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
Research ArticleNEUROPHARMACOLOGY

Central Mechanisms Regulating Penile Erection in Conscious Rats: The Dopaminergic Systems Related to the Proerectile Effect of Apomorphine

Gin C. Hsieh, Peter R. Hollingsworth, Brenda Martino, Renjie Chang, Marc A. Terranova, Alyssa B. O'Neill, James J. Lynch, Robert B. Moreland, Diana L. Donnelly-Roberts, Teodozyi Kolasa, Joseph P. Mikusa, Jill M. McVey, Kennan C. Marsh, James P. Sullivan and Jorge D. Brioni
Journal of Pharmacology and Experimental Therapeutics January 2004, 308 (1) 330-338; DOI: https://doi.org/10.1124/jpet.103.057455
Gin C. Hsieh
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Peter R. Hollingsworth
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Brenda Martino
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Renjie Chang
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Marc A. Terranova
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Alyssa B. O'Neill
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
James J. Lynch
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Robert B. Moreland
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Diana L. Donnelly-Roberts
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Teodozyi Kolasa
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Joseph P. Mikusa
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Jill M. McVey
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Kennan C. Marsh
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
James P. Sullivan
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Jorge D. Brioni
  • 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

Apomorphine has been used as a pharmacological probe of dopaminergic receptors in a variety of central nervous system disorders. The utility of apomorphine as an agent for the treatment of erectile dysfunction has also been demonstrated clinically. Apomorphine is a nonselective dopaminergic receptor agonist with potent binding affinity (Ki) of 101, 32, 26, 2.6, and 10 nM for D1, D2, D3, D4, and D5, respectively. When administered either subcutaneously (s.c.) or intracerebroventricularly (i.c.v.), apomorphine fully evoked penile erections in conscious rats with maximum effect at 0.1 μmol/kg s.c. and 3 nmol/rat i.c.v., respectively. Apomorphine was less efficacious when injected intrathecally (i.t.) to L4-L6 spinal levels (50% at 30–100 nmol/rat i.t.). Penile erection facilitated by apomorphine was blocked by haloperidol and clozapine (i.p. and i.c.v.) but not by domperidone (a peripherally acting dopaminergic receptor antagonist). In this model using conscious rats, penile erection was significantly induced by quinpirole (D2-D3-D4 receptor agonist), but not by R(+)-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol (SKF38393) and R(+)-6-chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzapine (SKF81297) (D1 receptor agonists), or a D2 receptor agonist R-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine (PNU-95666E). The role of D4 receptors in penile erection was demonstrated using selective D4 receptor agonists [(4-phenylpiperazinyl)-methyl]benzamide (PD168077) and 5-fluoro-2-{[4-(2-pyridinyl)-1-piperazinyl]methyl}-1H-indole (CP226269), whether administered systemically (s.c.) or locally in the brain (i.c.v.). The ability of apomorphine to activate D3 receptors in relation to its proerectile activity remains to be elucidated by use of selective subtype agonists. These results suggest that the proerectile action of apomorphine in rats is mediated at supraspinal levels and that this effect is not mimicked by a D2 receptor agonist but associated with activation of D4 receptors.

Footnotes

  • This work was funded by Abbott Laboratories.

  • DOI: 10.1124/jpet.103.057455.

  • ABBREVIATIONS: ED, erectile dysfunction; CNS, central nervous system; MPOA, medial preoptic area; PVN, paraventricular nucleus; PE, polyethylene; CHO, Chinese hamster ovary; GTPγS, guanosine 5′-O-(3-thio)triphosphate; 5HT, 5-hydroxytryptamine; SKF38393, R(+)-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol; SKF81297, R(+)-6-chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzapine; PNU-95666E, R-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine; PD168077, (4-phenylpiperazinyl)-methyl]benzamide; CP226269, 5-fluoro-2-{[4-(2-pyridinyl)-1-piperazinyl]methyl}-1H-indole; BP897, 1-4-2-naphthoylaminobutyl-4-2-methoxyphenyl-1A-piperazine.

    • Received July 21, 2003.
    • Accepted September 17, 2003.
  • The American Society for Pharmacology and Experimental Therapeutics
View Full Text

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: 308 (1)
Journal of Pharmacology and Experimental Therapeutics
Vol. 308, Issue 1
1 Jan 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 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.
Central Mechanisms Regulating Penile Erection in Conscious Rats: The Dopaminergic Systems Related to the Proerectile Effect of Apomorphine
(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
Research ArticleNEUROPHARMACOLOGY

Central Mechanisms Regulating Penile Erection in Conscious Rats: The Dopaminergic Systems Related to the Proerectile Effect of Apomorphine

Gin C. Hsieh, Peter R. Hollingsworth, Brenda Martino, Renjie Chang, Marc A. Terranova, Alyssa B. O'Neill, James J. Lynch, Robert B. Moreland, Diana L. Donnelly-Roberts, Teodozyi Kolasa, Joseph P. Mikusa, Jill M. McVey, Kennan C. Marsh, James P. Sullivan and Jorge D. Brioni
Journal of Pharmacology and Experimental Therapeutics January 1, 2004, 308 (1) 330-338; DOI: https://doi.org/10.1124/jpet.103.057455

Citation Manager Formats

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

Share
Research ArticleNEUROPHARMACOLOGY

Central Mechanisms Regulating Penile Erection in Conscious Rats: The Dopaminergic Systems Related to the Proerectile Effect of Apomorphine

Gin C. Hsieh, Peter R. Hollingsworth, Brenda Martino, Renjie Chang, Marc A. Terranova, Alyssa B. O'Neill, James J. Lynch, Robert B. Moreland, Diana L. Donnelly-Roberts, Teodozyi Kolasa, Joseph P. Mikusa, Jill M. McVey, Kennan C. Marsh, James P. Sullivan and Jorge D. Brioni
Journal of Pharmacology and Experimental Therapeutics January 1, 2004, 308 (1) 330-338; DOI: https://doi.org/10.1124/jpet.103.057455
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
    • Footnotes
    • References
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF

Related Articles

Cited By...

More in this TOC Section

  • Iclepertin (BI 425809) in schizophrenia-related models
  • D1 agonist vs. methylphenidate on PFC working memory
  • Obesity Thwarts Preconditioning in TBI
Show more Neuropharmacology

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 © 2022 by the American Society for Pharmacology and Experimental Therapeutics