Abstract
The alpha-receptor blockers were the first adrenergic receptor antagonists to be developed for cardiovascular therapy. This occurred shortly after Alquist suggested the alpha/beta classification scheme to explain differences between the pharmacologic actions of adrenergic agonists. The alpha blockers, phenoxybenzamine and phentolamine (now recognized as antagonists for both alpha1 and alpha2 receptors), have been in use since the 1960s, primarily for management of massive catecholamine excess in pheochromocytoma. Subsequently, the quinazolines were found to have antagonism For a set of alpha receptors, primarily found on postsynaptic sites, thus characterized as alpha 1. In the cardiovascular system, alpha1 receptors are found in vascular smooth muscle. These receptors mediate the action of nor-epinephrine released from presynaptic adrenergic nerve terminals, thus causing vasoconstriction, as shown in Figure 1.1. There may be two subtypes of the alpha1 teceptors—alphala and alpha 1b. The former regulates transmembrane calcium entry channels, whereas the latter, through its intracellular action on phospholipase-C and the phosphoinositol system, controls intracellular sequestration of free calcium.
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Frishman, W.H., Cheng-Lai, A., Chen, J. (2000). Alpha-Adrenergic Blockers (Peripherally Acting Antihypertensive Agents). In: Frishman, W.H., Cheng-Lai, A., Chen, J. (eds) Current Cardiovascular Drugs. Current Medicine Group, London. https://doi.org/10.1007/978-1-4615-6767-7_2
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DOI: https://doi.org/10.1007/978-1-4615-6767-7_2
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