Chen Z, Vaughn D A, Blakely P, Fanestil D D
Department of Medicine, School of Medicine, University of California, San Diego, La Jolla 92093-0623.
J Am Soc Nephrol. 1994 Dec;5(6):1361-8. doi: 10.1681/ASN.V561361.
The density of the rat renal pharmacologic receptor for thiazide-type diuretics, as quantitated by the maximal specific binding of (3H)metolazone, decreased to one-third normal after adrenalectomy. Selective glucocorticoid (dexamethasone or RU-28362) replacement increased thiazide receptor density to or above the normal level over the dose range of steroid that decreased thymus weight, which served as a bioassay for glucocorticoid activity. Mineralocorticoid (fludrocortisone or aldosterone), in doses that did not decrease thymus weight, also increased thiazide diuretic receptor density to or above normal. The addition of glucocorticoid (RU-28362) to maximal aldosterone increased thiazide receptor above that produced by aldosterone alone and to threefold normal. Similarly, the addition of aldosterone to high-dose RU-28362 also increased thiazide receptor density above that produced by the glucocorticoid alone and to threefold normal. Hence, the effects of glucocorticoids and mineralocorticoids appeared to be additive. The increase in renal thiazide receptor density produced by fludrocortisone, at a dose that elicited both mineralocorticoid and glucocorticoid effects, was unrelated to the basal (prethiazide) renal excretion of sodium, potassium, chloride, or calcium. However, fludrocortisone-pretreated animals responded to bendroflumethiazide with a greater natriuresis than did controls. In addition, the magnitudes of the thiazide-elicited natriuresis and chloriuresis correlated significantly with thiazide receptor. It was concluded that both the density of the renal thiazide receptor and the quantity of sodium and chloride reabsorbed by the thiazide-sensitive Na-Cl cotransporter in the kidney are under adrenocortical regulation.
用(3H)美托拉宗的最大特异性结合定量测定,噻嗪类利尿剂的大鼠肾药理受体密度在肾上腺切除术后降至正常水平的三分之一。选择性糖皮质激素(地塞米松或RU - 28362)替代在降低胸腺重量(作为糖皮质激素活性的生物测定指标)的类固醇剂量范围内,可使噻嗪受体密度增加至正常水平或以上。盐皮质激素(氟氢可的松或醛固酮)在不降低胸腺重量的剂量下,也可使噻嗪类利尿剂受体密度增加至正常水平或以上。在最大剂量醛固酮基础上加用糖皮质激素(RU - 28362),可使噻嗪受体高于单独使用醛固酮时的水平,并增至正常水平的三倍。同样,在高剂量RU - 28362基础上加用醛固酮,也可使噻嗪受体密度高于单独使用糖皮质激素时的水平,并增至正常水平的三倍。因此,糖皮质激素和盐皮质激素的作用似乎具有相加性。氟氢可的松在引起盐皮质激素和糖皮质激素效应的剂量下,使肾噻嗪受体密度增加,这与基础(噻嗪类药物治疗前)肾钠、钾、氯或钙的排泄无关。然而,氟氢可的松预处理的动物对苄氟噻嗪的利钠反应比对照组更大。此外,噻嗪类药物引起的利钠和利氯幅度与噻嗪受体显著相关。得出的结论是,肾噻嗪受体的密度以及肾脏中噻嗪敏感的钠 - 氯共转运体重吸收的钠和氯的量均受肾上腺皮质调节。