Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists

SN Mistry, JG Baker, PM Fischer, SJ Hill…

Index: Mistry, Shailesh N.; Baker, Jillian G.; Fischer, Peter M.; Hill, Stephen J.; Gardiner, Sheila M.; Kellam, Barrie Journal of Medicinal Chemistry, 2013 , vol. 56, # 10 p. 3852 - 3865

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Citation Number: 10

Abstract

β-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-selective molecules exist. To address this clinical need, we re-evaluated LK 204-545 (1), 1 a selective β1-adrenoceptor antagonist, and discovered it possessed significant partial agonism. ...