Multiple serotonin receptors: regional distribution and effect of Raphe lesions.
Multiple serotonin receptors: regional distribution and effect of Raphe lesions.
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多种血清素受体：中缝病变的区域分布和影响。
DOI：
10.1016/0014-2999(81)90103-5
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发表时间：
1981
影响因子：
5
通讯作者：
Sanders-Bush,E
中科院分区：
文献类型：
--
作者：
Blackshear,MA;Steranka,LR;Sanders-Bush,E
这些研究证实并扩展了最近的工作，表明[3 H]麦角酸二乙酰胺（LSD）标记两个不同的结合位点在大鼠脑类似5-羟色胺（5 HT）受体。虽然Scatchard分析[3 H]LSD结合到从皮层/海马制备的膜是线性的，[3 H]LSD结合位点的异质性在置换研究中被清楚地证明。5 HT和螺哌隆的位移曲线均为双S形，使高亲和力组分饱和所需的浓度比使低亲和力组分饱和所需的浓度低近3个数量级。加和性研究表明，5-HT和螺哌隆的高亲和力的网站是不同的，独立的网站。这些位点分别被称为5 HT 1和5 HT 2。区域分析表明，在额叶皮层，5 HT 2位点的密度略大于5 HT 1位点，而5 HT 1位点在所有其他脑区（包括脊髓）中占主导地位。这两个网站的药理学性质具有共同的功能与5 HT受体，然而，中脑中缝核的电解病变并没有改变两个明显的5 HT受体亚型的密度或结合常数，即使高亲和力的5 HT摄取位点的数量显着减少。
These studies confirm and extend the recent work suggesting that [3H]lysergic acid dielhylamide (LSD) labels two distinct binding sites in rat brain resembling serotonin (5HT) receptors. Although Scatchard analyses of [3H]LSD binding to membranes prepared from cortex/hippocampus were linear, the heterogeneity of the [3H]LSD binding sites was clearly demonstrated in displacement studies. The displacement curves for both 5HT and spiperone were bisigmoidal with the concentration required to saturate the high affinity components nearly 3 orders of magnitude lower than the concentrations necessary to saturate the low affinity components. Additivity studies suggested that the sites with high affinity for 5HT and spiperone are different, independent sites. These sites are referred to as 5HT1and 5HT2, respectively. Regional analyses showed, that in the frontal cortex, the density of the 5HT2site was slightly greater than the 5HT1site, whereas the 5HT1, site was predominant in all other brain areas, including the spinal cord. The pharmacological properties of the two sites have features in common with 5HT receptors; however, electrolytic lesions of the midbrain raphe nuclei did not change the densities or binding constants of the two apparent 5HT receptor subtypes, even though the number of high affinity 5HT uptake sites was markedly reduced.