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 ArticleGastrointestinal, Hepatic, Pulmonary, and Renal

In Vitro Pharmacological Characterization of Vilanterol, a Novel Long-Acting β2-Adrenoceptor Agonist with 24-Hour Duration of Action

Robert J. Slack, Victoria J. Barrett, Valerie S. Morrison, Richard G. Sturton, Amanda J. Emmons, Alison J. Ford and Richard G. Knowles
Journal of Pharmacology and Experimental Therapeutics January 2013, 344 (1) 218-230; DOI: https://doi.org/10.1124/jpet.112.198481
Robert J. Slack
Respiratory TAU Biology (R.J.S., V.J.B, V.S.M., A.J.F, R.G.K.) and Screening and Compound Profiling, Platform Technology and Sciences (A.J.E.), GlaxoSmithKline, Stevenage, Hertfordshire, United Kingdom; Department of Thoracic Medicine, National Heart and Lung Institute, London, United Kingdom (R.G.S.); and Arachos Pharma, Stevenage Bioscience Catalyst, Stevenage, Hertfordshire, United Kingdom (R.G.K.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Victoria J. Barrett
Respiratory TAU Biology (R.J.S., V.J.B, V.S.M., A.J.F, R.G.K.) and Screening and Compound Profiling, Platform Technology and Sciences (A.J.E.), GlaxoSmithKline, Stevenage, Hertfordshire, United Kingdom; Department of Thoracic Medicine, National Heart and Lung Institute, London, United Kingdom (R.G.S.); and Arachos Pharma, Stevenage Bioscience Catalyst, Stevenage, Hertfordshire, United Kingdom (R.G.K.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Valerie S. Morrison
Respiratory TAU Biology (R.J.S., V.J.B, V.S.M., A.J.F, R.G.K.) and Screening and Compound Profiling, Platform Technology and Sciences (A.J.E.), GlaxoSmithKline, Stevenage, Hertfordshire, United Kingdom; Department of Thoracic Medicine, National Heart and Lung Institute, London, United Kingdom (R.G.S.); and Arachos Pharma, Stevenage Bioscience Catalyst, Stevenage, Hertfordshire, United Kingdom (R.G.K.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Richard G. Sturton
Respiratory TAU Biology (R.J.S., V.J.B, V.S.M., A.J.F, R.G.K.) and Screening and Compound Profiling, Platform Technology and Sciences (A.J.E.), GlaxoSmithKline, Stevenage, Hertfordshire, United Kingdom; Department of Thoracic Medicine, National Heart and Lung Institute, London, United Kingdom (R.G.S.); and Arachos Pharma, Stevenage Bioscience Catalyst, Stevenage, Hertfordshire, United Kingdom (R.G.K.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Amanda J. Emmons
Respiratory TAU Biology (R.J.S., V.J.B, V.S.M., A.J.F, R.G.K.) and Screening and Compound Profiling, Platform Technology and Sciences (A.J.E.), GlaxoSmithKline, Stevenage, Hertfordshire, United Kingdom; Department of Thoracic Medicine, National Heart and Lung Institute, London, United Kingdom (R.G.S.); and Arachos Pharma, Stevenage Bioscience Catalyst, Stevenage, Hertfordshire, United Kingdom (R.G.K.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Alison J. Ford
Respiratory TAU Biology (R.J.S., V.J.B, V.S.M., A.J.F, R.G.K.) and Screening and Compound Profiling, Platform Technology and Sciences (A.J.E.), GlaxoSmithKline, Stevenage, Hertfordshire, United Kingdom; Department of Thoracic Medicine, National Heart and Lung Institute, London, United Kingdom (R.G.S.); and Arachos Pharma, Stevenage Bioscience Catalyst, Stevenage, Hertfordshire, United Kingdom (R.G.K.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Richard G. Knowles
Respiratory TAU Biology (R.J.S., V.J.B, V.S.M., A.J.F, R.G.K.) and Screening and Compound Profiling, Platform Technology and Sciences (A.J.E.), GlaxoSmithKline, Stevenage, Hertfordshire, United Kingdom; Department of Thoracic Medicine, National Heart and Lung Institute, London, United Kingdom (R.G.S.); and Arachos Pharma, Stevenage Bioscience Catalyst, Stevenage, Hertfordshire, United Kingdom (R.G.K.)
  • 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

Vilanterol trifenatate (vilanterol) is a novel, long-acting β2-adrenoceptor (β2-AR) agonist with 24 h activity. In this study, we describe the preclinical pharmacological profile of vilanterol using radioligand binding and cAMP studies in recombinant assays as well as human and guinea pig tissue systems to characterize β2-AR binding and functional properties. Vilanterol displayed a subnanomolar affinity for the β2-AR that was comparable with that of salmeterol but higher than olodaterol, formoterol, and indacaterol. In cAMP functional activity studies, vilanterol demonstrated similar selectivity as salmeterol for β2- over β1-AR and β3-AR, but a significantly improved selectivity profile than formoterol and indacaterol. Vilanterol also showed a level of intrinsic efficacy that was comparable to indacaterol but significantly greater than that of salmeterol. In cellular cAMP production and tissue-based studies measuring persistence and reassertion, vilanterol had a persistence of action comparable with indacaterol and longer than formoterol. In addition, vilanterol demonstrated reassertion activity in both cell and tissue systems that was comparable with salmeterol and indacaterol but longer than formoterol. In human airways, vilanterol was shown to have a faster onset and longer duration of action than salmeterol, exhibiting a significant level of bronchodilation 22 h after treatment. From these investigations, the data for vilanterol are consistent, showing that it is a novel, potent, and selective β2-AR receptor agonist with a long duration of action. This pharmacological profile combined with clinical data is consistent with once a day dosing of vilanterol in the treatment of both asthma and chronic obstructive pulmonary disease (COPD).

Footnotes

  • dx.doi.org/10.1124/jpet.112.198481.

  • Received September 7, 2012.
  • Accepted November 6, 2012.
  • Copyright © 2013 by 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: 344 (1)
Journal of Pharmacology and Experimental Therapeutics
Vol. 344, Issue 1
1 Jan 2013
  • Table of Contents
  • Table of Contents (PDF)
  • About the Cover
  • 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.
In Vitro Pharmacological Characterization of Vilanterol, a Novel Long-Acting β2-Adrenoceptor Agonist with 24-Hour Duration of Action
(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 ArticleGastrointestinal, Hepatic, Pulmonary, and Renal

In Vitro Pharmacology of Vilanterol

Robert J. Slack, Victoria J. Barrett, Valerie S. Morrison, Richard G. Sturton, Amanda J. Emmons, Alison J. Ford and Richard G. Knowles
Journal of Pharmacology and Experimental Therapeutics January 1, 2013, 344 (1) 218-230; DOI: https://doi.org/10.1124/jpet.112.198481

Citation Manager Formats

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

Share
Research ArticleGastrointestinal, Hepatic, Pulmonary, and Renal

In Vitro Pharmacology of Vilanterol

Robert J. Slack, Victoria J. Barrett, Valerie S. Morrison, Richard G. Sturton, Amanda J. Emmons, Alison J. Ford and Richard G. Knowles
Journal of Pharmacology and Experimental Therapeutics January 1, 2013, 344 (1) 218-230; DOI: https://doi.org/10.1124/jpet.112.198481
Reddit logo Twitter logo Facebook logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One

Jump to section

  • Article
    • Abstract
    • Introduction
    • Materials and Methods
    • Results
    • Discussion
    • Acknowledgments
    • Authorship Contributions
    • Footnotes
    • Abbreviations
    • References
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF

Related Articles

Cited By...

More in this TOC Section

  • MIP3α in Progressive Renal Injury Associated with Obesity
  • A Novel Long-Acting GLP-2, HM15912, for Short Bowel Syndrome
  • H2S Overproduction and Colonic Hypomotility in DM
Show more Gastrointestinal, Hepatic, Pulmonary, and Renal

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