MICHAEL STOCKS MICHAEL.STOCKS@NOTTINGHAM.AC.UK
Professor of Medicinal Chemistry and Drug Discovery
Discovery of AZD3199, An Inhaled Ultralong Acting ?2 Receptor Agonist with Rapid Onset of Action
Stocks, Michael; Alcaraz, Lilian; Bailey, Andrew; Bonnert, Roger; Cadogan, Elaine; Christie, Jadeen; Dixon, John; Connolly, Stephen; Cook, Anthony; Fisher, Adrian; Flaherty, Alice; Humphries, Alexander; Ingall, Anthony; Jordan, Stephen; Lawson, Mandy; Mullen, Alex; Nicholls, David; Paine, Stuart; Pairaudeau, Garry; Young, Alan
Authors
Lilian Alcaraz
Andrew Bailey
Roger Bonnert
Elaine Cadogan
Jadeen Christie
John Dixon
Stephen Connolly
Anthony Cook
Adrian Fisher
Alice Flaherty
Alexander Humphries
Anthony Ingall
Stephen Jordan
Mandy Lawson
Alex Mullen
David Nicholls
STUART PAINE Stuart.Paine@nottingham.ac.uk
Associate Professor
Garry Pairaudeau
Alan Young
Abstract
A series of dibasic des-hydroxy ?2 receptor agonists has been prepared and evaluated for potential as inhaled ultra-long acting bronchodilators. Determination of activities at the human ?-adrenoreceptors demonstrated a series of highly potent and selective ?2 receptor agonists that were progressed to further study in a guinea pig histamine-induced bronchoconstriction model. Following further assessment by; onset studies in guinea pig tracheal rings and human bronchial rings contracted with methacholine (guinea pigs) or carbachol (humans), duration of action studies in guinea pigs after intratracheal (i. t.) administration and further selectivity and safety profiling AZD3199 was shown to have an excellent over all profile and was progressed into clinical evaluation as a new ultra-long acting inhaled ?2 receptor agonist with rapid onset of action.
Citation
Stocks, M., Alcaraz, L., Bailey, A., Bonnert, R., Cadogan, E., Christie, J., …Young, A. (2014). Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action. ACS Medicinal Chemistry Letters, 5(4), 416-421. https://doi.org/10.1021/ml4005232
Journal Article Type | Article |
---|---|
Acceptance Date | Feb 8, 2014 |
Online Publication Date | Feb 11, 2014 |
Publication Date | Apr 10, 2014 |
Deposit Date | Apr 17, 2014 |
Publicly Available Date | Apr 17, 2014 |
Journal | ACS Medicinal Chemistry Letters |
Print ISSN | 1948-5875 |
Electronic ISSN | 1948-5875 |
Publisher | American Chemical Society |
Peer Reviewed | Peer Reviewed |
Volume | 5 |
Issue | 4 |
Pages | 416-421 |
DOI | https://doi.org/10.1021/ml4005232 |
Public URL | https://nottingham-repository.worktribe.com/output/723363 |
Publisher URL | https://pubs.acs.org/doi/10.1021/ml4005232 |
Additional Information | This document is the unedited Author’s version of a Submitted Work that was subsequently accepted for publication in ACS Medicinal Chemistry Letters copyright © American Chemical Society after peer review. To access the final edited and published work see: http://pubs.acs.org/doi/ipdf/10.1021/ml4005232 |
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