Valtin H, Coffey A K, O'Sullivan D J, Homma S, Dousa T P
Department of Physiology, Dartmouth Medical School, Hanover, NH.
Physiol Bohemoslov. 1990;39(1):103-11.
In a strain of mice called DI +/+ Severe, nephrogenic (or vasopressin-resistant) diabetes insipidus is caused by an inability of the antidiuretic hormone (ADH, or vasopressin) to increase the water permeability of the renal collecting system. That inability, in turn, arises from abnormally high activity of the enzyme cAMP-phosphodiesterase, specifically of the isozyme type III (PDE-III), which hydrolyzes cAMP and prevents the intracellular buildup of this second messenger. Two rather specific inhibitors of PDE-III, rolipram and cilostamide, used either in vitro or in vivo, reverse the deficiencies in DI +/+ Severe mice by increasing intracellular cAMP and water permeability toward or to their normal values. These results have implications for the treatment of nephrogenic diabetes insipidus in human patients.
在一种名为DI +/+ Severe的小鼠品系中,肾性(或抗血管加压素性)尿崩症是由抗利尿激素(ADH,即血管加压素)无法增加肾集合系统的水通透性所致。而这种无能反过来又源于酶cAMP - 磷酸二酯酶,特别是III型同工酶(PDE - III)的异常高活性,该酶水解cAMP并阻止这种第二信使在细胞内积累。两种相当特异的PDE - III抑制剂,咯利普兰和西洛酰胺,无论是在体外还是体内使用,都能通过将细胞内cAMP和水通透性提高到正常水平来逆转DI +/+ Severe小鼠的缺陷。这些结果对人类患者肾性尿崩症的治疗具有启示意义。