BENZODIAZEPINE RECEPTORS ALONG THE NEPHRON - [PK-11195-H-3 BINDING IN RAT TUBULES
BENZODIAZEPINE RECEPTORS ALONG THE NEPHRON - [PK-11195-H-3 BINDING IN RAT TUBULES
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DOI：
10.1016/0014-5793(84)80305-1
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发表时间：
1984-01-01
期刊：
影响因子：
3.5
通讯作者：
BUTLEN, D
中科院分区：
文献类型：
--
作者：
BUTLEN, D
在显微解剖的大鼠肾小管段上，测定了异喹啉甲酰胺类化合物[~3H]PK-11195的结合。在粗大的Henle‘s环升支和集合管中有较高的特异性结合容量(1.1~1.8fmol·mm−-1)，而在近端小管未检测到特异性结合。在延髓集合管中，4℃时的结合和解离速率常数分别为1=3.0×10 6M−1·m in−1和k−1=0.021 m in−1，其比值−1/k 1=7.0 nM与估算的平衡解离常数(Kd=2.4 nM)一致。[3 H]大鼠延髓升支和延髓集合管的[3 H]PK 11195结合位点具如下特异性序列：PK 11195=Ro 5-4 864⪢氯硝西潘，提示肾小管结合部位可能是大鼠肾脏的外周苯二氮卓受体。
Binding of [3H]PK 11195, an isoquinoline carboxamide derivative, was measured in microdissected tubule segments of rat nephron. High specific binding capacities (1.1–1.8 fmol·mm−1) were found in the thick ascending limb of the Henle's loop and in the collecting tubule, whereas specific binding could not be detected in the proximal tubule. In the medullary collecting tubule, the association and dissociation rate constants at 4°C werek1= 3.0 × 106M−1·min−1andk−1= 0.021 min−1; the ratiok−1/k1= 7.0 nM was in agreement with the estimated equilibrium dissociation constant (Kd= 2.4 nM). [3H]PK 11195 binding sites from medullary ascending limb and medullary collecting tubule revealed the following sequence of specificity: PK 11195 = Ro 5-4864 ⪢ clonazepan, indicating that tubule binding sites might be the peripheral benzodiazepine receptors of the rat kidney.