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Predicting in vivo cardiovascular properties of β-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

Jillian G. Baker

Philip Kemp

Julie March

Laurice Fretwell

Stephen J. Hill

Sheila M. Gardiner



Abstract

β-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 (β1; HR) and hindquarters vascular conductance (β2; HVC) were used to measure receptor selectivity and ligand efficacy in vivo. CGP 20712A caused a dose-dependent decrease in basal HR (P

Journal Article Type Article
Publication Date Dec 1, 2011
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
APA6 Citation Baker, J. G., Kemp, P., March, J., Fretwell, L., Hill, S. J., & Gardiner, S. M. (2011). Predicting in vivo cardiovascular properties of β-blockers from cellular assays: a quantative comparison of cellular and cardiovascular pharmacological responses. FASEB Journal, 25(12), doi:10.1096/fj.11-192435
DOI https://doi.org/10.1096/fj.11-192435
Keywords β-adrenoceptor, Partial agonism, Intrinsic sympathomimetic activity, Heart rate, Vascular conductance
Publisher URL http://www.fasebj.org/content/25/12/4486.full
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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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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