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采用放射配体结合方法观察外源性氧自由基对大鼠心肌α_1肾上腺素受体(α_1受体)及其亚型α_(1A)与α_(1B)的影响和对β肾上腺素受体(β受体)的影响。发现:(1)·OH,使α_1受体与~(125)IBE2254最大结合量(B_(max))分别下降55%与36%。(2)·OH可使α_1受体与~(125)IBE2254结合的K_d值增高171%,而对K_d值无影响。(3)·OH,均使α_1受体亚型α_(1A)与α_(1B)之间的比例增加。(4)·OH,对β受体与~(125)IPIN最大结合量B_(max)和K_d值均无影响。(5)氧自由基清除剂甘露醇或超氧化物歧化酶均可对抗氧自由基引起α_1受体及其亚型的改变。上述结果提示,氧自由基可直接作用于心肌膜,引起α_1受体数量和亲和性下降,α_1受体亚型α_(1A)与α_(1B)之间的比例改变。
Radioligand binding assay was used to observe the effects of exogenous oxygen free radicals on α 1 adrenoceptor (α 1 receptor) and its subtypes α 1 (1A) and α 1 (1B) in rat myocardium and the effects of adrenergic receptor beta receptors). The results showed that: (1) · OH, the maximum binding capacity of α_1 receptor to 125EBE2254 decreased by 55% and 36% respectively. (2) · OH increased the K_d value of α_1 receptor binding to 125EBE2254 by 171%, but had no effect on K_d. (3) · OH, both increased the ratio of α_1 receptor subtype α 1A and α 1B. (4) · OH, had no effect on the maximum binding amount of β-adrenoceptor with ~ (125) IPIN B_ (max) and K_d. (5) Oxygen free radical scavengers mannitol or superoxide dismutase against oxygen free radicals caused by α_1 receptor and its subtypes. These results suggest that oxygen free radicals can act directly on the myocardial membrane, causing a decline in the number and affinity of α 1 receptors, α 1 receptor subtypes α 1A and α 1B ratio changes.