High affinity binding sites for a somatostatin-28 analog in rat brain.
High affinity binding sites for a somatostatin-28 analog in rat brain.
复制标题
大鼠脑中生长抑素 28 类似物的高亲和力结合位点。
DOI：
10.1016/0024-3205(81)90628-7
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发表时间：
1981
期刊：
影响因子：
6.1
通讯作者：
W. Vale
中科院分区：
文献类型：
--
作者：
J. Reubi;M. Perrin;J. Rivier;W. Vale
使用生长抑素的大（28 个残基）和生物活性形式的碘化类似物 125I[Leu8,D-Trp22,Tyr25]SS-28，可以在大鼠皮质膜中证明可饱和且高亲和力的结合位点（解离常数 = 0.46 ± 0.04 nM）。生长抑素，生长抑素-28，以及两种有效的类似物，[D-Trp8]生长抑素和[D-Trp22]生长抑素-28，可以在纳摩尔范围内完全取代放射腺，而无活性的类似物Des-Trp8-生长抑素和不相关的肽GnRH对这些结合位点没有亲和力；生长抑素的八肽和九肽类似物没有活性。在海马、杏仁核、嗅结节、尾壳核和皮质中发现了高结合；中脑和下丘脑有中等结合，小脑没有结合。这些结果表明，可以用 125 I[Leu8,D-Trp22,Tyr25] SS-28 作为放射性配体来测量大脑内的特定生长抑素受体。
Using an iodinated analog of a large (28 residues) and biologically active form of somatostatin,125I[Leu8,D-Trp22,Tyr25]SS-28, it was possible to demonstrate saturable and high affinity binding sites (dissociation constant = 0.46 ± 0.04 nM) in rat cortical membranes. Somatostatin, somatostatin-28, as well as two potent analogs, [D-Trp8] somatostatin and [D-Trp22] somatostatin-28, could completely displace the radiogland in the nanomolar range whereas the inactive analog Des-Trp8-somatostatin and the unrelated peptide GnRH showed no affinity for these binding sites; octa- and nona-peptide analogs of somatostatin were inactive. High binding was found in hippocampus, amygdala, tuberculum olfactorium, caudate-putamen and cortex; moderate binding in midbrain and hypothalamus, and no binding in the cerebellum. These results suggest that specific somatostatin receptors can be measured within the brain with125I[Leu8,D-Trp22,Tyr25] SS-28 as radioligand.
DOI：
10.1016/0006-291x(80)91415-1
发表时间：
1980-01-01
影响因子：
3.1
作者：
BOHLEN, P;BRAZEAU, P;GUILLEMIN, R
通讯作者：
GUILLEMIN, R