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
Research ArticleArticle

High-Affinity Interactions between Human α1A-Adrenoceptor C-Terminal Splice Variants Produce Homo- and Heterodimers but Do Not Generate the α1L-Adrenoceptor

Douglas Ramsay, I. Craig Carr, John Pediani, Juan F. Lopez-Gimenez, Richard Thurlow, Mark Fidock and Graeme Milligan
Molecular Pharmacology August 2004, 66 (2) 228-239; DOI: https://doi.org/10.1124/mol.66.2.228
Douglas Ramsay
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
I. Craig Carr
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
John Pediani
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Juan F. Lopez-Gimenez
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Richard Thurlow
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Mark Fidock
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Graeme Milligan
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
  • Article
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF
Loading

Abstract

Using combinations of bioluminescence resonance energy transfer, time-resolved fluorescence resonance energy transfer and the functional complementation of pairs of inactive receptor-G protein fusion proteins, the human α1A-1-adrenoceptor was shown to form homodimeric/oligomeric complexes when expressed in human embryonic kidney (HEK) 293 cells. Saturation bioluminescence resonance energy transfer studies indicated the α1A-1-adrenoceptor homodimer interactions to be high affinity and some 75 times greater than interactions between the α1A-1-adrenoceptor and the δ opioid peptide receptor. Only a fraction of the α1A-1-adrenoceptors was at the plasma membrane of HEK293 cells at steady state. However, dimers of α1A-1-adrenoceptors were also present in intracellular membranes, and the dimer status of those delivered to the cell surface was unaffected by the presence of agonist. Splice variation can generate at least three forms of the human α1A-1-adrenoceptor with differences limited to the C-terminal tail. Each of the α1A-1, α1A-2a, and α1A-3a-adrenoceptor splice variants formed homodimers/oligomers, and all combinations of these splice variants were able to generate heterodimeric/oligomeric interactions. Despite the coexpression of these splice variants in human tissues that possess the pharmacologically defined α1L-adrenoceptor binding site, coexpression of any pair in HEK293 cells failed to generate ligand binding characteristic of the α1L-adrenoceptor.

  • Received December 11, 2003.
  • Accepted April 21, 2004.
  • The American Society for Pharmacology and Experimental Therapeutics
View Full Text

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: 66 (2)
Molecular Pharmacology
Vol. 66, Issue 2
1 Aug 2004
  • Table of Contents
  • About the Cover
  • Index by author
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.
High-Affinity Interactions between Human α1A-Adrenoceptor C-Terminal Splice Variants Produce Homo- and Heterodimers but Do Not Generate the α1L-Adrenoceptor
(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
Research ArticleArticle

High-Affinity Interactions between Human α1A-Adrenoceptor C-Terminal Splice Variants Produce Homo- and Heterodimers but Do Not Generate the α1L-Adrenoceptor

Douglas Ramsay, I. Craig Carr, John Pediani, Juan F. Lopez-Gimenez, Richard Thurlow, Mark Fidock and Graeme Milligan
Molecular Pharmacology August 1, 2004, 66 (2) 228-239; DOI: https://doi.org/10.1124/mol.66.2.228

Citation Manager Formats

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

Share
Research ArticleArticle

High-Affinity Interactions between Human α1A-Adrenoceptor C-Terminal Splice Variants Produce Homo- and Heterodimers but Do Not Generate the α1L-Adrenoceptor

Douglas Ramsay, I. Craig Carr, John Pediani, Juan F. Lopez-Gimenez, Richard Thurlow, Mark Fidock and Graeme Milligan
Molecular Pharmacology August 1, 2004, 66 (2) 228-239; DOI: https://doi.org/10.1124/mol.66.2.228
Reddit logo Twitter logo Facebook logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One

Jump to section

  • Article
    • Abstract
    • Materials and Methods
    • Results
    • Discussion
    • Footnotes
    • References
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF

Related Articles

Cited By...

More in this TOC Section

  • Analgesic Effects and Mechanisms of Licochalcones
  • Induced Fit Ligand Binding to CYP3A4
  • Englerin A Inhibits T-Type Channels
Show more Article

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