Outputs (2)

Novel selective ?1-adrenoceptor antagonists for concomitant cardiovascular and respiratory disease (2017)
Journal Article
Baker, J. G., Gardiner, S. M., Woolard, J., Fromont, C., Jadhav, G. P., Mistry, S. N., …Fischer, P. M. (2017). Novel selective β1-adrenoceptor antagonists for concomitant cardiovascular and respiratory disease. FASEB Journal, 31(7), 3150-3166. https://doi.org/10.1096/fj.201601305R

?-Blockers reduce mortality and improve symptoms in people with heart disease. However, current clinically available ?-blockers have poor selectivity for the cardiac ?1-adrenoceptor (AR) over the lung ?2-AR. Unwanted ?2-blockade risks causing life-th... Read More about Novel selective ?1-adrenoceptor antagonists for concomitant cardiovascular and respiratory disease.

Similarity- and substructure-based development of ?2-adrenergic receptor ligands based on unusual scaffolds (2017)
Journal Article
Schmidt, D., Gunera, J., Baker, J. G., & Kolb, P. (in press). Similarity- and substructure-based development of ?2-adrenergic receptor ligands based on unusual scaffolds. ACS Medicinal Chemistry Letters, https://doi.org/10.1021/acsmedchemlett.6b00363

The ?2-adrenergic receptor (?2AR) is a G protein-coupled receptor (GPCR) and a well-explored target. Here, we report the discovery of 13 ligands, ten of which are novel, of this particular GPCR. They have been identified by similarity- and substructu... Read More about Similarity- and substructure-based development of ?2-adrenergic receptor ligands based on unusual scaffolds.