In vitro determination of the ability of drugs to bind to adrenergic receptors.
In vitro determination of the ability of drugs to bind to adrenergic receptors.
复制标题
体外测定药物与肾上腺素能受体结合的能力。
DOI：
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发表时间：
1977
影响因子：
4.4
通讯作者：
Page
中科院分区：
文献类型：
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作者：
A. Neufeld;Ellen;Page
用兔虹膜睫状体匀浆制备膜，分别测定~(3)H-二氢麦角隐亭和~(3+)-二氢阿普洛尔与膜的结合，研究α和β-肾上腺素能受体。~3H-二氢麦角隐亭的结合似乎是α-肾上腺素能受体所特有的，因为肾上腺素能药物以下列效力顺序取代该放射性配基：酚妥拉明大于肾上腺素大于或等于去甲肾上腺素大于或等于异丙肾上腺素=心得安。~3H-二氢阿普洛尔的结合似乎是β-肾上腺素能受体所特有的，因为肾上腺素能药物以下列效力顺序取代该放射性配基：心得安大于或等于异丙肾上腺素大于或等于肾上腺素大于或等于去甲肾上腺素大于或等于酚妥拉明。可乐定和多巴胺与α-肾上腺素能受体结合，但对β-肾上腺素能受体几乎没有活性。噻吗洛尔、D-异丙肾上腺素和异丙肾上腺素与β-肾上腺素能受体结合，但对α-肾上腺素能受体几乎没有活性。结果表明，α-和β-肾上腺素能受体的体外结合试验有助于研究药物的作用机制。
Alpha- and beta-adrenergic receptors were studied by measuring the binding of 3H-dihydroergocryptine and 3H-dihydroalprenolol, respectively, to membranes prepared from homogenized rabbit iris--ciliary bodies. The binding of 3H-dihydroergocryptine appears to be specific for alpha-adrenergic receptors, since adrenergic agents displace this radioligand with the following order of potency: phentolamine greater than epinephrine greater than or equal to norepinephrine greater than or equal to isoproterenol = propranolol. The binding of 3H-dihydroalprenolol appears to be specific for beta-adrenergic receptors, since adrenergic agents displace this radioligand with the following order of potency: propranolol greater than or equal to isoproterenol greater than or equal to epinephrine greater than norepinephrine greater than or equal to phentolamine. Clonidine and dopamine bind to the alpha-adrenergic receptor but have little activity at the beta-adrenergic receptor. Timolol, d-isoproterenol, and dipivalyl epinephrine bind to the beta-adrenergic receptor but have little activity at the alpha-adrenergic receptor. The results demonstrate that in vitro binding assays for alpha- and beta-adrenergic receptors are useful for studying the mechanism of drug action.