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

Structure-activity profile of calcitonin gene-related peptide in peripheral and brain tissues. Evidence for receptor multiplicity.

T Dennis, A Fournier, S St Pierre and R Quirion
Journal of Pharmacology and Experimental Therapeutics November 1989, 251 (2) 718-725;
T Dennis
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
A Fournier
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
S St Pierre
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
R Quirion
  • 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

The radioligand binding characteristics and in vitro biological activities of human calcitonin gene-related peptide (hCGRP) homologs, analogs and fragments have been tested in a variety of preparations in order to determine the structural requirements of the calcitonin gene-related peptide (CGRP) receptor. The ligand selectivity profile observed in this study suggests that [125I] hCGRP binding sites present in rat brain and spleen are similar. The high affinity of the analogs [Cys(ACM)2.7]hCGRP and cyclo2.7 [Asp2, Lys7]hCGRP indicates that the disulfide bridge between positions 2 and 7 is not essential for the binding of the ligand to the CGRP receptor. On the other hand, the lack of affinity of various N-terminal fragments in the binding assays demonstrates the importance of amino acids 9-37 in maintaining appropriate receptor recognition. The existence of CGRP receptor subtypes is supported by data obtained in various in vitro bioassays. For example, the linear analog, [Cys(ACM)2.7]hCGRP, which retained high potency in the rat vas deferens bioassay displayed no agonistic activity in the right and left guinea pig atrial preparations. Additionally, the C-terminal fragment hCGRP 12-37 possessed some antagonist properties in atrial but not vas deferens preparations. Thus, it appears that it is possible to differentiate between CGRP receptor subtypes on the basis of differential agonistic (e.g.[Cys(ACM)2.7]hCGRP) and antagonistic (e.g., hCGRP 12-37) potencies in various isolated tissues. Moreover, the weak but significant antagonistic properties of hCGRP 12-37 may be most useful in order to design more potent CGRP receptor antagonists.

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. 251, Issue 2
1 Nov 1989
  • Table of Contents
  • 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.
Structure-activity profile of calcitonin gene-related peptide in peripheral and brain tissues. Evidence for receptor multiplicity.
(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

Structure-activity profile of calcitonin gene-related peptide in peripheral and brain tissues. Evidence for receptor multiplicity.

T Dennis, A Fournier, S St Pierre and R Quirion
Journal of Pharmacology and Experimental Therapeutics November 1, 1989, 251 (2) 718-725;

Citation Manager Formats

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

Share
Abstract

Structure-activity profile of calcitonin gene-related peptide in peripheral and brain tissues. Evidence for receptor multiplicity.

T Dennis, A Fournier, S St Pierre and R Quirion
Journal of Pharmacology and Experimental Therapeutics November 1, 1989, 251 (2) 718-725;
Reddit logo Twitter logo Facebook 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