Issue 54, 2022

Rational drug design of CB2 receptor ligands: from 2012 to 2021

Abstract

Cannabinoid receptors belong to the large family of G-protein-coupled receptors, which can be divided into two receptor types, cannabinoid receptor type-1 (CB1) and cannabinoid receptor type-2 (CB2). Marinol, Cesamet and Sativex are marketed CB1 drugs which are still in use and work well, but the central nervous system side effects caused by activation CB1, which limited the development of CB1 ligands. So far, no selective CB2 ligand has been approved for marketing, but lots of its ligands in the clinical stage and pre-clinical stage have positive effects on the treatment of some disease models and have great potential for development. Most selective CB2 agonists are designed and synthesized based on non-selective CB2 agonists through the classical med-chem strategies, e.g. molecular hybridization, scaffold hopping, bioisosterism, etc. During these processes, the balance between selectivity, activity, and pharmacokinetic properties needs to be achieved. Hence, we summarized some reported ligands on the basis of the optimization strategies in recent 10 years, and the limitations and future directions.

Graphical abstract: Rational drug design of CB2 receptor ligands: from 2012 to 2021

Article information

Article type
Review Article
Submitted
08 9月 2022
Accepted
03 12月 2022
First published
08 12月 2022
This article is Open Access
Creative Commons BY license

RSC Adv., 2022,12, 35242-35259

Rational drug design of CB2 receptor ligands: from 2012 to 2021

Y. Wu, J. Tang, W. Zhang, C. Zhuang and Y. Shi, RSC Adv., 2022, 12, 35242 DOI: 10.1039/D2RA05661E

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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