BML-190

426, 89

0 uM -100 uM

BML-190 has 50-fold selectivity for CB2 receptors over CB1 receptors. In HEK-293 cells stably expressing the human CB2 receptor, BML-190 potentiates the forskolin-stimulated accumulation of cAMP. BML-190 reduces the basal levels of inositol phosphate production in cells expressing the CB2 receptor. 10 uM of BML-190 decreases inositol phosphates accumulation by 38%. [1] BML-190 is an aminoalkylindole. BML-190 is found to yield at least 15 metabolic products. [2] BML-190 diminishes LPS-induced NO and IL-6 production in a concentration-dependent manner. BML-190 also inhibits LPS-induced PGE2 production and COX-2 induction. [3]

293/CB2 cells are labeled with [3H]adenine (1 uCi/mL) in MEM with 1% FBS for 20 hours-24 hours. Labelled cells are challenged with 50 uM forskolin and appropriate BML-190 for 30 minutes at 37C and assayed for cAMP accumulation. For IP assays, 2, 105 293/CB2 cells are transiently transfected with 16z44 and/or pcDNA3 using transfection reagents. Cells are labelled, challenged with BML-190 and assayed for IP production. Triplicates are performed for each data point and at least three separate trials are done for each ligand.

BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor.