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镓对去甲肾上腺素诱导的家兔主动脉平滑肌张力及相关的45Ca转运的特定作用。

Specific actions of gallium on norepinephrine-induced tension and associated 45Ca movements in rabbit aortic smooth muscle.

作者信息

Shetty S S, Weiss G B

机构信息

Research Department, CIBA-GEIGY Corporation, Summit, New Jersey.

出版信息

J Pharmacol Exp Ther. 1987 Nov;243(2):614-7.

PMID:3681698
Abstract

Gallium ion (Ga) dose-dependently (60-360 microM) inhibited contractions induced by norepinephrine (NE, 1 microM) in rabbit aortic (and media intimal) strips, but did not affect contractions elicited with high K+ (80 mM) solution. The initial phasic portion of the NE-induced response was either unaffected or only slightly (less than 10%) reduced, but the tonic portion of the response was inhibited completely by higher concentrations (greater than or equal to 300 microM) of Ga . In resting muscles, the equilibrated (90 min) 45Ca uptake was not altered by Ga (360 microM). Also, 45Ca efflux from either high- or low-affinity Ca++ binding sites was unaltered by Ga . The effects of Ga (360 microM) on 45Ca retained after a subsequent 60-min washout at 0.5 degrees C in an isosmotic (80.8 mM) La solution were also examined. High affinity La -resistant 45Ca released by NE (1 microM) was not altered by Ga . Under conditions favoring low affinity Ca++ uptake, 45Ca retention in control and K+-treated muscles was not changed by Ga , but the additional incremental 45Ca uptake associated with NE (in the presence of high K+) was blocked. Thus, Ga appears to have a selective inhibitory action on NE-associated 45Ca uptake without affecting either resting and high K+-induced 45Ca uptake or that 45Ca fraction released by NE. This action may result from a selective blockade by Ga of receptor-linked Ca++ channels in rabbit aortic smooth muscle.

摘要

镓离子(Ga)以剂量依赖方式(60 - 360微摩尔)抑制去甲肾上腺素(NE,1微摩尔)诱导的兔主动脉(和中膜内膜)条带收缩,但不影响高钾(80毫摩尔)溶液引发的收缩。NE诱导反应的初始相部分未受影响或仅略有(小于10%)降低,但反应的张力部分被较高浓度(大于或等于300微摩尔)的Ga完全抑制。在静息肌肉中,平衡(90分钟)的45Ca摄取不受Ga(360微摩尔)影响。此外,Ga对高亲和力或低亲和力Ca++结合位点的45Ca外流没有影响。还研究了Ga(360微摩尔)对在0.5℃下于等渗(80.8毫摩尔)镧溶液中随后60分钟冲洗后保留的45Ca的影响。NE(1微摩尔)释放的高亲和力抗镧45Ca不受Ga影响。在有利于低亲和力Ca++摄取的条件下,对照和钾处理肌肉中的45Ca保留量不受Ga影响,但与NE相关的额外增量45Ca摄取(在高钾存在下)被阻断。因此,Ga似乎对与NE相关的45Ca摄取具有选择性抑制作用,而不影响静息和高钾诱导的45Ca摄取或NE释放的45Ca部分。这种作用可能是由于Ga对兔主动脉平滑肌中受体连接的Ca++通道的选择性阻断所致。

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