GW-405,833

GW-405,833 is a drug that was initially developed by GlaxoSmithKline for the treatment of pain. It is a potent and selective agonist for the cannabinoid receptor CB2, with a Ki of 5.2nM at CB2 vs 1,300nM at CB1, giving it around 250x selectivity for CB2.

Pharmacology[edit | edit source]

GW-405,833 is a cannabinoid drug that is a selective agonist for the CB2 receptor. It does not have a high affinity for the CB1 receptor, which is primarily found in the brain and is responsible for the psychoactive effects of cannabis. This makes GW-405,833 a potentially useful drug for pain relief without the risk of psychoactive side effects.

Clinical Trials[edit | edit source]

GW-405,833 has undergone clinical trials for the treatment of pain, but development was discontinued due to adverse side effects. However, it continues to be used in scientific research due to its selectivity for the CB2 receptor.

Side Effects[edit | edit source]

The most common side effects of GW-405,833 in clinical trials were nausea, dizziness, and headache. These side effects led to the discontinuation of its development as a pain medication.

Research[edit | edit source]

Despite its discontinuation as a therapeutic drug, GW-405,833 continues to be used in research due to its selectivity for the CB2 receptor. It has been used in studies investigating the role of the CB2 receptor in pain and inflammation, and in the potential therapeutic uses of CB2 agonists.