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• W2053735523 abstract "AM-1241, a novel, racemic cannabinoid-2 receptor (CB2) ligand, is the primary experimental agonist used to characterize the role of CB2-mediated lipid signaling in health and disease, including substance abuse disorders. In vivo pharmacological effects have been used as indirect proxies for AM-1241 biotransformation processes that could modulate CB2 activity. We report the initial pre-clinical characterization of AM-1241 biotransformation and in vivo distribution. AM-1241 metabolism was characterized in a variety of predictive in vitro systems (Caco-2 cells; mouse, rat and human microsomes) and in the mouse in vivo. Liquid chromatography and mass spectrometry techniques were used to quantify AM-1241 tissue distribution and metabolic conversion. AM-1241 bound extensively to plasma protein/albumin. A pharmacological AM-1241 dose (25 mg/kg, i.v.) was administered to mice for direct determination of its plasma half-life (37 min), following which AM-1241 was quantified in brain, spleen, liver, and kidney. After p.o. administration, AM-1241 was detected in plasma, spleen, and kidney; its oral bioavailability was ~ 21%. From Caco-2 permeability studies and microsomal-based hepatic clearance estimates, in vivo AM-1241 absorption was moderate. Hepatic microsomal metabolism of AM-1241 in vitro generated hydroxylation and demethylation metabolites. Species-dependent differences were discovered in AM-1241's predicted hepatic clearance. Our data demonstrate that AM-1241 has the following characteristics: a) short plasma half-life; b) limited oral bioavailability; c) extensive plasma/albumin binding; d) metabolic substrate for hepatic hydroxylation and demethylation; e) moderate hepatic clearance. These results should help inform the design, optimization, and pre-clinical profiling of CB2 ligands as pharmacological tools and medicines." @default.
• W2053735523 created "2016-06-24" @default.
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• W2053735523 date "2013-03-01" @default.
• W2053735523 modified "2023-09-25" @default.
• W2053735523 title "Therapeutic modulation of cannabinoid lipid signaling: Metabolic profiling of a novel antinociceptive cannabinoid-2 receptor agonist" @default.
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• W2053735523 doi "https://doi.org/10.1016/j.lfs.2012.06.019" @default.
• W2053735523 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3493696" @default.
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• W2053735523 hasPublicationYear "2013" @default.
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