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肾上腺素能阻滞剂是一种与肾上腺素能受体亲和的物质,当与受体结合即可阻止肾上腺素能神经释放的递质与受体结合产生效应。阻滞剂曾被称为肾上腺素能神经阻滞剂,后者包括干扰递质生物合成、储存及释放的药物,故与阻滞剂并不等同。Langley于1905年提出了有关效应细胞包括兴奋与抑制两种受体物质的概念。1948年Ahlqist观察到拟交感胺在各种效应器官的作用,分为两大类,即α-及β-肾上腺素能受体。1958年Powell及Stater介绍了第一种有效的肾上腺素能β-受体阻滞剂,即双氯异丙肾素(DCI),由于有显著的内源性拟交感活性,故无临床价值。1962年Blach及Stephenson试
Adrenergic blockers are substances that bind to adrenergic receptors that, when combined with a receptor, prevent the transmitter of adrenergic neurons from binding to the receptor. Blockers, once known as adrenergic blockers, include drugs that interfere with the biosynthesis, storage and release of the transmitter and are therefore not equivalent to blockers. Langley in 1905 put forward the concept of effector cells including excitatory and inhibitory receptors. In 1948 Ahlqist observed the role of sympathomimetic in various effector organs, divided into two broad categories, namely, alpha- and beta-adrenergic receptors. In 1958 Powell and Stater introduced the first potent adrenergic beta-blocker, diclofenac (DCI), which has no clinical value due to its significant endogenous sympathomimetic activity. 1962 Blach and Stephenson try