All Outputs (3)

Predicting in vivo cardiovascular properties of β-blockers from cellular assays: a quantative comparison of cellular and cardiovascular pharmacological responses (2011)
Journal Article
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), https://doi.org/10.1096/fj.11-192435

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.... Read More about Predicting in vivo cardiovascular properties of β-blockers from cellular assays: a quantative comparison of cellular and cardiovascular pharmacological responses.

Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors (2011)
Journal Article
Baker, J. G., Adams, L. A., Salchow, K., Mistry, S. N., Middleton, R. J., Hill, S. J., & Kellam, B. (2011). Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors. Journal of Medicinal Chemistry, 54(19), 6874-6887. https://doi.org/10.1021/jm2008562

The growing practice of exploiting noninvasive fluorescence-based techniques to study G protein-coupled receptor pharmacology at the single cell and single molecule level demands the availability of high-quality fluorescent ligands. To this end, this... Read More about Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.

Evolution of β-blockers: from anti-anginal drugs to ligand-directed signalling (2011)
Journal Article
Baker, J. G., Hill, S. J., & Summers, R. J. (2011). Evolution of β-blockers: from anti-anginal drugs to ligand-directed signalling. Trends in Pharmacological Sciences, 32(4), https://doi.org/10.1016/j.tips.2011.02.010

Sir James Black developed β-blockers, one of the most useful groups of drugs in use today. Not only are they being used for their original purpose to treat angina and cardiac arrhythmias, but they are also effective therapeutics for hypertension, car... Read More about Evolution of β-blockers: from anti-anginal drugs to ligand-directed signalling.