Ali M, Guillon G, Balestre M N, Clos J
Horm Metab Res. 1987 Mar;19(3):115-21. doi: 10.1055/s-2007-1011755.
The effects of propylthiouracil (PTU) treatment on renal vasopressin sensitive adenylate cyclase in young and adult rats were studied by measuring the binding of tritiated vasopressin and adenylate cyclase activation by vasopressin in kidney medulla plasma membranes. Thyroxine therapy completely corrected the effects of PTU treatment on the vasopressin-adenylate cyclase system. Thus, the abnormalities observed after a such treatment are directly related to thyroid deficiency and not to toxic effects of PTU. The inability of the kidney to normally concentrate urine in developing and adult animals with induced hypothyroidism was mainly related to the reduction of the number of binding sites without significant changes in the basal and guanylyl-imidodiphosphate (Gpp(NH)p)-stimulated adenylate cyclase activities, the apparent dissociation constant (Kbind) of labeled vasopressin from its specific receptor and the apparent activation constant (Kact) of vasopressin for adenylate cyclase. These results also show that thyroid deficiency has more effect on the ontogenesis of receptors than on their turnover, and demonstrate that a normal antidiuretic response occurs at very low receptor occupancy. Since, on the one hand, the hypothyroidism-induced abnormalities in renal medulla responsiveness to vasopressin were reversible and, on the other, only a permanent therapy consisting of two daily physiological doses of thyroxine from birth to the age of sacrifice fully restored them, the responsiveness of developing kidney to thyroid hormones appears to be fundamentally different from that of the CNS.
通过测量肾髓质细胞膜中氚标记血管加压素的结合以及血管加压素对腺苷酸环化酶的激活作用,研究了丙硫氧嘧啶(PTU)治疗对幼年和成年大鼠肾血管加压素敏感性腺苷酸环化酶的影响。甲状腺素治疗完全纠正了PTU治疗对血管加压素-腺苷酸环化酶系统的影响。因此,这种治疗后观察到的异常与甲状腺功能减退直接相关,而非PTU的毒性作用。在诱导甲状腺功能减退的发育中和成年动物中,肾脏不能正常浓缩尿液主要与结合位点数量减少有关,而基础和鸟苷酰亚胺二磷酸(Gpp(NH)p)刺激的腺苷酸环化酶活性、标记血管加压素与其特异性受体的表观解离常数(Kbind)以及血管加压素对腺苷酸环化酶的表观激活常数(Kact)均无显著变化。这些结果还表明,甲状腺功能减退对受体的发生影响大于对其周转的影响,并证明在受体占有率非常低时也会出现正常的抗利尿反应。一方面,甲状腺功能减退引起的肾髓质对血管加压素反应性异常是可逆的;另一方面,只有从出生到处死每天给予两个生理剂量的甲状腺素进行长期治疗才能完全恢复这些异常,因此发育中的肾脏对甲状腺激素的反应性似乎与中枢神经系统的反应性有根本不同。