The Alpha-1 adrenergic receptors

Cover of: The Alpha-1 adrenergic receptors |

Published by Humana Press in Clifton, N.J .

Written in English

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Subjects:

  • Alpha adrenoceptors,
  • Receptors, Adrenergic, Alpha

Edition Notes

Includes bibliographies and index.

Book details

Other titlesAlpha-one adrenergic receptors.
Statementedited by Robert R. Ruffolo, Jr.
SeriesThe Receptors
ContributionsRuffolo, Robert R.
Classifications
LC ClassificationsQP364.7 .A47 1987
The Physical Object
Paginationxx, 543 p. :
Number of Pages543
ID Numbers
Open LibraryOL2387916M
ISBN 100896031101
LC Control Number87017006

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It is the purpose of this book to present a series of reviews of key experimental findings that shed new light on the alpha-l adrenergic receptor and the manner in which it functions. Classically, most receptors have been characterized based on structure-activity relationships obtained for selective agonists and antagonists interacting with the Cited by: It is the purpose of this book to present a series of reviews of key experimental findings that shed new light on the alpha-l adrenergic receptor and the manner in which it functions.

Classically, most receptors have been characterized based on structure-activity relationships obtained for selective agonists and antagonists interacting with the. Receptor Reserve and Vascular Heterogeneity.- 6. Are There Subtypes of alpha-1 Adrenergic Receptors in Vascular Smooth Muscle?.- Pulmonary Artery of the Rabbit.- Aorta of the Rat.- Are There Differences in alpha-1 Adrenergic Receptors Between Species?.- References.- 10 alpha-1 Adrenergic Receptors in the Central Nervous System.- 1.

Much has been learned about the biochemistry relating to the alpha-1 adrenergic receptor, both at the receptor level and at the subcellular alpha-1 adrenergic receptor-mediated responses involve the translocation of extracellular.

Author: Jr. Ruffolo. Publisher: Springer Science & Business Media ISBN: Category: Medical Page: View: Abstract. As is abundantly clear from the chapters contained in this volume, the combination of the receptor binding technique along with classical pharmacological methods has resulted in significant advances in our understanding of alpha-1 adrenergic receptors during the past 10 : David B.

Bylund, Robert R. Ruffolo. The biochemical and pharmacological characterization of the alpha-1 adrenergic receptor binding site has been dependent upon two advances, one conceptual and the other technical. The conceptual development was the subclassification of alpha-adrenergic receptors into alpha-1 and alpha-2 receptors, as detailed in the first chapter of this book.

Although these receptors influence important cellular responses, it is clear that the physiological response to alpha-1 adrenergic receptor activation is not fixed, but may vary in a range of situations.

For example, prolonged exposure to catecholamines may modify the effects of subsequent alpha-1 adrenergic receptor activation. D.B. Bylund, in Encyclopedia of Biological Chemistry (Second Edition), Adrenergic Receptor Signal Transduction Pathways.

The alpha-1 adrenergic receptors The Alpha-1 adrenergic receptors book the G q/11 family of G proteins leading to the dissociation of the α and βγ subunits and the subsequent stimulation of the enzyme phospholipase C. This enzyme hydrolyzes phosphatidylinositol 1,2-biphosphate in the.

In this respect, the alpha-1 adrenergic receptors differ from myocardial beta-adrenergic receptors. Another difference between alpha-1 and beta-1 adrenergic receptors in cardiac tissue is the slower onset and washout for alphamediated responses (Schumann The Alpha-1 adrenergic receptors book al., ).

Electrophysiologic differences resulting from alpha-1 and beta-1 receptor. Alpha-1 receptors bind catecholamines including, both epinephrine and norepinephrine. In instances in which there is hypoperfusion secondary to The indication for the use of an alpha-receptor modifying medication depends The Alpha-1 adrenergic receptors book which receptor is the target: the alpha-1 receptor or the alpha-2 receptor.

The indication for the use of an alpha-receptor modifying medication depends on which receptor is the target: the alpha-1 receptor or the alpha-2 receptor. Alpha-1 receptors bind catecholamines including, both epinephrine and norepinephrine. In instances in which there is hypoperfusion secondary to decreased cardiac output or decreased systemic vasculature resistance, alpha-1 receptors Cited by: 1.

The Alpha1 Receptor is a G-protein coupled receptor is a generally excitatory receptor connected to the G q G-protein. Briefly, following receptor stimulation, G q leads to activation of Phospholipase C that in turn liberates IP3 and diacylglycerol.

Liberation of IP3 yields release of intracellular calcium, which together with diacylglycerol, leads to activation of Protein Kinase C (PKC).

The alpha-2 Adrenergic Receptors (The Receptors) th Edition, Kindle Edition by Lee E. Limbird (Author) › Visit Amazon's Lee E. Limbird Page. Find all the books, read about the author, and more.

See search results for this author. Are you an author. Learn about Author Central Cited by: Ann M. Graybiel, John B. Penney, in Handbook of Chemical Neuroanatomy, Adrenergic receptors. Norepinephrine receptors are all G-protein coupled and have two pharmacological subtypes, α and β.

α receptors are linked to the inositol phosphate system and to the inhibition of cyclic AMP, whereas β receptors are linked to the stimulation of cyclic AMP. The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like beta blockers, β 2 agonists and α 2 agonists, which are used to treat high blood pressure and asthma, for example.

Mechanism of Beta Receptor Activation in Cardiac Muscle. Agonist binds to the myocardial beta 1-adrenergic receptor is a typical G-protein coupled receptor. In the unstimulated state the G-protein is complexed with GDP (refer to p.

18 of The Receptors handout).; The receptor promotes exchange of GTP for GDP and release of G. "/GTP. This page includes the following topics and synonyms: Alpha Adrenergic Receptor, Alpha 1 Adrenergic Receptor, Alpha 2 Adrenergic Receptor.

Alpha-1 blockers (also called alpha-adrenergic blocking agents) constitute a variety of drugs that block the effect of alphaadrenergic are mainly used to treat benign prostatic hyperplasia (BPH), hypertension and post-traumatic stress disorder.

Alpha-1 adrenergic receptors are present in vascular smooth muscle, the central nervous system, and other tissues.

Beta-1 receptors, along with beta-2, alpha-1, and alpha-2 receptors, are adrenergic receptors primarily responsible for signaling in the sympathetic nervous system. Beta-agonists bind to the beta receptors on various tissues throughout the body. Beta-1 receptors are predominantly found in three locations: the heart, the kidney, and the fat cells.

On the basis of the above findings and of the central distributions of adrenergic neurons and alpha(1)-adrenoceptors, the existence of a central EPI-innervated alpha(1)-adrenergic receptor system is postulated which serves to coexcite or enhance signaling in several monoaminergic brain regions involved in movement and motor activity.

Alpha1-specific adrenergic antagonists are compounds that antagonize with high specificity the alpha1 subtype of adrenergic receptors. In general, these drugs have the suffix "-zosin" with common examples being Terazosin, Prazosin, Doxazosin. Adrenergic alpha-1 Receptor Antagonists Adrenergic alpha-Antagonists / classification* Adrenergic alpha-Antagonists / therapeutic use* Animals Humans Receptors, Adrenergic, alpha-1 / classification* Receptors, Adrenergic, alpha-1 / drug effects*.

Adrenergic alpha-agonists (or alpha-adrenergic agonists) are a class of sympathomimetic agents that selectively stimulates alpha adrenergic alpha-adrenergic receptor has two subclasses α 1 and α 2 receptors are associated with sympatholytic properties.

Alpha-adrenergic agonists have the opposite function of alpha adrenoreceptor ligands mimic the action of. The identification of a nuclear pathway for alpha 1-receptor signaling will be useful for elucidating the intracellular effectors of alpha 1-adrenergic receptors. Full text Get a printable copy (PDF file) of the complete article (M), or click on a page image below to browse page by page.

A quinazoline with antihypertensive and antineoplastic properties. Doxazosin is an alpha-adrenergic antagonist that selectively inhibits alpha-1 adrenergic receptors. Blockages of the alpha-1 adrenergic action on the vascular smooth muscles lead to a decrease in.

Adrenergic receptors can be divided into two primary categories: alpha and beta receptors (see Chapter 18). Each category can then be subdivided, so that five receptor subtypes are commonly identified: alpha-1, alpha-2, beta-1, beta-2, and beta 1 Alpha-1 receptors have been further categorized as alpha-1a, -1b, and -1d receptors, and alpha Renal alpha 1- and alpha 2B-adrenoceptor numbers are frequently increased in genetically hypertensive rats but alpha 1-adrenoceptor-stimulated inositol phosphate formation is unchanged or decreased and alpha 2-adrenoceptor functions remain unclear.

Renal beta-adrenoceptor numbers are elevated in man Adrenergic receptors and their signal. Epinephrine and norepinephrine are equipotent at both alpha 1 and alpha 2 receptors.

Three subtypes of the alpha 1-receptor, the alpha 1A, the alpha 1B, and the alpha 1D, and 3 subtypes of the alpha 2-receptor, the alpha 2A, the alpha 2B, and the alpha 2C have been isolated, cloned and characterized.

However, we will refer to only the alpha 1. [3H]WB and p-[3H]aminoclonidine were used for light microscopic autoradiographic localization of alpha 1 and alpha 2 adrenergic receptors, respectively, in the rat brain.

The binding of these ligands to slide-mounted tissue sections had all of the characteristics associated with alpha 1 and alpha 2 receptors.

Alpha Adrenergic Receptors. There are two types of alpha receptors: alpha-1 and alpha Alpha receptors result in a variety of actions depending on the type as well as location in various organs and tissues.

Smooth muscle contraction is the primary action of alpha-1 receptors. Ildus I. Ahmetov, Olga N. Fedotovskaya, in Advances in Clinical Chemistry, ADRA2A kb, ADRB1 49Gly, ADRB2 16Arg, and ADRB3 64Arg Alleles.

The adrenergic receptors are a prototypic family of guanine nucleotide-binding regulatory protein-coupled receptors that mediate the physiological effects of the hormone epinephrine and the neurotransmitter norepinephrine. Effects. The α 1-adrenergic receptor has several general functions in common with the α 2-adrenergic receptor, but also has specific effects of its own.

α1-receptors primarily mediate smooth muscle contraction, but have important functions elsewhere as well. The neurotransmitter noradrenaline has higher affinity for the α1 receptor than does adrenaline (which is a hormone).

Adrenergic receptors (AR) are G-protein-coupled receptors (GPCRs) that have a crucial role in cardiac physiology in health and disease. Alpha1-ARs signal through G α q, and signaling through Gq, for example, by endothelin and angiotensin receptors, is thought to be detrimental to the heart.

In contrast, cardiac alpha1-ARs mediate important protective and adaptive functions in the. The accompanying multivariate analysis of the binding profiles of antiparkinson agents revealed contrasting patterns of affinities at diverse classes of monoaminergic receptor.

Herein, we characterized efficacies at human (h)D(2SHORT(S)), hD(2LONG(L)), hD(3), and hD() receptors and at halpha(2A). Alpha adrenoreceptor antagonists prevent the stimulation of alpha-adrenergic receptors at the nerve endings of the sympathetic nervous system. There are two types of alpha-adrenergic receptors, alpha 1 (on the vascular smooth muscle) and alpha 2 (on the vascular smooth muscle and.

Dopamine binds to alpha and beta adrenergic receptors. Mediated through myocardial betaadrenergic receptors, dopamine increase heart rate and force, thereby increasing cardiac output. Alphaadrenergic receptor stimulation on vascular smooth muscle, leads to vasoconstriction and results in an increase in systemic vascular resistance.

Receptors, Adrenergic, alpha-1 () Definition (MSH) A subclass of alpha-adrenergic receptors that mediate contraction of SMOOTH MUSCLE in a variety of tissues such as ARTERIOLES; VEINS; and the UTERUS. Early pharmacological experiments demonstrated two basic subclasses of adrenergic receptors: alpha and beta.

Further studies have shown that the majority of the physiological effects of adrenergic receptors are carried out by four basic subtypes: Alpha1 Receptor, Alpha2 Receptor, Beta1 Receptor, and Beta2 Receptor.

These subtypes display tissue-specific expression and generate distinct. Receptor. There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G-proteins and different subtypes show different patterns of activation. They activate mitogenic responses and regulate growth and proliferation of many cells.

"Receptors, Adrenergic, alpha-1" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings).Descriptors are arranged in a hierarchical structure, which enables searching at various levels of specificity.

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