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苏拉明对麻醉大鼠泮库溴铵所致神经肌肉阻滞的逆转作用。

Reversal by suramin of neuromuscular block produced by pancuronium in the anaesthetized rat.

作者信息

Henning R H, Nelemans A, Houwertjes M, Agoston S

机构信息

Department of Pharmacology/Clinical Pharmacology, University of Groningen, The Netherlands.

出版信息

Br J Pharmacol. 1993 Mar;108(3):717-20. doi: 10.1111/j.1476-5381.1993.tb12867.x.

DOI:10.1111/j.1476-5381.1993.tb12867.x
PMID:8467359
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1908058/
Abstract
  1. Rats were anaesthetized with sodium pentobarbitone and maximal twitches of a tibialis anterior muscle were evoked by stimulation of the motor nerve. 2. Suramin, injected intravenously in a series of cumulative bolus doses, each 15 mg kg-1, completely reversed a 90% depression of twitches maintained by a continuous intravenous infusion of pancuronium. The cumulated dose necessary to restore twitches to 50% of their control amplitude was 35 mg kg-1. Suramin did not modify a similar degree of block produced by suxamethonium, nor did it affect the amplitude of control maximal twitches, even in cumulative doses up to 150 mg kg-1. 3. The effects of bolus doses of suramin (85 mg kg-1), neostigmine (0.03 mg kg-1) and 4-aminopyridine (1.2 mg kg-1), calculated to restore pancuronium-blocked twitches to 95% of control amplitude, were compared. Suramin produced the most rapid reversal (1.1 +/- 0.5 min), but its duration of action was the shortest (9.4 +/- 1.6 min). Suramin was without effect on heart rate or blood pressure in the doses used. 4. The results showed that suramin reversed neuromuscular block produced by nondepolarizing blocking drug, pancuronium, but was without effect on a block produced by the depolarizing blocking drug, suxamethonium. Its short duration of action suggests that suramin would probably not be of value clinically as a reversal agent. However, it is possible that it might serve as a starter compound for the synthesis and development of a new class of reversal agents for use in anaesthetic practice.
摘要
  1. 用戊巴比妥钠麻醉大鼠,通过刺激运动神经诱发胫前肌的最大抽搐。2. 苏拉明以每15 mg kg-1的一系列累积推注剂量静脉注射,完全逆转了由持续静脉输注泮库溴铵维持的90%的抽搐抑制。将抽搐恢复至对照幅度50%所需的累积剂量为35 mg kg-1。苏拉明对琥珀胆碱产生的类似程度的阻滞没有影响,即使在高达150 mg kg-1的累积剂量下,它也不影响对照最大抽搐的幅度。3. 比较了推注剂量的苏拉明(85 mg kg-1)、新斯的明(0.03 mg kg-1)和4-氨基吡啶(1.2 mg kg-1)的效果,这些剂量经计算可将泮库溴铵阻滞的抽搐恢复至对照幅度的95%。苏拉明产生的逆转最快(1.1 +/- 0.5分钟),但其作用持续时间最短(9.4 +/- 1.6分钟)。所用剂量的苏拉明对心率或血压没有影响。4. 结果表明,苏拉明可逆转非去极化阻滞药泮库溴铵产生的神经肌肉阻滞,但对去极化阻滞药琥珀胆碱产生的阻滞没有影响。其作用持续时间短表明,苏拉明作为一种逆转剂在临床上可能没有价值。然而,它有可能作为合成和开发一类用于麻醉实践的新型逆转剂的起始化合物。

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本文引用的文献

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Actions of 4-aminopyridine on the cardiovascular systems of anaesthetized cats and dogs.
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Comparison of the pharmacological actions of some new 4-aminopyridine derivatives.
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Transmitter-like action of ATP on patched membranes of cultured myoblasts and myotubes.ATP对培养的成肌细胞和肌管的膜片钳记录显示出类似递质的作用。
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Suramin: a potent ATPase inhibitor which acts on the inside surface of the sodium pump.苏拉明:一种作用于钠泵内表面的强效ATP酶抑制剂。
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Purinoceptors in the rat heart.大鼠心脏中的嘌呤受体。
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Suramin: a reversible P2-purinoceptor antagonist in the mouse vas deferens.苏拉明:小鼠输精管中的一种可逆性P2嘌呤受体拮抗剂。
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A dual function for adenosine 5'-triphosphate in the regulation of vascular tone. Excitatory cotransmitter with noradrenaline from perivascular nerves and locally released inhibitory intravascular agent.三磷酸腺苷在血管张力调节中的双重作用。作为来自血管周围神经的去甲肾上腺素的兴奋性共递质以及局部释放的抑制性血管内介质。
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Suramin: an anticancer drug with a unique mechanism of action.苏拉明:一种具有独特作用机制的抗癌药物。
J Clin Oncol. 1989 Apr;7(4):499-508. doi: 10.1200/JCO.1989.7.4.499.
9
The inhibitory action of suramin on the P2-purinoceptor response in smooth muscle cells of guinea-pig taenia caeci.苏拉明对豚鼠盲肠带平滑肌细胞中P2嘌呤受体反应的抑制作用。
Eur J Pharmacol. 1989 Aug 3;166(3):531-4. doi: 10.1016/0014-2999(89)90370-1.
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ATP compartmentation in neuroendocrine secretory vesicles.
Ann N Y Acad Sci. 1990;603:353-63; discussion 364-5. doi: 10.1111/j.1749-6632.1990.tb37685.x.