Highly selective and potent mu opioid ligands by unexpected substituent on morphine skeleton

Wei Li; Yi-Min Tao; Yun Tang; Xue-Jun Xu; Jie Chen; Wei Fu; Xing-Hai Wang; Bo Chao; Wei Sheng; Qiong Xie; Zhui-Bai Qiu; Jing-Gen Liu

doi:10.1016/j.bmcl.2009.07.119

Highly selective and potent mu opioid ligands by unexpected substituent on morphine skeleton

Bioorg Med Chem Lett. 2010 Jan 1;20(1):418-21. doi: 10.1016/j.bmcl.2009.07.119. Epub 2009 Jul 29.

Authors

Wei Li¹, Yi-Min Tao, Yun Tang, Xue-Jun Xu, Jie Chen, Wei Fu, Xing-Hai Wang, Bo Chao, Wei Sheng, Qiong Xie, Zhui-Bai Qiu, Jing-Gen Liu

Affiliation

¹ Department of Medicinal Chemistry, School of Pharmacy, Fudan University, 138 Yixueyuan Road, Shanghai 200032, China.

PMID: 19932964
DOI: 10.1016/j.bmcl.2009.07.119

Abstract

Unexpected substituent on the well-known morphine skeleton is described to be account for highly selective and potent mu opioid ligands, which is strongly connected to substituted aromatic groups on this omitted 8alpha-position.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Crystallography, X-Ray
Humans
Ligands*
Molecular Conformation
Morphine / chemistry*
Protein Binding
Receptors, Opioid, mu / metabolism*
Thebaine / chemistry

Substances

Ligands
Receptors, Opioid, mu
Thebaine
Morphine