Schoeffter P, Stoclet J C
Laboratoire de Pharmacologie Cellulaire et Moleculaire, CNRS URA 600, University Louis Pasteur, Strasbourg, France.
Mech Ageing Dev. 1990 Jun;54(3):197-205. doi: 10.1016/0047-6374(90)90050-p.
Experiments were designed to investigate the respective roles of adenylate cyclase and cyclic nucleotide phosphodiesterase in the alterations with age of cyclic AMP metabolism-dependent relaxation in rat aorta. Neither basal nor stimulated aortic adenylate cyclase activities from 7- and 18-week-old rats differed significantly. The maximal cyclic AMP accumulation induced by isoproterenol in the aorta decreased with the age of the rat as did the maximal relaxation produced by the beta-adrenergic agonist in pre-contracted aorta strips. The age-related difference in cyclic AMP accumulation was abolished when the experiment was performed in the presence of a high concentration (500 microM) of the phosphodiesterase inhibitor, 3-isobutyl-1-methylxanthine (IBMX). In addition, four phosphodiesterase inhibitors, IBMX, rolipram, Ro 20-1724 and zaprinast relaxed aorta strips pre-contracted by serotonin with concentration-effect curves which were displaced to the right in the older rats, the maximal effects being unchanged. The results suggest that the previously reported increased phosphodiesterase activity could be responsible for (1) the diminution with age of isoproterenol-induced cyclic AMP accumulation and relaxation in rat aorta; (2) the age-related decrease in potency of phosphodiesterase inhibitors as relaxing agents.
设计实验以研究腺苷酸环化酶和环核苷酸磷酸二酯酶在大鼠主动脉中与年龄相关的环磷酸腺苷(cAMP)代谢依赖性舒张改变中的各自作用。7周龄和18周龄大鼠的基础或刺激的主动脉腺苷酸环化酶活性均无显著差异。异丙肾上腺素在主动脉中诱导的最大cAMP积累随大鼠年龄的增长而降低,β-肾上腺素能激动剂在预收缩主动脉条中产生的最大舒张也随年龄增长而降低。当在高浓度(500 microM)的磷酸二酯酶抑制剂3-异丁基-1-甲基黄嘌呤(IBMX)存在下进行实验时,cAMP积累的年龄相关差异被消除。此外,四种磷酸二酯酶抑制剂,即IBMX、咯利普兰、Ro 20-1724和扎普司特使由5-羟色胺预收缩的主动脉条舒张,其浓度-效应曲线在老年大鼠中向右移位,最大效应不变。结果表明,先前报道的磷酸二酯酶活性增加可能是导致(1)异丙肾上腺素诱导的大鼠主动脉中cAMP积累和舒张随年龄降低;(2)磷酸二酯酶抑制剂作为舒张剂的效力随年龄降低的原因。