A HPLC method for simultaneous determination of 5-aminoimidazole-4-carboxamide riboside and its active metabolite 5-aminoimidazole-4-carboxamide ribotide in tumor-bearing nude mice plasma and its application to pharmacokinetics study

Traumatic brain injury decreases AMP‐activated protein kinase activity and pharmacological enhancement of its activity improves cognitive outcome

“…), and has a short half‐life (Cheng et al . ), relatively high doses of this chemical were used to allow for sufficient brain penetration to increase AMPK phosphorylation. Our results show that systemic administration of 500 mg/kg of AICAR significantly increased AMPK phosphorylation in the injured brain, but did not influence learning in either the abbreviated or the standard water maze tasks.…”

“…Once inside the cell, AICAR is metabolized to 5-aminoimidazole-4-carboxamide-1-b-D-ribofuranotide, an AMP analog that interacts with the c subunit of AMPK allowing its activation (Merrill et al 1997;Jin et al 2007). As AICAR does not efficiently cross the bloodbrain barrier (Marangos et al 1990), and has a short half-life (Cheng et al 2013), relatively high doses of this chemical were used to allow for sufficient brain penetration to increase AMPK phosphorylation. Our results show that systemic administration of 500 mg/kg of AICAR significantly increased AMPK phosphorylation in the injured brain, but did not influence learning in either the abbreviated or the standard water maze tasks.…”

Gossypetin Prevents the Progression of Nonalcoholic Steatohepatitis by Regulating Oxidative Stress and AMP-Activated Protein Kinase

“…Although, it has been reported to have a preventive effect on liver steatosis, it suffers from poor selectivity and rapid clearance in vivo system (Feng et al, 2018). The elimination half-life (T 1/2 ) of AICAR after its intravenous administration at a dose of 200 mg/kg was 0.44 h in mice (Cheng et al, 2013). Furthermore, AICAR tends to accumulate in cells at millimolar concentrations through adenosine transporter leading to AMPK-independent or off-target effects, which hinders its use as a specific AMPK activator (Gadalla et al, 2004).…”

Methotrexate and 5-aminoimidazole-4-carboxamide riboside exert synergistic anticancer action against human breast cancer and hepatocellular carcinoma

“…PBS (250 μL, pH 2.5) was added per 250 mg tumor tissue and tumor tissue was homogenized. The concentrations of AICA riboside and its active metabolite AICA ribotide in plasma and tumors were assayed by an HPLC method developed by Cheng et al [29] . The pharmacokinetic parameters of AICA riboside and its active metabolite AICA ribotide in nude mouse plasma and tumors were estimated by non-compartment analysis.…”