UCM1341 (UCM 1341) is a bivalent ligand with melatonin receptor agonist (hMT1/hMT2, pKi=9.11/8.77) and fatty acid amide hydrolase (FAAH) inhibitory activity (rFAAH IC5=0.85 nM).
UCM1341 exhibited greater neuroprotection against neuroinflammatory degeneration, compared with the reference compounds URB597 (FAAH inhibitor) and melatonin.
UCM1341 augmented the levels of anandamide and N-oleoylethanolamine, but not N-palmitoylethanolamine, up-regulated PPAR-α levels, attenuated demyelination and prevented the release of TNF-α, during neuroinflammation.
UCM1341 modulated inflammatory responses by contributing to microglia/macrophage polarization, stimulating formation of lipid-laden macrophages and regulating expression of proteins controlling cholesterol metabolism and efflux.
