Chivers J, Jenner P, Marsden C D
Br J Pharmacol. 1987 Mar;90(3):467-78. doi: 10.1111/j.1476-5381.1987.tb11196.x.
[3H]-spiperone is commonly used to label dopamine receptors in vitro in brain tissue. However, spiperone also interacts with brain 5-hydroxytryptamine and noradrenaline receptors. In vivo, [3H]-spiperone has been used for identifying dopamine receptors in both animals and man but the nature of the sites identified is unknown. The in vivo administration of [3H]-spiperone to rats leads to a selective accumulation of radioactivity in the olfactory lobes, tuberculum olfactorium, nucleus accumbens, striatum, substantia nigra, hippocampus, frontal cortex and hypothalamus, when compared to the cerebellum. In vivo drug displacement studies suggest that the binding of [3H]-spiperone in these areas may be to dopamine, 5-HT or noradrenaline receptors. [3H]-spiperone in vivo mainly labels dopamine receptors in striatum, tuberculum olfactorium, hypothalamus, substantia nigra and olfactory lobes. However, in the frontal cortex and nucleus accumbens specific binding involves not only dopamine receptors but also 5-HT and/or noradrenaline receptors. Interpretation of in vivo studies in man using radioactive spiperone and its derivatives must take into account the fact that this ligand only labels dopamine receptors in some brain areas.
[3H] - 司哌隆常用于在体外标记脑组织中的多巴胺受体。然而，司哌隆也会与脑内的5 - 羟色胺和去甲肾上腺素受体相互作用。在体内，[3H] - 司哌隆已被用于鉴定动物和人类体内的多巴胺受体，但所鉴定位点的性质尚不清楚。与小脑相比，给大鼠体内注射[3H] - 司哌隆会导致放射性在嗅叶、嗅结节、伏隔核、纹状体、黑质、海马体、额叶皮质和下丘脑选择性蓄积。体内药物置换研究表明，[3H] - 司哌隆在这些区域的结合可能是与多巴胺、5 - 羟色胺或去甲肾上腺素受体。[3H] - 司哌隆在体内主要标记纹状体、嗅结节、下丘脑、黑质和嗅叶中的多巴胺受体。然而，在额叶皮质和伏隔核中，特异性结合不仅涉及多巴胺受体，还涉及5 - 羟色胺和/或去甲肾上腺素受体。使用放射性司哌隆及其衍生物对人体进行体内研究的解释必须考虑到这种配体仅在某些脑区标记多巴胺受体这一事实。
