Aradrenergic receptor

Stromal tissue is the primary locus of aradrenergic receptors in the prostate. It is estimated that 98% of the a-adrenergic receptors in the prostate are found in prostatic stromal tissue. Of the arreceptors found in the prostate, 70% of them are of the a1A-sub-type.5 This explains why a-adrenergic antagonists are effective for managing symptoms of BPH.6... 

Hypertension, or a chronic elevation in blood pressure, is a major risk factor for coronary artery disease congestive heart failure stroke kidney failure and retinopathy. An important cause of hypertension is excessive vascular smooth muscle tone or vasoconstriction. Prazosin, an aradrenergic receptor antagonist, is very effective in management of hypertension. Because oq-receptor stimulation causes vasoconstriction, drugs that block these receptors result in vasodilation and a decrease in blood pressure. 

Prazosin is a selective aradrenergic receptor antagonist that, at therapeutic doses, has little activity at a2-adrenergic receptors and clinically insignificant direct vasodilating activity The drug does not cause the other effects attributed to phentolamine. Most important, it produces less tachycardia than does phentolamine and, therefore, is useful in the treatment of essential hypertension. 

TABLE 12-4 Properties of human aradrenergic receptor subtypes... 

Computational Modeling of Selective Pharmacophores at the arAdrenergic Receptors... 

Data for aradrenergic receptor binding. Data for p-opiate receptor binding. 

The a-blockers act as antagonists for the aradrenergic receptor. The a -adrenergic receptor, when stimulated, triggers vasoconstriction. Blocking this receptor prevents vasoconstriction and reduces blood pressure. Doxazosin (Cardura, A.131) is structurally... 

Kiss A, Aguilera G (1992) Participation of aradrenergic receptors in the secretion of hypothalamic corticotropin-releasing hormone during stress. Neuroendocrinol 56 153-160. 

Zhao MM, Hwa J, Perez DM. Identification of critical extracellular loop residues involved in aradrenergic receptor subtype-selective antagonist binding. Mol Pharmacol 1996 50 1118-1126. 

Kanterman RY, Felder CC, Brenneman DE, Ma AL, Fitzgerald S, Axelrod J. arAdrenergic receptor mediates arachidonic-acid release in spinal-cord neurons independent of inositol phospholipid turnover. J Neurochem 1990 54 1225-1232. 

Vicentic A, Robeva A, Rogge G, Uberti M, Minneman KP. Biochemistry and pharmacology of epitope-tagged aradrenergic receptor subtypes. J Pharmacol Exp Ther 2002 302 58-65. 

The presence of aradrenergic receptor subtypes has been mapped in the human vasculature at the mRNA level (29), but few vessels have been studied functionally. In resistance vessels, a1A-adrenergic receptors appear to dominate... 

Prior to their use in BPH patients, aradrenergic receptor antagonists were used in the treatment of arterial hypertension. Therefore, a,-antagonists originally developed for the treatment of hypertension, such as doxazosin and terazosin, lower blood pressure when used to treat BPH patients as a result, such... 

Akhter SA, Milano CA, Shotwell KF, et al. Transgenic mice with cardiac overexpression of a1B-adrenergic receptors. In vivo aradrenergic receptor-mediated regulation of [J-adrenergic signaling. J Biol Chem 1997 272 21,253-21,259. 

Minneman KP, Lee D, Zhong H, Berts A, Abbott KL, Murphy TJ. Transcriptional responses to growth factor and G protein-coupled receptors in PC 12 cells comparison of aradrenergic receptor subtypes. J Neurochem 2000 74 2392-2400. 

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