Pharmacological characterization of a novel 5-hydroxybenzothiazolone-derived b2-adrenoceptor agonist with functional selectivity for anabolic effects on skeletal muscle resulting in a wider cardiovascular safety window in preclinical studies

Koziczak-Holbro, Magdalena; Rigel, Dean F.; Dumotier, B�reng�re; Sykes, David A.; Tsao, Jeffrey; Nguyen, Ngoc Hong; B�sch, Julian; Jourdain, Marie; Flotte, Ludivine; Adachi, Yuichiro; Kiffe, Michael; Azria, Mo�se; Fairhurst, Robin A.; Charlton, Steven J.; Richardson, Brian P.; Lach-Trifilieff, Estelle; Glass, David J.; Ullrich, Thomas; Hatakeyama, Shinji

doi:10.1124/jpet.118.255307

All Outputs (3)

Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor (2019)
Journal Article
Fyfe, T. J., Kellam, B., Sykes, D. A., Capuano, B., Scammells, P. J., Lane, J. R., …Mistry, S. N. (2019). Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor. Journal of Medicinal Chemistry, 62(21), 9488-9520. https://doi.org/10.1021/acs.jmedchem.9b00864

Haloperidol is a typical antipsychotic drug (APD) associated with an increased risk of extrapyramidal side-effects (EPS) and hyperprolactinemia relative to atypical APDs such as clozapine. Both drugs are dopamine D2 receptor (D2R) antagonists, with c... Read More about Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor.

Investigating the Influence of Tracer Kinetics on Competition-Kinetic Association Binding Assays: Identifying the Optimal Conditions for Assessing the Kinetics of Low-Affinity Compounds (2019)
Journal Article
Sykes, D. A., Jain, P., & Charlton, S. J. (2019). Investigating the Influence of Tracer Kinetics on Competition-Kinetic Association Binding Assays: Identifying the Optimal Conditions for Assessing the Kinetics of Low-Affinity Compounds. Molecular Pharmacology, 96(3), 378-392. https://doi.org/10.1124/mol.119.116764

An increased appreciation of the importance of optimizing drug-binding kinetics has lead to the development of various techniques for measuring the kinetics of unlabeled compounds. One approach is the competition-association kinetic binding method fi... Read More about Investigating the Influence of Tracer Kinetics on Competition-Kinetic Association Binding Assays: Identifying the Optimal Conditions for Assessing the Kinetics of Low-Affinity Compounds.

Pharmacological characterization of a novel 5-hydroxybenzothiazolone-derived b2-adrenoceptor agonist with functional selectivity for anabolic effects on skeletal muscle resulting in a wider cardiovascular safety window in preclinical studies (2019)
Journal Article
Koziczak-Holbro, M., Rigel, D. F., Dumotier, B., Sykes, D. A., Tsao, J., Nguyen, N. H., …Hatakeyama, S. (2019). Pharmacological characterization of a novel 5-hydroxybenzothiazolone-derived b2-adrenoceptor agonist with functional selectivity for anabolic effects on skeletal muscle resulting in a wider cardiovascular safety window in preclinical studies. Journal of Pharmacology and Experimental Therapeutics, 369(2), 188-199. https://doi.org/10.1124/jpet.118.255307

Copyright ª 2019 by The Author(s) The anabolic effects of b2-adrenoceptor (b2-AR) agonists on skeletal muscle have been demonstrated in various species. However, the clinical use of b2-AR agonists for skeletal muscle wasting conditions has been limit... Read More about Pharmacological characterization of a novel 5-hydroxybenzothiazolone-derived b2-adrenoceptor agonist with functional selectivity for anabolic effects on skeletal muscle resulting in a wider cardiovascular safety window in preclinical studies.