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|Section2= |Section3= }} 5-Aminoimidazole-4-carboxamide ribonucleotide (AICAR) is an intermediate in the generation of inosine monophosphate. AICAR is an analog of adenosine monophosphate (AMP) that is capable of stimulating AMP-dependent protein kinase (AMPK) activity. AICAR has been used clinically to treat and protect against cardiac ischemic injury.〔Corton JM, Gillespie JG, Hawley SA, Hardie DG. 5-aminoimidazole-4-carboxamide ribonucleoside. A specific method for activating AMP-activated protein kinase in intact cells? Eur J Biochem 229:558–565(1995)〕 The drug was first used in the 1980s as a method to preserve blood flow to the heart during surgery.〔Galinanes M, Bullough D, Mullane KM, Hearse DJ. Sustained protection by acadesine against ischemia- and reperfusion-induced injury. Studies in the transplanted rat heart.Circulation 86:589–597 (1992)〕 Currently, the drug has also been shown as a potential treatment for diabetes by increasing the metabolic activity of tissues by changing the physical composition of muscle.〔Zarembo, Alan. ("'Exercise pill' could take the work out of workouts." ) Los Angeles Times. 01 08 2008, n. pag. Web. 21 Jan. 2012.〕 ==Mechanism of action== Acadesine is an analog of adenosine that enters cardiac cells to inhibit adenosine kinase and adenosine deaminase. It enhances the rate of nucleotide re-synthesis increasing adenosine generation from adenosine monophosphate only during conditions of myocardial ischemia.〔Kristiansen, S.B. et al. 5-Aminoimidazole-4-carboxamide-1- β - d -ribofuranoside Increases Myocardial Glucose Uptake during Reperfusion and Induces Late Pre-conditioning : Potential Role of AMP-Activated Protein Kinase. Pharmacology Toxicology 10-16 (2009).doi:10.1111/j.1742-7843.2009.00402.x〕 In cardiac myocytes, acadesine is phosphorylated to AICAR to activate AMPK without changing the levels of the nucleotides.〔Zhang, L., Frederich, M., He, H., & Balschi, J. a. Relationship between 5-aminoimidazole-4-carboxamide-ribotide and AMP-activated protein kinase activity in the perfused mouse heart. American journal of physiology. Heart and circulatory physiology, 290(3), .H1235-43. (2006)doi:10.1152/ajpheart.00906.2005〕 AICAR is able to enter the de novo synthesis pathway for adenosine synthesis to inhibit adenosine deaminase causing an increase in ATP levels and adenosine levels.〔Longnus SL, Wambolt RB, Parsons HL, Brownsey RW, Allard MF 5-Aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside (AICAR) stimulates myocardial glycogenolysis by allosteric mechanisms. Am J Physiol Regul Integr Comp Physiol 284:R936–R944 (2003)〕 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「AICA ribonucleotide」の詳細全文を読む スポンサード リンク
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