Abstract
The synthesis and biological evaluation of a novel class of cannabinoid receptor agonists based on a 5- sulfonamide benzimidazole scaffold are reported. They showed a high binding affinity to both receptors with great in vivo potency. When given orally to rats, they produced a robust analgesia in different models of inflammatory and neuropathic pain.
Keywords: Benzimidazoles, Cannabinoid agonists, Antinociception
Letters in Drug Design & Discovery
Title: 5-Sulfonamide Benzimidazoles: A Class of Cannabinoid Receptors Agonists with Potent In Vivo Antinociception Activity
Volume: 7 Issue: 3
Author(s): William Brown, Thierry Hong Groblewski, Xiao Hong Yu, Rosemarie Panetta, Kemal Payza, Etienne Lessard, Stephane St-Onge, Mirek Tomaszewski, Christopher Walpole, Daniel Page, Hua Yang, Sanjay Srivastava, Claire Milburn, Helene Desfosses, Maxime Tremblay, Ziping Liu and Zhongyong Wei
Affiliation:
Keywords: Benzimidazoles, Cannabinoid agonists, Antinociception
Abstract: The synthesis and biological evaluation of a novel class of cannabinoid receptor agonists based on a 5- sulfonamide benzimidazole scaffold are reported. They showed a high binding affinity to both receptors with great in vivo potency. When given orally to rats, they produced a robust analgesia in different models of inflammatory and neuropathic pain.
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Brown William, Groblewski Hong Thierry, Yu Hong Xiao, Panetta Rosemarie, Payza Kemal, Lessard Etienne, St-Onge Stephane, Tomaszewski Mirek, Walpole Christopher, Page Daniel, Yang Hua, Srivastava Sanjay, Milburn Claire, Desfosses Helene, Tremblay Maxime, Liu Ziping and Wei Zhongyong, 5-Sulfonamide Benzimidazoles: A Class of Cannabinoid Receptors Agonists with Potent In Vivo Antinociception Activity, Letters in Drug Design & Discovery 2010; 7 (3) . https://dx.doi.org/10.2174/157018010790596669
DOI https://dx.doi.org/10.2174/157018010790596669 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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