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妥洛特罗对妊娠子宫肌层离体标本的作用。

The actions of tulobuterol on isolated preparations of gravid human myometrium.

作者信息

Ziccone S P, Paull J D

机构信息

Royal Women's Hospital, Department of Anaesthetics, Carlton, Victoria, Australia.

出版信息

Clin Exp Pharmacol Physiol. 1990 Sep;17(9):637-44. doi: 10.1111/j.1440-1681.1990.tb01364.x.

Abstract
  1. The effects of tulobuterol (Abbott 54173) on the contractile force developed by electrically stimulated strips of gravid (gestation 36-40 weeks) human uterine muscle were compared with those of isoprenaline and adrenalin. 2. Isoprenaline produced inhibition of electrically evoked contractions of myometrium from 12 of 17 women at concentrations at or below 1 mumol/L (range 0.001-1 mumol/L). It enhanced contractions at concentrations of 10-50 mumol/L. In tissues from the remaining five women isoprenaline produced neither inhibitory nor excitatory effects. Adrenalin (0.1-50 mumol/L) was found to enhance contractile force in a concentration-dependent manner (EC50 = 0.30 mumol/L). 3. In the presence of metoprolol (0.3 mumol/L), a selective antagonist at beta 1-adrenoceptors, the isoprenaline concentration-response relationship was shifted to the left, indicating that beta 1-adrenoceptors are present and that they mediate excitation in the human uterus. 4. In contrast tulobuterol (in neither the presence nor absence of metoprolol), in the same concentration range as isoprenaline and adrenalin, (0.001-50 mumol/L) was found to have no effect on the electrically evoked contraction of gravid human uterine muscle strips.
摘要
  1. 将妥洛特罗(雅培54173)对妊娠(妊娠36 - 40周)期人体子宫肌条电刺激产生的收缩力的影响,与异丙肾上腺素和肾上腺素的影响进行了比较。2. 异丙肾上腺素在浓度为1 μmol/L及以下(范围0.001 - 1 μmol/L)时,抑制了17名女性中12名的子宫肌层电诱发收缩。在浓度为10 - 50 μmol/L时增强了收缩。在其余五名女性的组织中,异丙肾上腺素既未产生抑制作用也未产生兴奋作用。发现肾上腺素(0.1 - 50 μmol/L)以浓度依赖方式增强收缩力(EC50 = 0.30 μmol/L)。3. 在β1 - 肾上腺素受体选择性拮抗剂美托洛尔(0.3 μmol/L)存在的情况下,异丙肾上腺素浓度 - 反应关系向左移动,表明存在β1 - 肾上腺素受体,且它们介导人体子宫的兴奋。4. 相比之下,妥洛特罗(无论有无美托洛尔),在与异丙肾上腺素和肾上腺素相同的浓度范围(0.001 - 50 μmol/L)内,对妊娠人体子宫肌条的电诱发收缩没有影响。

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