Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid Receptor Agonist

[Image: see text] Recently, targeting the G protein-biased signaling has emerged as an attractive therapeutic strategy for treating severe acute pain with the potential to reduce the side effect of the traditional opioid drug. Herein, we describe the discovery of a highly potent G protein-biased μ-o...

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Detalles Bibliográficos
Autores principales: Li, Xin, He, Wei, Chen, Yang, Yang, Guimei, Wan, Hong, Zhang, Lei, Hu, Qiyue, Feng, Jun, Zhang, Zhigao, He, Feng, Bai, Chang, Zhang, Lianshan, You, Li, Tao, Weikang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2017
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6645658/
https://www.ncbi.nlm.nih.gov/pubmed/31457439
http://dx.doi.org/10.1021/acsomega.7b01452
Descripción
Sumario:[Image: see text] Recently, targeting the G protein-biased signaling has emerged as an attractive therapeutic strategy for treating severe acute pain with the potential to reduce the side effect of the traditional opioid drug. Herein, we describe the discovery of a highly potent G protein-biased μ-opioid receptor (MOR) agonist, SHR9352. This novel molecule exhibited excellent MOR activity and limited β-arrestin recruitment, as well as a high selectivity over κ-opioid receptor and δ-opioid receptor demonstrated robust in vivo efficacy and displayed favorable pharmacokinetic properties across species.

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