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精氨酸加压素抗利尿作用拮抗剂的进一步体内证据。

Further in vivo evidence for antagonist-to-antidiuretic action of arginine vasopressin.

作者信息

Ishikawa S, Kim J K, Schrier R W

出版信息

Am J Physiol. 1983 Nov;245(5 Pt 1):R713-9. doi: 10.1152/ajpregu.1983.245.5.R713.

DOI:10.1152/ajpregu.1983.245.5.R713
PMID:6688929
Abstract

The effect of a new arginine vasopressin (AVP) analogue, [1-(beta-mercapto-beta,beta-cyclopentamethylenepropionic acid), 2-O-ethyltyrosine, 4-valine]AVP or d(CH2)5Tyr(Et)VAVP, was examined on exogenous and endogenous AVP in the conscious rat. An intravenous injection of 8 micrograms/kg body wt of the AVP analogue completely blocked the antidiuretic effect of exogenous AVP (4 ng/kg body wt iv). Similarly, 8 micrograms/kg of the AVP analogue totally abolished the antidiuretic effect of infused AVP (0.1 mU X kg-1 X min-1) in the homozygous Brattleboro rats with central diabetes insipidus. The antagonism of this antidiuretic effect of exogenous AVP occurred in the absence of changes in urinary solute excretion, glomerular filtration rate (GFR), and mean arterial pressure. Intraperitoneal administration of the AVP analogue (30 micrograms/kg body wt) decreased the mean urinary osmolality in rats after 24 h of fluid deprivation from 3,098 +/- 140 to 797 +/- 155 mosmol/kg H2O (P less than 0.001). The duration of the antagonism of endogenous AVP was approximately 4.5 h. The antagonism of AVP was not dependent on the vascular properties of AVP, since the AVP analogue also blocked the antidiuretic effect of exogenous 1-deamino-8-D-AVP (DDAVP), an AVP analogue with negligible vascular properties. These in vivo results therefore indicate that d(CH2)5Tyr(Et)VAVP is a specific antagonist of the hydrosmotic effect of exogenous and endogenous AVP. In contrast to some previous analogues, this effect of the AVP analogue occurred in the absence of any known diuretic factors including an increase in GFR, solute excretion, and blood pressure.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

研究了一种新型精氨酸加压素(AVP)类似物,即[1-(β-巯基-β,β-环戊亚甲基丙酸),2-O-乙基酪氨酸,4-缬氨酸]AVP或d(CH2)5Tyr(Et)VAVP,对清醒大鼠中外源性和内源性AVP的影响。静脉注射8微克/千克体重的AVP类似物可完全阻断外源性AVP(4纳克/千克体重静脉注射)的抗利尿作用。同样,在患有中枢性尿崩症的纯合布拉特洛维大鼠中,8微克/千克的AVP类似物完全消除了输注AVP(0.1毫单位×千克-1×分钟-1)的抗利尿作用。外源性AVP这种抗利尿作用的拮抗作用发生时,尿溶质排泄、肾小球滤过率(GFR)和平均动脉压均无变化。腹腔注射AVP类似物(30微克/千克体重)可使禁水24小时后的大鼠平均尿渗透压从3098±140降至797±155毫摩尔/千克H2O(P<0.001)。内源性AVP拮抗作用的持续时间约为4.5小时。AVP的拮抗作用不依赖于AVP 的血管特性,因为该AVP类似物也能阻断外源性1-脱氨基-8-D-精氨酸加压素(DDAVP)的抗利尿作用,DDAVP是一种血管特性可忽略不计的AVP类似物。因此,这些体内实验结果表明,d(CH2)5Tyr(Et)VAVP是外源性和内源性AVP渗透作用的特异性拮抗剂。与一些先前的类似物不同,该AVP类似物的这种作用发生时,不存在任何已知的利尿因子,包括GFR增加、溶质排泄增加和血压升高。(摘要截取自250字)

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