Skip to main content
Advertisement

Main menu

  • Home
  • Articles
    • Current Issue
    • Fast Forward
    • Latest Articles
    • Special Sections
    • Archive
  • Information
    • Instructions to Authors
    • Submit a Manuscript
    • FAQs
    • For Subscribers
    • Terms & Conditions of Use
    • Permissions
  • Editorial Board
  • Alerts
    • Alerts
    • RSS Feeds
  • Virtual Issues
  • Feedback
  • Submit
  • Other Publications
    • Drug Metabolism and Disposition
    • Journal of Pharmacology and Experimental Therapeutics
    • Molecular Pharmacology
    • Pharmacological Reviews
    • Pharmacology Research & Perspectives
    • ASPET

User menu

  • My alerts
  • Log in
  • My Cart

Search

  • Advanced search
Molecular Pharmacology
  • Other Publications
    • Drug Metabolism and Disposition
    • Journal of Pharmacology and Experimental Therapeutics
    • Molecular Pharmacology
    • Pharmacological Reviews
    • Pharmacology Research & Perspectives
    • ASPET
  • My alerts
  • Log in
  • My Cart
Molecular Pharmacology

Advanced Search

  • Home
  • Articles
    • Current Issue
    • Fast Forward
    • Latest Articles
    • Special Sections
    • Archive
  • Information
    • Instructions to Authors
    • Submit a Manuscript
    • FAQs
    • For Subscribers
    • Terms & Conditions of Use
    • Permissions
  • Editorial Board
  • Alerts
    • Alerts
    • RSS Feeds
  • Virtual Issues
  • Feedback
  • Submit
  • Visit molpharm on Facebook
  • Follow molpharm on Twitter
  • Follow molpharm on LinkedIn
Abstract

Reevaluation of the regulation of beta-adrenergic receptor binding by desipramine treatment.

M A Riva and I Creese
Molecular Pharmacology July 1989, 36 (1) 211-218;
M A Riva
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
I Creese
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
  • Article
  • Info & Metrics
  • eLetters
  • PDF
Loading

Abstract

Treatment of rats with desipramine (DMI) has been shown to down-regulate beta-adrenergic receptor-stimulated adenylate cyclase and reduce the Bmax of beta-adrenergic receptors in some brain areas. Recent reports have indicated that the down-regulation in the number of beta-adrenergic receptors following DMI treatment does not occur if the serotonin system has been impaired following parachlorophenylalanine (PCPA) or 5,7-dihydroxytryptamine injection. We have previously shown that [3H]dihydroalprenolol ([3H]DHA), the most commonly used radioligand to measure central nervous system beta-adrenergic receptors, labels another site under normal experimental procedures, in addition to the beta-adrenergic receptors. This second site has some pharmacological characteristics of the 5-hydroxytryptamine1A receptor. The depletion of serotonin following PCPA injection was indeed able to prevent the down-regulation of [3H]DHA binding sites after DMI injection. However, PCPA alone increased the density of [3H]DHA binding sites. If the nonlinear, least squares, curve-fitting program LIGAND was allowed to define [3H]DHA nonspecific binding or if the more selective beta-adrenergic receptor radioligand [3H]CGP-1277 was used, the Bmax of beta-adrenergic receptors was not changed after PCPA injection. Importantly, PCPA did not prevent beta-adrenergic receptor down-regulation following DMI treatment. The blockade of 5-hydroxytryptamine2 receptors, via ketanserin administration, during DMI treatment did not change the response of beta-adrenergic receptors. Furthermore, if LIGAND was used to define the nonspecific binding of [3H]DHA, the down-regulation of beta-adrenergic receptors was significant 24 hr after a single DMI injection. The same rapid down-regulation was demonstrated with [3H]CGP-12177. However, if [3H]DHA was used to label beta-adrenergic receptors in the "typical" manner (nonspecific binding defined by 10 microM alprenolol), a decrease in the number of beta-adrenergic receptors was significant only after seven daily DMI injections. These data demonstrate that the use of [3H]DHA to measure beta-adrenergic receptors can be misleading, because changes in its second binding site can conceal the changes occurring in beta-adrenergic receptors. Moreover, these results suggest that a similarity in the time course of action of DMI cannot be used to support the hypothesis that its therapeutic antidepressant action is related to beta-adrenergic receptor down-regulation.

MolPharm articles become freely available 12 months after publication, and remain freely available for 5 years. 

Non-open access articles that fall outside this five year window are available only to institutional subscribers and current ASPET members, or through the article purchase feature at the bottom of the page. 

 

  • Click here for information on institutional subscriptions.
  • Click here for information on individual ASPET membership.

 

Log in using your username and password

Forgot your user name or password?

Purchase access

You may purchase access to this article. This will require you to create an account if you don't already have one.
PreviousNext
Back to top

In this issue

Molecular Pharmacology
Vol. 36, Issue 1
1 Jul 1989
  • Table of Contents
  • Table of Contents (PDF)
  • Index by author
  • Back Matter (PDF)
  • Editorial Board (PDF)
  • Front Matter (PDF)
Download PDF
Article Alerts
Sign In to Email Alerts with your Email Address
Email Article

Thank you for sharing this Molecular Pharmacology article.

NOTE: We request your email address only to inform the recipient that it was you who recommended this article, and that it is not junk mail. We do not retain these email addresses.

Enter multiple addresses on separate lines or separate them with commas.
Reevaluation of the regulation of beta-adrenergic receptor binding by desipramine treatment.
(Your Name) has forwarded a page to you from Molecular Pharmacology
(Your Name) thought you would be interested in this article in Molecular Pharmacology.
CAPTCHA
This question is for testing whether or not you are a human visitor and to prevent automated spam submissions.
Citation Tools
Abstract

Reevaluation of the regulation of beta-adrenergic receptor binding by desipramine treatment.

M A Riva and I Creese
Molecular Pharmacology July 1, 1989, 36 (1) 211-218;

Citation Manager Formats

  • BibTeX
  • Bookends
  • EasyBib
  • EndNote (tagged)
  • EndNote 8 (xml)
  • Medlars
  • Mendeley
  • Papers
  • RefWorks Tagged
  • Ref Manager
  • RIS
  • Zotero

Share
Abstract

Reevaluation of the regulation of beta-adrenergic receptor binding by desipramine treatment.

M A Riva and I Creese
Molecular Pharmacology July 1, 1989, 36 (1) 211-218;
del.icio.us logo Digg logo Reddit logo Twitter logo Facebook logo Google logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One

Jump to section

  • Article
  • Info & Metrics
  • eLetters
  • PDF

Related Articles

Cited By...

Similar Articles

Advertisement
  • Home
  • Alerts
Facebook   Twitter   LinkedIn   RSS

Navigate

  • Current Issue
  • Fast Forward by date
  • Fast Forward by section
  • Latest Articles
  • Archive
  • Search for Articles
  • Feedback
  • ASPET

More Information

  • About Molecular Pharmacology
  • Editorial Board
  • Instructions to Authors
  • Submit a Manuscript
  • Customized Alerts
  • RSS Feeds
  • Subscriptions
  • Permissions
  • Terms & Conditions of Use

ASPET's Other Journals

  • Drug Metabolism and Disposition
  • Journal of Pharmacology and Experimental Therapeutics
  • Pharmacological Reviews
  • Pharmacology Research & Perspectives
ISSN 1521-0111 (Online)

Copyright © 2023 by the American Society for Pharmacology and Experimental Therapeutics