Biochemical properties of spiperone binding to rat brain membranes.
Biochemical properties of spiperone binding to rat brain membranes.
复制标题
螺哌酮与大鼠脑膜结合的生化特性。
DOI：
10.1159/000137444
复制
发表时间：
1980
期刊：
影响因子：
3.1
通讯作者：
Wooten,GF
中科院分区：
文献类型：
--
作者：
Sundermann,RH;Wooten,GF
用大鼠纹状体膜匀浆和过滤分离法系统研究了~ 3 H-螺哌隆体外结合的生化特性。Scatchard分析显示一个单一的高亲和力位点，KD为0.14 nM，Bmax为26 fmol/mg组织。在平衡时通过测量获得的解离常数与通过测量缔合和解离速率获得的解离常数相似。高亲和力结合是立体特异性的，热不稳定的和高度pH依赖性的，在pH 7.6至7.8时最大。改变Na+、Ca++、Mg++、Mn++和Tris缓冲液的浓度对螺哌隆的特异性结合量没有显着影响。在神经递质中，多巴胺是特异性螺哌隆结合的最有效抑制剂，其次是5-羟色胺、肾上腺素和去甲肾上腺素。阿扑吗啡比多巴胺更有效，但不如氯丙嗪和未标记的螺哌隆。在大鼠大脑的八个区域中，证明了螺哌隆结合位点的数量与每个区域的多巴胺含量之间存在直接相关性，而这些区域之间的KD值没有重大差异。
The biochemical properties of3H-spiperone bindingin vitrowere studied systematically using a crude membrane homogenate of rat corpus striatum and separation by filtration. Scatchard analysis revealed a single high affinity site with a KDof 0.14 nMand Bmaxof 26 fmol/mg of tissue. The dissociation constant obtained by measurements at equilibrium was similar to that obtained by measuring the rates of association and dissociation. The high affinity binding was stereospecific, thermolabile and highly pH dependent, being maximal from pH 7.6 to 7.8. Varying the concentration of Na+, Ca++, Mg++, Mn++, and Tris buffer had no significant effect on the amount of specific spiperone binding. Of the neurotransmitters, dopamine was the most potent inhibitor of specific spiperone binding, followed by serotonin, epinephrine, and norepinephrine. Apomorphine was more potent than dopamine, but less so than chlorpromazine and unlabelled spiperone. In eight regions of the rat brain, a direct correlation between the number of spiperone binding sites and the dopamine content of each region was demonstrated, while there were no major difference in KDvalues among these regions.