BML-190

Uses

BML-190, is a selective cannabinoid CB2 receptor, and it is also used for treatment of organophosphate and carbamate toxicity.

Definition

ChEBI: 2-[1-[(4-chlorophenyl)-oxomethyl]-5-methoxy-2-methyl-3-indolyl]-1-(4-morpholinyl)ethanone is a N-acylindole.

Biological Activity

Potent and selective CB 2 receptor ligand (K i values are 435 nM and > 2 μ M for CB 2 and CB 1 respectively).

References

[1] new dc, wong yh. bml-190 and am251 act as inverse agonists at the human cannabinoid cb2 receptor: signalling via camp and inositol phosphates. febs lett. 2003 feb 11;536(1-3):157-60. pubmed pmid: 12586356.
[2] chang yh, lee st, lin ww. effects of cannabinoids on lps-stimulated inflammatory mediator release from macrophages: involvement of eicosanoids. j cell biochem. 2001;81(4):715-23. pubmed pmid: 11329626.
[3] klegeris a, bissonnette cj, mcgeer pl. reduction of human monocytic cell neurotoxicity and cytokine secretion by ligands of the cannabinoid-type cb2 receptor. br j pharmacol. 2003 jun;139(4):775-86. pubmed pmid: 12813001; pubmed central pmcid: pmc1573900.
[4] scutt a, williamson em. cannabinoids stimulate fibroblastic colony formation by bone marrow cells indirectly via cb2 receptors. calcif tissue int. 2007 jan;80(1):50-9. epub 2007 jan 4. pubmed pmid: 17205329.
[5] zhang l, zhang x, wu p, li h, jin s, zhou x, li y, ye d, chen b, wan j. bml-111, a lipoxin receptor agonist, modulates the immune response and reduces the severity of collagen-induced arthritis. inflamm res. 2008 apr;57(4):157-62. doi: 10. 1007/s00011-007-7141-z. pubmed pmid: 18648754.
[6] zhang q, ma p, cole rb, wang g. in vitro metabolism of indomethacin morpholinylamide (bml-190), an inverse agonist for the peripheral cannabinoid receptor (cb(2)) in rat liver microsomes. eur j pharm sci. 2010 sep 11;41(1):163-72. doi: 10.1016/j.ejps.2010.06.004. epub 2010 jun 11. pubmed pmid: 20542112; pubmed central pmcid: pmc2907062.