Metabolic and pharmacokinetic characterization of a new synthetic cannabinoid APINAC in rats

摘要: Adamantan-1-yl 1-pentyl-1H-indazole-3-carboxylate (APINAC), a new synthetic cannabinoid, was recently isolated from dietary supplement and identified in our laboratories. The metabolism pharmacokinetics of APINAC were studied vitro vivo with rat model. (2.0 μM) incubated liver microsomes (RLMs) for up to 90 min determine its phase I metabolic profile. also administered rats at dose 5 mg/kg intravenously (i.v.) or 10 mg/kg per os (p.o.). Blood samples collected specific time points, urine 1 day following administration. analyses conducted by both high- low-resolution liquid chromatography–tandem mass spectrometry. Although rapidly metabolized RLMs (t 1/2, 15.2 ± 0.4 min), pharmacokinetic experiments revealed moderate long half-lives [11.3 h 3.8 h (p.o.)]. A total 22 metabolites could be detected the urine. predominantly via ester hydrolysis carboxylic acids M1 (with hydroxylation) M18 (without hydroxylation), representative markers intake. Hydroxylation APINAC, without subsequent oxidation glucuronidation, observed case other metabolites. diagnosis illegal intake can realized through detection several characteristic human and/or itself blood.