High affinity [3H]flunitrazepam binding: characterization, localization, and alteration in hypertension.
High affinity [3H]flunitrazepam binding: characterization, localization, and alteration in hypertension.
复制标题
高亲和力[3H]氟硝西泮结合：高血压的特征、定位和改变。
DOI：
10.1016/0024-3205(81)90744-x
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发表时间：
1981
期刊：
影响因子：
6.1
通讯作者：
Roeske,WR
中科院分区：
文献类型：
--
作者：
Regan,JW;Yamamura,HI;Yamada,S;Roeske,WR
在单侧肾切除大鼠的肾脏和大脑皮层制备的膜中研究[3H]氟硝西泮的结合，这些大鼠通过同时给予醋酸去氧皮质酮（DOCA）和氯化钠而患上高血压。在高血压大鼠的肾膜中发现 [3H]氟硝西泮结合位点 (Bmax) 的数量显着增加了 35-43%；从大脑皮层获得的膜中结合位点的密度没有变化。 Kdof [3H]氟硝西泮结合在肾脏或脑膜中均未改变（肾脏中约 12 nM，大脑中约 2.0 nM）。肾膜药物特异性研究表明，各种苯二氮卓类药物对[3H]氟硝西泮结合的抑制作用与其作为抗焦虑药的药理效力不相符。在牛肾中发现了特异性[3H]氟硝西泮结合的肾内分布；特异性结合在外皮质中最强，而在髓质、小萼和肾动脉中几乎不存在。肾脏苯二氮卓结合位点具有高亲和力、特异性、分布独特且在高血压期间受到调节的证据表明它可能与重要的病理生理结构有关。
The binding of [3H]flunitrazepam was studied in membranes prepared from the kidney and cerebral cortex of unilaterally nephrectomized rats made hypertensive by simultaneous deoxycorticosterone acetate (DOCA) and NaCl administration. A significant 35–43% increase in the number of [3H]flunitrazepam binding sites (Bmax) was found in the renal membranes prepared from the hypertensive rats; there was no change in the density of binding sites in the membranes obtained from the cerebral cortex. The Kdof [3H]flunitrazepam binding did not change either in the renal or in the cerebral membranes (∼ 12 nM in the kidney and ∼2.0 nM in the brain). Drug specificity studies with renal membranes showed that the inhibition of [3H]flunitrazepam binding by various benzodiazepines did not jibe with their pharmacologic potency as anxiolytic agents. An intrarenal distribution of specific [3H]flunitrazepam binding was found in the bovine kidney; specific binding was greatest in the outer cortex and virtually absent in the medulla, the minor calyx and the renal artery. The evidence that the renal benzodiazepine binding site is of high affinity, is specific, has a unique distribution, and is regulated during hypertension suggests that it may be associated with an important pathophysiologic structure.