{"title":"Could positive allosteric modulators of the cannabinoid CB1 receptor be efficacious and safe for the treatment of chronic pain?","authors":"Hayley M. Green , Michelle Glass","doi":"10.1016/j.coph.2024.102495","DOIUrl":null,"url":null,"abstract":"<div><div>Cannabinoids are effective analgesics but induce adverse cannabimimetic effects and the development of tolerance. Allosteric ligands of the cannabinoid CB<sub>1</sub> receptor (CB<sub>1</sub>) may harness the pain-relieving effects of cannabinoids with reduced adverse effects. CB<sub>1</sub> allosteric ligands bind at a site topographically distinct from the orthosteric binding site. CB<sub>1</sub> allosteric ligands have been shown to be effective pain-relieving drugs that do not appear to result in the production of adverse effects or the development of tolerance. While this therapeutic profile indicates that CB<sub>1</sub> allosteric ligands could be an effective treatment for chronic pain, their molecular mechanism of action remains unclear.</div></div>","PeriodicalId":50603,"journal":{"name":"Current Opinion in Pharmacology","volume":"79 ","pages":"Article 102495"},"PeriodicalIF":4.0000,"publicationDate":"2024-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Opinion in Pharmacology","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1471489224000651","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0
Abstract
Cannabinoids are effective analgesics but induce adverse cannabimimetic effects and the development of tolerance. Allosteric ligands of the cannabinoid CB1 receptor (CB1) may harness the pain-relieving effects of cannabinoids with reduced adverse effects. CB1 allosteric ligands bind at a site topographically distinct from the orthosteric binding site. CB1 allosteric ligands have been shown to be effective pain-relieving drugs that do not appear to result in the production of adverse effects or the development of tolerance. While this therapeutic profile indicates that CB1 allosteric ligands could be an effective treatment for chronic pain, their molecular mechanism of action remains unclear.
期刊介绍：
Current Opinion in Pharmacology (COPHAR) publishes authoritative, comprehensive, and systematic reviews. COPHAR helps specialists keep up to date with a clear and readable synthesis on current advances in pharmacology and drug discovery. Expert authors annotate the most interesting papers from the expanding volume of information published today, saving valuable time and giving the reader insight on areas of importance.
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