JILLIAN BAKER jillian.baker@nottingham.ac.uk
Professor of Drug Discovery and Respiratory Medicine
Predicting in vivo cardiovascular properties of ?-blockers from cellular assays: a quantative comparison of cellular and cardiovascular pharmacological responses
Baker, Jillian G.; Kemp, Philip; March, Julie; Fretwell, Laurice; Hill, Stephen J.; Gardiner, Sheila M.
Authors
Philip Kemp
Julie March
Laurice Fretwell
Stephen J. Hill
Sheila M. Gardiner
Abstract
?-Adrenoceptor antagonists differ in their degree of partial agonism. In vitro assays have provided information on ligand affinity, selectivity, and intrinsic efficacy. However, the extent to which these properties are manifest in vivo is less clear. Conscious freely moving rats, instrumented for measurement of heart rate (?1; HR) and hindquarters vascular conductance (?2; HVC) were used to measure receptor selectivity and ligand efficacy in vivo. CGP 20712A caused a dose-dependent decrease in basal HR (P
Citation
Baker, J. G., Kemp, P., March, J., Fretwell, L., Hill, S. J., & Gardiner, S. M. (2011). Predicting in vivo cardiovascular properties of ?-blockers from cellular assays: a quantative comparison of cellular and cardiovascular pharmacological responses. FASEB Journal, 25(12), https://doi.org/10.1096/fj.11-192435
Journal Article Type | Article |
---|---|
Publication Date | Dec 1, 2011 |
Deposit Date | Apr 16, 2014 |
Publicly Available Date | Mar 29, 2024 |
Journal | FASEB Journal |
Print ISSN | 0892-6638 |
Electronic ISSN | 0892-6638 |
Publisher | Federation of American Society of Experimental Biology |
Peer Reviewed | Peer Reviewed |
Volume | 25 |
Issue | 12 |
DOI | https://doi.org/10.1096/fj.11-192435 |
Keywords | ?-adrenoceptor, Partial agonism, Intrinsic sympathomimetic activity, Heart rate, Vascular conductance |
Public URL | https://nottingham-repository.worktribe.com/output/1009501 |
Publisher URL | http://www.fasebj.org/content/25/12/4486.full |
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Copyright Statement
Copyright information regarding this work can be found at the following address: http://creativecommons.org/licenses/by-nc/4.0
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