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α-和β-肾上腺素能药物的现状 一、肾上腺素能受体

Present state of alpha- and beta-adrenergic drugs I. The adrenergic receptor.

作者信息

Ahlquist R P

出版信息

Am Heart J. 1976 Nov;92(5):661-4. doi: 10.1016/s0002-8703(76)80086-5.

Abstract

The cardiovascular alpha adrenergic receptors evoke vasoconstriction, the cardiovascular beta receptors evoke vasodilation and cardiac stimulation. All blood vessels have both alpha and beta receptors. In some areas, for example skin and kidney, the alpha receptors predominate. In some vascular beds, for example the nutrient vessels in skeletal muscle, beta receptors predominate. In other beds, such as coronary, visceral, and connective tissue both receptors are active. The cardiovascular effects of adrenergic agonists depend on which receptor they act on. Phenylephrine is specific for alpha receptors. Isoproterenol is specific for beta receptors. Epinephrine and norepinephrine act on both. The real value of knowing the receptor specificity of each agonist is that side effects can more easily be predicted. For example, adrenergic cardiac stimulants are antiasthmatics. Therefore, adrenergic antiasthmatics can produce excessive cardiac stimulation. For the future, agonists that are not only receptor-specific but also tissue-specific will be developed. The first of these in the United States is terbutaline. The rest of the world has in addition a similar drug, salbutamol. No one knows if this drug will be approved for use by American physicians.

摘要

心血管系统的α肾上腺素能受体可引起血管收缩,β肾上腺素能受体可引起血管舒张和心脏兴奋。所有血管都同时存在α和β受体。在某些区域,如皮肤和肾脏,α受体占主导。在一些血管床,如骨骼肌中的营养血管,β受体占主导。在其他血管床,如冠状动脉、内脏血管和结缔组织,两种受体都有活性。肾上腺素能激动剂对心血管系统的作用取决于它们作用于哪种受体。去氧肾上腺素对α受体具有特异性。异丙肾上腺素对β受体具有特异性。肾上腺素和去甲肾上腺素对两者都有作用。了解每种激动剂的受体特异性的实际价值在于更容易预测副作用。例如,肾上腺素能心脏兴奋剂是抗哮喘药。因此,肾上腺素能抗哮喘药可能会产生过度的心脏兴奋。未来,将会研发出不仅具有受体特异性而且具有组织特异性的激动剂。在美国,第一种这样的药物是特布他林。世界其他地区还有一种类似的药物,沙丁胺醇。没有人知道这种药物是否会被美国医生批准使用。

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