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
Journal of Pharmacology and Experimental Therapeutics
  • 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
Journal of Pharmacology and Experimental Therapeutics

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 jpet on Facebook
  • Follow jpet on Twitter
  • Follow jpet on LinkedIn
Abstract

Species differences in chlorethylclonidine antagonism at vascular alpha-1 adrenergic receptors.

W N Tian, S Gupta and R C Deth
Journal of Pharmacology and Experimental Therapeutics May 1990, 253 (2) 877-883;
W N Tian
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
S Gupta
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
R C Deth
  • 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

Chloroethylclonidine (CEC) inhibition of norepinephrine-induced contractile response was studied in rat and rabbit aorta. CEC inhibition was irreversible, but displayed a competitive pattern characterized by rightward shifts of the norepinephrine EC50 with little or no decrease in maximum response. CEC appeared to shift response to a discrete but lower affinity state. The time course for irreversible inhibition by 10 microM CEC was faster for rat aorta (T1/2 = 18 min) than for rabbit aorta (T1/2 = 118 min) indicating a difference either in receptor occupation or in the rate of alkylation after occupation. Measurements of reversible CEC affinity in rabbit aorta yielded a pKB of 6.3 and the rate of alkylation was not significantly increased at 100 microM CEC so that lower occupation could not account for the difference. Pretreatment with phenoxybenzamine significantly increased the sensitivity of rabbit aorta to CEC indicating a role for receptor reserve in determining the extent of CEC inhibition. Membrane fluidity measured by diphenylhexatriene fluorescence was lower in rabbit than rat aorta; however, dimethylsulfoxide or ethanol failed to alter the rate of irreversible CEC inhibition in the rabbit. Protein kinase C activation with phorbol dibutyrate failed to alter CEC alkylation in rabbit aorta. WB 4101 [2-(2,6-dimethoxyphenoxyethyl)-aminomethyl-1,4-benzodioxane] affinity was higher in rabbit aorta (pKB = 8.9) than rat aorta (pKB = 8.3) consistent with a contribution of alpha-1A and alpha-1B adrenergic receptor subtypes to differences in CEC sensitivity, although the difference was not as great as would be predicted.(ABSTRACT TRUNCATED AT 250 WORDS)

JPET 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

Journal of Pharmacology and Experimental Therapeutics
Vol. 253, Issue 2
1 May 1990
  • Table of Contents
  • Table of Contents (PDF)
  • Index by author
  • 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 Journal of Pharmacology and Experimental Therapeutics 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.
Species differences in chlorethylclonidine antagonism at vascular alpha-1 adrenergic receptors.
(Your Name) has forwarded a page to you from Journal of Pharmacology and Experimental Therapeutics
(Your Name) thought you would be interested in this article in Journal of Pharmacology and Experimental Therapeutics.
CAPTCHA
This question is for testing whether or not you are a human visitor and to prevent automated spam submissions.
Citation Tools
Abstract

Species differences in chlorethylclonidine antagonism at vascular alpha-1 adrenergic receptors.

W N Tian, S Gupta and R C Deth
Journal of Pharmacology and Experimental Therapeutics May 1, 1990, 253 (2) 877-883;

Citation Manager Formats

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

Share
Abstract

Species differences in chlorethylclonidine antagonism at vascular alpha-1 adrenergic receptors.

W N Tian, S Gupta and R C Deth
Journal of Pharmacology and Experimental Therapeutics May 1, 1990, 253 (2) 877-883;
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 JPET
  • 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
  • Molecular Pharmacology
  • Pharmacological Reviews
  • Pharmacology Research & Perspectives
ISSN 1521-0103 (Online)

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