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      An α-Adrenoceptor-Blocking Action of SGB-483, a New Piperazine Antihypertensive Agent in Isolated Vascular Smooth Muscles

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          Abstract

          SGB (10<sup>-7</sup>–10<sup>–5</sup> M), a new piperazinyl antihypertensive agent, like prazosin (10<sup>–8_</sup>10<sup>–6</sup> M), a potent preferential α<sub>1</sub>-adrenoceptor antagonist, inhibited the contractile response of rabbit aorta to norepinephrine and methoxamine in a competitive manner whereas in the cat coronary and rabbit basilar artery, the inhibition by SGB was not a competitive one. The potency of the inhibitory action of SGB was less than that of prazosin in all preparations used. Neither SGB nor prazosin had any inhibitory effect on the response to potassium, 5-hydroxytryptamine, prostaglandin F<sub>2α</sub>, and excess Ca<sup>2+</sup> in all preparations. In the rabbit aortic membrane preparation, the specific binding of [<sup>3</sup>H]-prazosin was inhibited, concentration-dependently, by SGB with IC<sub>50</sub> value of 1.4 ± 0.09 µ M. These studies indicated that SGB has an α<sub>1-</sub>adrenoceptor-blocking action though its potency is weaker than prazosin.

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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
          1984
          1984
          23 September 2008
          : 21
          : 6
          : 298-305
          Affiliations
          Department of Pharmacology, School of Medicine, University of Hawaii, Honolulu, Hawaii, USA
          Article
          158532 Blood Vessels 1984;21:298–305
          10.1159/000158532
          © 1984 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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