Discovery of AZD3199, an inhaled ultralong acting β2 receptor agonist with rapid onset of action
A series of dibasic des-hydroxy β2 receptor agonists has been prepared and evaluated for potential as inhaled ultra-long acting bronchodilators. Determination of activities at the human β-adrenoreceptors demonstrated a series of highly potent and selective β2 receptor agonists that were progressed...
| Main Authors: | , , , , , , , , , , , , , , , , , , , |
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| Format: | Article |
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American Chemical Society
2014
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| Online Access: | https://eprints.nottingham.ac.uk/2950/ |
| _version_ | 1848790915902078976 |
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| author | 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 |
| author_facet | 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 |
| author_sort | Stocks, Michael |
| building | Nottingham Research Data Repository |
| collection | Online Access |
| description | A series of dibasic des-hydroxy β2 receptor agonists has been prepared and evaluated for potential as inhaled ultra-long acting bronchodilators. Determination of activities at the human β-adrenoreceptors demonstrated a series of highly potent and selective β2 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 β2 receptor agonist with rapid onset of action. |
| first_indexed | 2025-11-14T18:20:12Z |
| format | Article |
| id | nottingham-2950 |
| institution | University of Nottingham Malaysia Campus |
| institution_category | Local University |
| last_indexed | 2025-11-14T18:20:12Z |
| publishDate | 2014 |
| publisher | American Chemical Society |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | nottingham-29502020-05-04T16:43:16Z https://eprints.nottingham.ac.uk/2950/ Discovery of AZD3199, an inhaled ultralong acting β2 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 A series of dibasic des-hydroxy β2 receptor agonists has been prepared and evaluated for potential as inhaled ultra-long acting bronchodilators. Determination of activities at the human β-adrenoreceptors demonstrated a series of highly potent and selective β2 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 β2 receptor agonist with rapid onset of action. American Chemical Society 2014-02-08 Article PeerReviewed 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 and Young, Alan (2014) Discovery of AZD3199, an inhaled ultralong acting β2 receptor agonist with rapid onset of action. ACS Medicinal Chemistry Letters, 5 (4). pp. 416-421. ISSN 1948-5875 http://pubs.acs.org/journal/amclct doi:10.1021/ml4005232 doi:10.1021/ml4005232 |
| spellingShingle | 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 Discovery of AZD3199, an inhaled ultralong acting β2 receptor agonist with rapid onset of action |
| title | Discovery of AZD3199, an inhaled ultralong acting β2 receptor agonist with rapid onset of action |
| title_full | Discovery of AZD3199, an inhaled ultralong acting β2 receptor agonist with rapid onset of action |
| title_fullStr | Discovery of AZD3199, an inhaled ultralong acting β2 receptor agonist with rapid onset of action |
| title_full_unstemmed | Discovery of AZD3199, an inhaled ultralong acting β2 receptor agonist with rapid onset of action |
| title_short | Discovery of AZD3199, an inhaled ultralong acting β2 receptor agonist with rapid onset of action |
| title_sort | discovery of azd3199, an inhaled ultralong acting β2 receptor agonist with rapid onset of action |
| url | https://eprints.nottingham.ac.uk/2950/ https://eprints.nottingham.ac.uk/2950/ https://eprints.nottingham.ac.uk/2950/ |