GW-405,833 (L-768,242) is a drug that acts as a potent and selective

partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonis ...

for the

cannabinoid receptor Cannabinoid receptors, located throughout the body, are part of the endocannabinoid system a class of cell membrane receptors in the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid recep ...

subtype CB₂, with an EC₅₀ of 0.65 nM and selectivity of around 1200x for CB₂ over CB₁ receptors. Animal studies have shown it to possess

antiinflammatory Anti-inflammatory is the property of a substance or treatment that reduces inflammation or swelling. Anti-inflammatory drugs, also called anti-inflammatories, make up about half of analgesics. These drugs remedy pain by reducing inflammation as ...

and anti- hyperalgesic effects at low doses, followed by

ataxia Ataxia is a neurological sign consisting of lack of voluntary coordination of muscle movements that can include gait abnormality, speech changes, and abnormalities in eye movements. Ataxia is a clinical manifestation indicating dysfunction of ...

and analgesic effects when the dose is increased. Selective CB₂ agonist drugs such as GW-405,833 are hoped to be particularly useful in the treatment of

allodynia Allodynia is a condition in which pain is caused by a stimulus that does not normally elicit pain. For example, bad sunburn can cause temporary allodynia, and touching sunburned skin, or running cold or warm water over it, can be very painful. It i ...

and

neuropathic pain Neuropathic pain is pain caused by damage or disease affecting the somatosensory system. Neuropathic pain may be associated with abnormal sensations called dysesthesia or pain from normally non-painful stimuli (allodynia). It may have continuous ...

for which current treatment options are often inadequate.

References

{{cannabinoid-stub Cannabinoids Aminoalkylindoles Benzoylindoles 4-Morpholinyl compunds Phenol ethers Chlorobenzenes CB2 receptor agonists