The composite influence of the imidazolone moiety of CGP 12177 on its affinity and efficacy at the two conformations of the human ?1-adrenoceptor
(2016)
Conference Proceeding
Mistry, S. N., & Baker, J. G. (2016). The composite influence of the imidazolone moiety of CGP 12177 on its affinity and efficacy at the two conformations of the human ?1-adrenoceptor.
All Outputs (7)
The effect of the N-alkyl moiety on the interaction of pindolol analogues with the two agonist conformations of the human ?1-adrenoceptor (2016)
Conference Proceeding
Mistry, S. N., & Baker, J. G. (2016). The effect of the N-alkyl moiety on the interaction of pindolol analogues with the two agonist conformations of the human ?1-adrenoceptor.
Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human ?1-adrenoceptor (2013)
Journal Article
Baker, J. G., Hill, S. J., & Proudman, R. G. (2013). Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human ?1-adrenoceptor. PLoS ONE, 8(11), https://doi.org/10.1371/journal.pone.0077582?-blockers are widely used to improve symptoms and prolong life in heart disease primarily by inhibiting the actions of endogenous catecholamines at the ?1-adrenoceptor. There are two common naturally occurring polymorphisms within the human ?1-adren... Read More about Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human ?1-adrenoceptor.
Synthesis and in vitro and in vivo characterization of highly ?1-Selective ?-Adrenoceptor partial agonists (2013)
Journal Article
Mistry, S. N., Baker, J. G., Fischer, P. M., Hill, S. J., Gardiner, S. M., & Kellam, B. (2013). Synthesis and in vitro and in vivo characterization of highly ?1-Selective ?-Adrenoceptor partial agonists. Journal of Medicinal Chemistry, 56(10), https://doi.org/10.1021/jm400348gβ-Adrenoceptor antagonists boast a 50-year use for symptomatic control in numerous cardiovascular diseases. One might expect highly selective antagonists are available for the human β-adrenoceptor subtype involved in these diseases, yet few truly β1-... Read More about Synthesis and in vitro and in vivo characterization of highly ?1-Selective ?-Adrenoceptor partial agonists.
In vitro and in vivo analysis of a novel highly selective ?1-adrenoceptor partial agonist. (2012)
Conference Proceeding
Baker, J. G., Mistry, S. N., Fischer, P. M., Hill, S. J., Gardiner, S. M., & Kellam, B. (2012). In vitro and in vivo analysis of a novel highly selective ?1-adrenoceptor partial agonist.
Predicting in vivo cardiovascular properties of ?-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 ?-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?-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 ?-blockers from cellular assays: a quantative comparison of cellular and cardiovascular pharmacological responses.
Evolution of ?-blockers: from anti-anginal drugs to ligand-directed signalling (2011)
Journal Article
Baker, J. G., Hill, S. J., & Summers, R. J. (2011). Evolution of ?-blockers: from anti-anginal drugs to ligand-directed signalling. Trends in Pharmacological Sciences, 32(4), https://doi.org/10.1016/j.tips.2011.02.010Sir James Black developed ?-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 ?-blockers: from anti-anginal drugs to ligand-directed signalling.