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

Molecular Cloning and Pharmacological Characterization of a Molluscan Octopamine Receptor

Cindy C. Gerhardt, Remko A. Bakker, Gerard J. Piek, Rudi J. Planta, Erno Vreugdenhil, Josée E. Leysen and Harm Van Heerikhuizen
Molecular Pharmacology February 1997, 51 (2) 293-300; DOI: https://doi.org/10.1124/mol.51.2.293
Cindy C. Gerhardt
1 2 3
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Remko A. Bakker
1 2 3
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Gerard J. Piek
1 2 3
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Rudi J. Planta
1 2 3
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Erno Vreugdenhil
1 2 3
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Josée E. Leysen
1 2 3
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Harm Van Heerikhuizen
1 2 3
  • 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

We describe the cloning and functional expression of a cDNA encoding a novel G protein-coupled receptor, which was isolated from the central nervous system of the pond snail Lymnaea stagnalis. The amino acid sequence predicted by this cDNA shows highest similarity with the sequence of the Locusta tyramine receptor, theDrosophila tyramine/octopamine receptor, and the mammalian α-adrenergic receptors. On expression in mammalian cells, [3H]rauwolscine, an α2-adrenergic receptor antagonist, binds with high affinity (K D = 2.9 × 10−9 m) to the receptor. Of several tested neurotransmitters, octopamine (which is considered to be the invertebrate counterpart of norepinephrine) showed the highest affinity (1.9 × 10−6 m) for the receptor. Therefore, we consider this receptor to be the first true octopamine receptor to be cloned. The ligand binding properties of the novel receptor, designated Lym oa1, seem to be distinct from any of the binding profiles described for octopamine receptors in tissue preparations. Although the pharmacological profile of Lym oa1 shows some similarity with that of Tyr/Oct-Dro and Tyr-Loc, there are also clear differences. In particular, phentolamine, chlorpromazine, and mianserine display markedly higher affinities for Lym oa1 than for the insect receptors. As far as the vertebrate adrenergic receptors are concerned, the ligand binding properties of Lym oa1 resemble α2-adrenergic receptors more than they do α1- or β-adrenergic receptors. Octopaminergic stimulation of Lym oa1 induces an increase in both inositol phosphates and cAMP (EC50 = 9.1 × 10−7 m and 5.1 × 10−6 m, respectively). This is in contrast to the signal transduction pathways described for the related tyramine- and α2-adrenergic receptors, which couple in an inhibitory way to adenylyl cyclase.

Footnotes

    • Received June 19, 1996.
    • Accepted November 7, 1996.
  • Send reprint requests to: Dr. H. van Heerikhuizen, Department of Biochemistry and Molecular Biology, Vrije Universiteit, De Boelelaan 1083, 1081 HV Amsterdam, the Netherlands. E-mail:vheerik{at}chem.vu.nl

  • ↵1 Current affiliation: Department of Medical Pharmacology, Sylvius Laboratories, P.O. Box 9503, 2300 RA Leiden, The Netherlands.

  • 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: 51 (2)
Molecular Pharmacology
Vol. 51, Issue 2
1 Feb 1997
  • 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.
Molecular Cloning and Pharmacological Characterization of a Molluscan Octopamine Receptor
(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

Molecular Cloning and Pharmacological Characterization of a Molluscan Octopamine Receptor

Cindy C. Gerhardt, Remko A. Bakker, Gerard J. Piek, Rudi J. Planta, Erno Vreugdenhil, Josée E. Leysen and Harm Van Heerikhuizen
Molecular Pharmacology February 1, 1997, 51 (2) 293-300; DOI: https://doi.org/10.1124/mol.51.2.293

Citation Manager Formats

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

Share
Research ArticleArticle

Molecular Cloning and Pharmacological Characterization of a Molluscan Octopamine Receptor

Cindy C. Gerhardt, Remko A. Bakker, Gerard J. Piek, Rudi J. Planta, Erno Vreugdenhil, Josée E. Leysen and Harm Van Heerikhuizen
Molecular Pharmacology February 1, 1997, 51 (2) 293-300; DOI: https://doi.org/10.1124/mol.51.2.293
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
    • Abstract
    • Materials and Methods
    • Results
    • Discussion
    • Acknowledgments
    • Footnotes
    • Abbreviations
    • References
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF

Related Articles

Cited By...

More in this TOC Section

  • Upacicalcet binds to the amino acid binding site of CaSR
  • Characterization of GRD and LCCH3 from Human Louse
  • Resveratrol Acts as an NR4A1 Antagonist in Lung Cancer
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 © 2022 by the American Society for Pharmacology and Experimental Therapeutics