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肾上腺素、异丙肾上腺素和福斯高林对人妊娠子宫肌层标本的作用。

Effects of adrenaline, isoprenaline and forskolin on pregnant human myometrial preparations.

作者信息

Story M E, Hall S, Ziccone S P, Paull J D

机构信息

Department of Pharmacology, Monash University, Clayton, Victoria, Australia.

出版信息

Clin Exp Pharmacol Physiol. 1988 Sep;15(9):703-13. doi: 10.1111/j.1440-1681.1988.tb01130.x.

DOI:10.1111/j.1440-1681.1988.tb01130.x
PMID:3271633
Abstract
  1. The effects of adrenaline, isoprenaline and forskolin upon the evoked contractions of field-stimulated preparations of human, pregnant, isolated myometrium have been examined. Specimens were obtained at lower segment Caesarean section from patients at 31 (n = 1) and 36-40 (n = 10) weeks of gestation. 2. Adrenaline enhanced the electrically evoked contractions of all preparations studied, indicating that its predominant action on these pregnant myometrial tissues was at alpha- and not beta-adrenoceptors. 3. Isoprenaline in concentrations at and below 10 mumol/l produced inhibitory effects in eight of 11 experiments. In the remaining three experiments, tissues were not responsive to the inhibitory effects of isoprenaline. 4. In all preparations exposed to higher concentrations of isoprenaline (30 or 100 mumol/l), its effects were excitatory. 5. Forskolin produced inhibitory effects on preparations from all uteri, including those from which tissues unresponsive to isoprenaline had been obtained. 6. It is suggested that forskolin in the concentrations which were effective in this study produced its inhibitory effects largely through activation of adenylate cyclase. This implies that the lack of an inhibitory response of some preparations to isoprenaline was not due to reduced activity of the adenylate cyclase system, but that the failure of isoprenaline to produce an inhibitory effect could be due to diminished numbers of beta-adrenoceptors and/or increased numbers of alpha-adrenoceptors, or to a defect in the coupling of the receptors to the adenylate cyclase system. Alternatively, the presence of an endogenous antagonist of the effects of isoprenaline (for example, an eicosanoid), could mask its inhibitory effects. 7. The absence of an inhibitory effect of isoprenaline on some specimens of human gravid myometrium could have clinical implications, in view of the widespread use of beta 2-adrenoceptor agonists as uterine relaxants.
摘要
  1. 已研究了肾上腺素、异丙肾上腺素和福斯高林对人妊娠离体子宫肌层场刺激标本诱发收缩的影响。标本取自妊娠31周(n = 1)和36 - 40周(n = 10)的患者,于下段剖宫产时获取。2. 肾上腺素增强了所有研究标本的电诱发收缩,表明其对这些妊娠子宫肌层组织的主要作用是作用于α - 而非β - 肾上腺素能受体。3. 浓度为10 μmol/l及以下的异丙肾上腺素在11个实验中的8个产生了抑制作用。在其余3个实验中,组织对异丙肾上腺素的抑制作用无反应。4. 在所有暴露于较高浓度异丙肾上腺素(30或100 μmol/l)的标本中,其作用是兴奋性的。5. 福斯高林对所有子宫的标本均产生抑制作用,包括那些对异丙肾上腺素无反应的子宫标本。6. 提示本研究中有效浓度的福斯高林主要通过激活腺苷酸环化酶产生抑制作用。这意味着一些标本对异丙肾上腺素缺乏抑制反应并非由于腺苷酸环化酶系统活性降低,而是异丙肾上腺素未能产生抑制作用可能是由于β - 肾上腺素能受体数量减少和/或α - 肾上腺素能受体数量增加,或受体与腺苷酸环化酶系统偶联存在缺陷。或者,存在异丙肾上腺素作用的内源性拮抗剂(例如,一种类二十烷酸)可能掩盖了其抑制作用。7. 鉴于β2 - 肾上腺素能受体激动剂作为子宫松弛剂的广泛应用,异丙肾上腺素对某些人妊娠子宫肌层标本缺乏抑制作用可能具有临床意义。

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Effects of adrenaline, isoprenaline and forskolin on pregnant human myometrial preparations.肾上腺素、异丙肾上腺素和福斯高林对人妊娠子宫肌层标本的作用。
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