[125I]SCH 23982在人脑中的结合特性：与[3H]SCH 23390的比较

Characterization of [125I]SCH 23982 binding in human brain: comparison with [3H]SCH 23390.

作者信息

Laruelle M, Sidhu A, Casanova M F, Weinberger D R, Kleinman J E

机构信息

Neuropathology Section, IRP, NIMH Neuroscience Center, Saint Elizzbeths, Washington, DC.

出版信息

Neurosci Lett. 1991 Oct 14;131(2):273-6. doi: 10.1016/0304-3940(91)90631-3.

DOI:10.1016/0304-3940(91)90631-3

PMID:1837073

Abstract

We studied binding of [125I]SCH 23982 in two regions of human brain, the caudate and the dorsolateral prefrontal cortex. Binding characteristics of [125I]SCH 23982 and of the non-iodinated tritiated analogue, [3H]SCH 23390, were compared. In caudate, binding of [125I]SCH 23982 was consistent with binding to D1 dopamine receptors while in frontal cortex, [125I]SCH 23982 bound mostly to serotonergic 5HT2 receptors. In contrast to [3H]SCH 23390, no evidence of binding of [125I]SCH 23982 to D1 receptors could be found in human frontal cortex. This indicates that iodination of SCH 23390 induces a decrease in its relative D1 versus 5HT2 selectivity that prohibits the use of [125I]SCH 23982 to label D1 receptors in human cortex.

摘要

我们研究了[125I]SCH 23982在人脑两个区域，即尾状核和背外侧前额叶皮质的结合情况。比较了[125I]SCH 23982与非碘化的氚代类似物[3H]SCH 23390的结合特性。在尾状核中，[125I]SCH 23982的结合与D1多巴胺受体的结合一致，而在额叶皮质中，[125I]SCH 23982主要与血清素能5HT2受体结合。与[3H]SCH 23390不同，在人类额叶皮质中未发现[125I]SCH 23982与D1受体结合的证据。这表明SCH 23390的碘化导致其相对D1与5HT2选择性降低，从而禁止使用[125I]SCH 23982标记人类皮质中的D1受体。