【摘要】 葡甲胺环磷酸腺苷(MGM-cAMP)可被依赖钙媒介蛋白的环核苷酸磷酸二酯酶(CaM-PDE)所水解,其降解速度仅及天然底物cAMP的75％。原因在于葡甲胺配基对PDE本身有抑制作用,抑制率约25％。MGM—cAMP对PDE的抑制作用可减慢分解,有利于其在体内发挥治疗作用。更多还原

【Abstract】 Meglumine-cAMP(MGM-cAMP), a new cAMP analog, commercially named as’Xin-Xian-An’, has been synthesized in our laboratory. Experiments showed that MGM-cAMP is susceptible to calmodulin-dependent phosphodiesterase (PDE), and the rate of its hydrolysis was 25% less, as compared with that of the natural substrate, cAMP. This inhibition was shown to be ascribed to meglumine, which, either in bound form or in free form, decreases the basal activity and restrains the stimulated adtivity of PDE. The presence of meglumine in the cAMP analog is a desirable feature of pharmacological importance, for the MGM ligand limits the hydrolysis of MGM-cAMP itself and thus prolongs its effect as a heart drug .更多还原