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Table of Contents
Vol. 33, Suppl. 2, 1998
Issue release date: March 1998
Section title: Paper
Eur Urol 1998;33(suppl 2):2–6
(DOI:10.1159/000052227)

Nomenclature and State of the Art on α1-Adrenoceptors

Langer S.Z.
Synthélabo Recherche (LERS), Bagneux, France

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Article / Publication Details

First-Page Preview
Abstract of Paper

Published online: March 11, 1998
Issue release date: March 1998

Number of Print Pages: 5
Number of Figures: 2
Number of Tables: 6

ISSN: 0302-2838 (Print)
eISSN: 1421-993X (Online)

For additional information: http://www.karger.com/EUR

Abstract

The concept of α1-adrenoceptor subtypes was first suggested in the mid 1980s on the basis of the different affinities of certain α1-adrenoceptor preparations for the α-adrenoceptor agonist, oxymetazoline, and the antagonists, WB4101 and phentolamine. Subsequent characterization of α1-adrenoceptors using radioligand binding and functional studies has led to the identification of three native prazosin high-affinity α1-adrenoceptor subtypes designated α1A, α1B and α1D, corresponding to the three α1-adrenoceptor subtypes (α1a, α1b and α1d) isolated by molecular cloning techniques. Since each of these three subtypes exhibits similar affinity for the selective α1-adrenoceptor antagonist, prazosin, [3H]prazosin can be used as a convenient probe to evaluate the interaction of compounds with these adrenoceptor subtypes. Considerable clinical experience over the last few years has provided convincing evidence to support the effectiveness of α1-adrenoceptor blockade in the treatment of bladder obstruction due to benign prostatic hyperplasia (BPH). The distribution of α1-adrenoceptors in the human prostate tissue has shown that the predominant cloned α1-adrenoceptor subtype characterized by RNAase protection assays corresponds to the α1a-subtype, formerly classified as α1c. Many of the α1-antagonists currently prescribed in the treatment of BPH do not exhibit in vitro selectivity between α1a-, α1b- and α1d-subtypes and yet they have good clinical tolerance in terms of low incidence of cardiovascular effects. One possibility to account for these findings is that another α1-adrenoceptor subtype could be implicated in human prostatic smooth muscle contraction. A recent report, although confirming the presence of an α1a-subtype in human prostate, suggested that an α1-adrenoceptor subtype with lower affinity for prazosin, designated α1L, which has not been cloned yet, is in fact the predominant α1-subtype involved in the contractile response of human prostatic smooth muscle to noradrenaline.


Article / Publication Details

First-Page Preview
Abstract of Paper

Published online: March 11, 1998
Issue release date: March 1998

Number of Print Pages: 5
Number of Figures: 2
Number of Tables: 6

ISSN: 0302-2838 (Print)
eISSN: 1421-993X (Online)

For additional information: http://www.karger.com/EUR


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Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in government regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug.
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