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      Alpha-Adrenoreceptor-Related Dissociation Constants and Intrinsic Efficacies of Stereoisomers of Epinephrine

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          Abstract

          The α-adrenoreceptor-related dissociation constant and intrinsic efficacy of the stereoisomers of epinephrine were determined on the rabbit aortic strip. (–)-Epinephrine showed higher affinity than (+)-epinephrine or the desoxy analogue epinine. Efficacy of (+)-epinephrine relative to (–)-epinephrine was low (relative efficacy, e<sub>r</sub> = 0.44). Epinine had about the same affinity and efficacy as (+)-epinephrine. When the α-adrenoreceptors were protected against dibenamine by an equimolar concentration of the isomers, (–)-epinephrine was found to be more effective than (+)-epinephrine or epinine. These results suggest that the stereoisomers of catecholamines differ not only in affinity but also in intrinsic efficacy.

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          Author and article information

          Journal
          JVR
          J Vasc Res
          10.1159/issn.1018-1172
          Journal of Vascular Research
          S. Karger AG
          1018-1172
          1423-0135
          1981
          1981
          19 September 2008
          : 18
          : 4-5
          : 145-152
          Affiliations
          College of Pharmacy, The Ohio State University, Columbus, Ohio, USA
          Article
          158349 Blood Vessels 1981;18:145–152
          10.1159/000158349
          © 1981 S. Karger AG, Basel

          Copyright: All rights reserved. No part of this publication may be translated into other languages, reproduced or utilized in any form or by any means, electronic or mechanical, including photocopying, recording, microcopying, or by any information storage and retrieval system, without permission in writing from the publisher. 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. Disclaimer: The statements, opinions and data contained in this publication are solely those of the individual authors and contributors and not of the publishers and the editor(s). The appearance of advertisements or/and product references in the publication is not a warranty, endorsement, or approval of the products or services advertised or of their effectiveness, quality or safety. The publisher and the editor(s) disclaim responsibility for any injury to persons or property resulting from any ideas, methods, instructions or products referred to in the content or advertisements.

          Page count
          Pages: 8
          Categories
          Research Paper

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