CB₁ cannabinoid receptor antagonism for treating inflammation and arthritis

Abstract

The application evaluated here describes the treatment of inflammation and arthritis as two new potential indications for CB₁ cannabinoid receptor antagonists. While these derivatives are known for their actions on food intake, energy metabolism and addictions, little is known on their anti-inflammatory properties. Here, the effects of three representative CB₁ antagonists, SR141716A, AM251 and a pyrazolo[1,5-a][1,3,5]triazine, are described in rodent in vivo models of inflammation. CB₁ receptor blockade decreased the lipopolysaccharide-induced cytokines production, the carrageenan-induced paw inflammation and hyperalgesia, and the signs of arthritis following complete Freund's adjuvant injection. However, no CB₁ knockout mice were used to confirm the involvement of the CB₁ receptors in the described effects. Thus, additional research is needed to confirm the usefulness of CB₁ antagonist in the claimed indications.

Keywords::

• arthritis
• carrageenan
• CB₁ cannabinoid receptor
• cytokines
• inflammation
• TNF-α.