BML-190 (Indomethacin morpholinylamide) is a drug used in scientific research that acts as a selective CB₂

inverse agonist In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agon ...

. BML-190 is structurally derived from the

NSAID Non-steroidal anti-inflammatory drugs (NSAID) are members of a therapeutic drug class which reduces pain, decreases inflammation, decreases fever, and prevents blood clots. Side effects depend on the specific drug, its dose and duration of ...

indomethacin Indometacin, also known as indomethacin, is a nonsteroidal anti-inflammatory drug (NSAID) commonly used as a prescription drug, prescription medication to reduce fever, pain, joint stiffness, stiffness, and swelling (medical), swelling from infl ...

but has a quite different biological activity. The activity produced by this compound is disputed, with some sources referring to it as a CB₂

agonist An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ago ...

rather than an inverse agonist; this may reflect an error in classification, or alternatively it may produce different effects in different tissues, and more research is required to resolve this dispute.

Lead optimization Hit to lead (H2L) also known as lead generation is a stage in early drug discovery where small molecule hits from a high throughput screen (HTS) are evaluated and undergo limited optimization to identify promising lead compounds. These lead compo ...

of the parent structure resulted in

L-768,242 GW-405,833 (L-768,242) is a drug that acts as a potent and selective partial agonist for the cannabinoid receptor subtype CB2, with an EC50 of 0.65 nM and selectivity of around 1200x for CB2 over CB1 receptors. Animal studies have shown i ...

& L-759,787.

References

Cannabinoids 4-Morpholinyl compunds Indole ethers at the benzene ring Benzamides Chloroarenes Tryptamines {{cannabinoid-stub