Discovery of an M-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethanotetrahydronorthebaine as a Selective, Potent, and Orally Active κ-Opioid Receptor Agonist with an Improved Central Nervous System Safety Profile-Reference-Cited by-同舟云学术

Discovery of an M-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethanotetrahydronorthebaine as a Selective, Potent, and Orally Active κ-Opioid Receptor Agonist with an Improved Central Nervous System Safety Profile

Published:2021-08-13 Issue:16 Volume:64 Page:12414-12433
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

He Qian¹,Wei Yuanyuan²³,Liu Xiao¹,Ye Rongrong⁴,Kong Linghui¹,Li Zixiang¹,Jiang Shuang⁵,Yu Linqian¹,Chai Jingrui²,Xie Qiong¹,Fu Wei¹^ORCID,Wang Yujun²,Li Wei¹,Qiu Zhuibai¹,Liu Jinggen²,Shao Liming¹⁶^ORCID

Affiliation:

1. Department of Medicinal Chemistry, School of Pharmacy, Fudan University, No. 826 Zhangheng Road, Shanghai 201203, China

2. CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences and Collaborative Innovation Center for Brain Science, 555 Zuchongzhi Road, Shanghai 201203, China

3. School of Basic Medicine Sciences and Clinical Pharmacy, China Pharmaceutical University, No.639 Longmian Road, Nanjing 210009, China

4. School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418, China

5. School of Pharmacy, Nanjing University of Chinese Medicine, No.138, Xianlin Road, Nanjing 210023, China

6. State Key Laboratory of Medical Neurobiology, Fudan University, No. 138 Yixueyuan Road, Shanghai 200032, China

Funder

Youth Innovation Promotion Association of the Chinese Academy of Sciences

National Natural Science Foundation of China

Chinese Academy of Sciences

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.1c01082

Reference47 articles.

1. The Opioid Crisis and the Future of Addiction and Pain Therapeutics

2. Kappa-opioid receptor agonists in pain treatment

3. Psychotomimesis Mediated by κ Opiate Receptors

4. Analgesic Efficacy of Enadoline Versus Placebo or Morphine in Postsurgical Pain

5. Enadoline, a selective kappa opioid agonist: comparison with butorphanol and hydromorphone in humans

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