BML-190

BML-190

Drugbox
IUPAC_name = 2- [1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl] -1-morpholin-4-ylethanone



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PubChem = 2415
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chemical_formula = |C=23|H=23|Cl=1|N=2|O=4
molecular_weight = 426.892
smiles = C4COCCN4C(=O)Cc(c(c1cc2)cc2OC)c(C)n1C(=O)c3ccc(Cl)cc3
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BML-190 (Indomethacin morpholinylamide) is a drug used in scientific research which acts as a selective CB2 inverse agonist. [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 Letters". 2003 Feb 11;53(1-3):157-60. PMID 12586356] BML-190 is structurally derived from the NSAID indomethacin but has a quite different biological activity. [Klegeris A, Bissonnette CJ, McGeer PL. Reduction of human monocytic cell neurotoxicity and cytokine secretion by ligands of the cannabinoid-type CB2 receptor. "British Journal of Pharmacology". 2003 Jun;139(4):775-86. PMID 12813001] The activity produced by this compound is disputed, with some sources referring to it as a CB2 agonist rather than an inverse agonist; [Melck D, De Petrocellis L, Orlando P, Bisogno T, Laezza C, Bifulco M, Di Marzo V. Suppression of nerve growth factor Trk receptors and prolactin receptors by endocannabinoids leads to inhibition of human breast and prostate cancer cell proliferation. "Endocrinology". 2000 Jan;141(1):118-26. PMID 10614630] [Scutt A, Williamson EM. Cannabinoids stimulate fibroblastic colony formation by bone marrow cells indirectly via CB2 receptors. "Calcified Tissue International". 2007 Jan;80(1):50-9. PMID 17205329] this may reflect an error in classification, or alternatively it may produce different effects in different tissues, more research is required to resolve this dispute.

References


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