一种合成激素拮抗剂对大鼠体内甲状旁腺激素介导的血钙反应的抑制作用。
Inhibition of the in vivo parathyroid hormone-mediated calcemic response in rats by a synthetic hormone antagonist.
作者信息
Doppelt S H, Neer R M, Nussbaum S R, Federico P, Potts J T, Rosenblatt M
出版信息
Proc Natl Acad Sci U S A. 1986 Oct;83(19):7557-60. doi: 10.1073/pnas.83.19.7557.
The parathyroid hormone (PTH) analog, [Tyr34]bovine PTH-(7-34)-amide, can inhibit the PTH-mediated elevation of plasma calcium in thyroparathyroidectomized rats in vivo. The analog is devoid of PTH-like agonist activity in this system. Repeated doses of analog inhibit the animal's calcemic response to PTH. The elevation in serum calcium levels mediated by PTH in this assay reflects PTH action (calcium mobilization) on bone. Earlier studies demonstrated antagonist properties of the analog in a renal-based assay; PTH-stimulated increases in urinary phosphate and cyclic AMP excretion were completely inhibited by the synthetic analog. Along with previous studies, this report indicates that [Tyr34]bovine PTH-(7-34)-amide is an effective in vivo antagonist for several major parameters of PTH action in both kidney and bone.
甲状旁腺激素（PTH）类似物，[酪氨酸34]牛PTH-（7-34）-酰胺，在体内可抑制甲状旁腺切除的大鼠中PTH介导的血浆钙升高。该类似物在该系统中没有PTH样激动剂活性。重复给予该类似物可抑制动物对PTH的血钙反应。在此测定中，PTH介导的血清钙水平升高反映了PTH对骨骼的作用（钙动员）。早期研究表明该类似物在基于肾脏的测定中具有拮抗特性；合成类似物可完全抑制PTH刺激的尿磷酸盐和环磷酸腺苷排泄增加。与先前的研究一起，本报告表明，[酪氨酸34]牛PTH-（7-34）-酰胺是肾脏和骨骼中PTH作用的几个主要参数的有效体内拮抗剂。
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