IBMX3-Isobutyl-1-methylxanthine是一种广谱的磷酸二酯酶PDE抑制剂属于甲基黄嘌呤类化合物[1]。IBMX3-异丁基-1-甲基黄嘌呤AbMoleM6804通过抑制PDE对环磷酸腺苷cAMP和环磷酸鸟苷cGMP的水解提高细胞内cAMP和cGMP的水平从而激活蛋白激酶APKA和蛋白激酶GPKG信号通路调控多种细胞功能[1]。IBMXIsobutylmethylxanthine还可作为腺苷受体的竞争性拮抗剂阻断腺苷的抑制性信号传导这使其在神经和心血管系统研究中具有重要价值[2]。在细胞实验层面IBMX在3T3-L1前脂肪细胞中可与Dexamethasone 、Insulin 联合使用诱导细胞分化为成熟脂肪细胞IBMX在卵母细胞中可抑制PDE3活性维持cAMP水平并阻止减数分裂恢复在神经元细胞中IBMX能增强cAMP依赖性突触可塑性IBMX在胰岛β细胞中可增强葡萄糖诱导的胰岛素分泌[3]。在动物实验层面IBMX3-异丁基-1-甲基黄嘌呤AbMoleM6804在小鼠记忆障碍模型中可改善认知功能IBMX还能在支气管哮喘模型中松弛气道平滑肌此外IBMX在脂肪代谢研究中可促进大鼠脂解作用并增加能量消耗[4]。IBMX还被广泛应用于研究cAMP/PKA信号在基因转录、离子通道调控、神经递质释放及细胞增殖中的分子机制[5]。参考文献及鸣谢[1] Beavo, J. A.; Reifsnyder, D. H. Primary sequence of cyclic nucleotide phosphodiesterase isozymes and the design of selective inhibitors. Trends in Pharmacological Sciences 1990, 11 (4), 150-155.[2] Daly, J. W. Mechanism of action of caffeine. Caffeine, Coffee, and Health 1993, 97-150.[3] Student, A. K.; Hsu, R. Y.; Lane, M. D. Induction of fatty acid synthetase synthesis in differentiating 3T3-L1 preadipocytes. Journal of Biological Chemistry 1980, 255 (10), 4745-4750.[4] Conti, M.; Beavo, J. Biochemistry and physiology of cyclic nucleotide phosphodiesterases: essential components in cyclic nucleotide signaling. Annual Review of Biochemistry 2007, 76, 481-511.[5] Houslay, M. D. Underpinning compartmentalised cAMP signalling through targeted cAMP breakdown. Trends in Biochemical Sciences 2010, 35 (2), 91-100.
