Shimohama S, Taniguchi T, Fujiwara M, Kameyama M
J Neurochem. 1987 Apr;48(4):1215-21. doi: 10.1111/j.1471-4159.1987.tb05649.x.
Using ligand binding techniques, we studied beta-adrenergic receptor subtypes in brains obtained at autopsy from seven histologically normal controls and seven histopathologically verified cases with Alzheimer-type dementia (ATD). Inhibition of [3H]dihydroalprenolol [( 3H]DHA) binding by the selective beta 1 antagonist, metoprolol, results in nonlinear Hofstee plots, suggesting the presence of the two receptor subtypes in the human brain. The calculated ratios of beta 1/beta 2-adrenergic receptors in control brains are as follows: frontal cortex, 49:51; temporal cortex, 31:69; hippocampus, 66:34; thalamus, 23:77; putamen, 70:30; caudate, 48:52; nucleus basalis of Meynert (NbM), 43:57; cerebellar hemisphere, 25:75. Compared with the controls, total concentrations of beta-adrenergic receptors were significantly reduced only in the thalamus of the ATD brains. beta 1-Adrenergic receptor concentrations were significantly reduced in the hippocampus and increased in the NbM and cerebellar hemisphere, whereas beta 2-adrenergic receptor concentrations were significantly reduced in the thalamus, NbM, and cerebellar hemisphere and increased in the hippocampus and putamen of the ATD brains. These results suggest that beta 1- and beta 2-adrenergic receptors are present in the human brain and that there are significant changes in both receptor subtypes in selected brain regions in patients with ATD.
我们运用配体结合技术，对取自7例组织学正常对照者及7例经组织病理学证实的阿尔茨海默型痴呆（ATD）患者尸检大脑中的β-肾上腺素能受体亚型进行了研究。选择性β1拮抗剂美托洛尔对[3H]二氢心得舒（[3H]DHA）结合的抑制作用导致Hofstee图呈非线性，提示人脑中存在两种受体亚型。对照大脑中计算出的β1/β2-肾上腺素能受体比率如下：额叶皮质，49:51；颞叶皮质，31:69；海马，66:34；丘脑，23:77；壳核，70:30；尾状核，48:52；迈内特基底核（NbM），43:57；小脑半球，25:75。与对照者相比，仅ATD大脑的丘脑中β-肾上腺素能受体的总浓度显著降低。β1-肾上腺素能受体浓度在海马中显著降低，在NbM和小脑半球中升高，而β2-肾上腺素能受体浓度在ATD大脑的丘脑、NbM和小脑半球中显著降低，在海马和壳核中升高。这些结果表明，β1-和β2-肾上腺素能受体存在于人脑中，且ATD患者某些脑区的两种受体亚型均有显著变化。
