai S Y, Allen A M, Adam W R, Mendelsohn F A
J Cardiovasc Pharmacol. 1986;8 Suppl 10:S35-9.
In order to gain insight into the local actions of angiotensin II (ANG II) we have determined the distribution of a component of the effector system for the peptide, the ANG II receptor, and that of an enzyme-catalysing ANG II formation, angiotensin converting enzyme (ACE), by in vitro autoradiography in several target tissues. The superagonist ANG II analog, 125I[Sar1]ANG II, or the antagonist analog, 125I[Sar1,Ile8]ANG II, were used as specific radioligands for ANG II receptors. A derivative of the specific ACE inhibitor, lysinopril, called 125I-351A, was used to label ACE in tissues. In the adrenal, a high density of ANG II receptors occurs in the glomerulosa zone of the cortex and in the medulla. ACE is also localized in these two zones, indicating that local production of ANG II may occur close to its sites of action in the zona glomerulosa and adrenal medulla. In the kidney, a high density of ANG II receptors is associated with glomeruli in the cortex and also with vasa recta bundles in the inner stripe of the outer medulla. ACE is found in very high concentration in deep proximal convoluted tubules of the cortex, while much lower concentrations of the enzyme occur in the vascular endothelium throughout the kidney. In the central nervous system three classes of relationships between ANG II receptors and ACE are observed: In the circumventricular organs, including the subfornical organ and organum vasculosum of the lamina terminalis, a high concentration of both components occurs. Since these structures have a deficient blood-brain barrier, local conversion of circulating angiotensin I (ANG I) to ANG II may contribute to the action of ANG II at these sites.(ABSTRACT TRUNCATED AT 250 WORDS)
为深入了解血管紧张素II(ANG II)的局部作用,我们通过体外放射自显影术,在多个靶组织中确定了该肽的效应系统成分——ANG II受体,以及催化ANG II形成的酶——血管紧张素转换酶(ACE)的分布。超激动剂ANG II类似物125I[Sar1]ANG II或拮抗剂类似物125I[Sar1,Ile8]ANG II被用作ANG II受体的特异性放射性配体。特异性ACE抑制剂赖诺普利的衍生物125I - 351A用于标记组织中的ACE。在肾上腺中,皮质的球状带和髓质存在高密度的ANG II受体。ACE也定位于这两个区域,表明ANG II可能在球状带和肾上腺髓质中其作用位点附近局部产生。在肾脏中,高密度的ANG II受体与皮质中的肾小球以及外髓质内带的直小血管束相关。ACE在皮质深层近端曲管中的浓度非常高,而该酶在整个肾脏的血管内皮中的浓度要低得多。在中枢神经系统中,观察到ANG II受体与ACE之间存在三类关系:在室周器官,包括穹窿下器官和终板血管器,这两种成分都有高浓度存在。由于这些结构的血脑屏障有缺陷,循环中的血管紧张素I(ANG I)局部转化为ANG II可能有助于ANG II在这些部位发挥作用。(摘要截短于250字)