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一系列双环双季铵酯的神经肌肉阻断作用

The neuromuscular blocking action of a series of bicyclic bis-oniu esters.

作者信息

Marshall I G

出版信息

Br J Pharmacol. 1968 Sep;34(1):56-69. doi: 10.1111/j.1476-5381.1968.tb07950.x.

DOI:10.1111/j.1476-5381.1968.tb07950.x
PMID:5676039
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1703435/
Abstract
  1. Thirteen bicyclic dicholine esters have been tested on mammalian and avian skeletal muscle preparations.2. One of the compounds exhibited depolarizing activity in all the preparations.3. Three of the compounds exhibited depolarizing or dual-blocking activity in avian and denervated mammalian preparations, but exhibited non-depolarizing blocking activity in innervated mammalian preparations.4. The remaining compounds exhibited non-depolarizing blocking activity with evidence of an additional facilitatory action.5. The activity exhibited was dependent upon the onium substituents and the structure of the bicyclic ring.6. All the compounds exhibited a choline-reversible block in the rapidly stimulated rat diaphragm preparation and six of them exhibited a secondary choline-reversible block of the rapidly stimulated cat tibialis anterior muscle.
摘要
  1. 已对13种双环二胆碱酯在哺乳动物和禽类骨骼肌制剂上进行了测试。

  2. 其中一种化合物在所有制剂中均表现出去极化活性。

  3. 三种化合物在禽类和去神经支配的哺乳动物制剂中表现出去极化或双重阻断活性,但在有神经支配的哺乳动物制剂中表现出非去极化阻断活性。

  4. 其余化合物表现出非去极化阻断活性,并伴有额外的促进作用。

  5. 所表现出的活性取决于鎓取代基和双环结构。

  6. 所有化合物在快速刺激的大鼠膈肌制剂中均表现出胆碱可逆性阻断,其中六种在快速刺激的猫胫前肌中表现出继发性胆碱可逆性阻断。

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1
The neuromuscular blocking action of a series of bicyclic bis-oniu esters.一系列双环双季铵酯的神经肌肉阻断作用
Br J Pharmacol. 1968 Sep;34(1):56-69. doi: 10.1111/j.1476-5381.1968.tb07950.x.
2
The neuromuscular blocking action of some NNN-tris and NN-bis-onium esters.某些NNN-三铵盐和NN-双铵酯的神经肌肉阻滞作用。
Eur J Pharmacol. 1968 Feb;2(4):258-64. doi: 10.1016/0014-2999(68)90075-7.
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Br J Pharmacol. 1970 Sep;40(1):68-77. doi: 10.1111/j.1476-5381.1970.tb10611.x.
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Studies on the blocking action of 2-(4-phenyl piperidino) cyclohexanol (AH5183).2-(4-苯基哌啶基)环己醇(AH5183)阻断作用的研究
Br J Pharmacol. 1970 May;38(3):503-16. doi: 10.1111/j.1476-5381.1970.tb10592.x.
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Arch Int Pharmacodyn Ther. 1974 Mar;208(1):35-51.
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Neuromuscular blocking activity of a new series of quaternary N-substituted choline esters.一系列新型季铵 N-取代胆碱酯的神经肌肉阻断活性
Br J Pharmacol. 1971 Sep;43(1):107-26. doi: 10.1111/j.1476-5381.1971.tb07161.x.
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引用本文的文献

1
Nicotinic stimulant action of some tolyl and xylyl analogues of 1,1-dimethyl-4-phenylpiperazinium (DMPP).1,1 - 二甲基 - 4 - 苯基哌嗪鎓(DMPP)的某些甲苯基和二甲苯基类似物的烟碱样兴奋作用。
Br J Pharmacol. 1971 Oct;43(2):370-8.
2
A comparison between the blocking actions of 2-(4-phenylpiperidino) cyclohexanol (AH 5183) and its N-methyl quaternary analogue (AH 5954).2-(4-苯基哌啶基)环己醇(AH 5183)及其N-甲基季铵类似物(AH 5954)阻断作用的比较。
Br J Pharmacol. 1970 Sep;40(1):68-77. doi: 10.1111/j.1476-5381.1970.tb10611.x.
3
Neuromuscular blocking activity of a new series of quaternary N-substituted choline esters.一系列新型季铵 N-取代胆碱酯的神经肌肉阻断活性
Br J Pharmacol. 1971 Sep;43(1):107-26. doi: 10.1111/j.1476-5381.1971.tb07161.x.

本文引用的文献

1
The Structure-Action Relationships to the Choline Group.胆碱基团的构效关系。
Science. 1949 Mar 11;109(2828):264-6. doi: 10.1126/science.109.2828.264-b.
2
Some aspects of the relationship between chemical constitution and curare-like activity.化学组成与箭毒样活性之间关系的某些方面。
Ann N Y Acad Sci. 1951 Oct;54(3):407-37. doi: 10.1111/j.1749-6632.1951.tb39934.x.
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A new series of synthetic curare-like compounds.
Ann N Y Acad Sci. 1951 Oct;54(3):395-406. doi: 10.1111/j.1749-6632.1951.tb39933.x.
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Curarization of denervated muscle.失神经肌肉的箭毒化作用。
Ann N Y Acad Sci. 1951 Oct;54(3):337-46. doi: 10.1111/j.1749-6632.1951.tb39929.x.
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An investigation of the molecular configurations favorable for stimulation or blockade of the acetylcholine-sensitive receptors of visceral organs.
J Pharmacol Exp Ther. 1951 Aug;102(4):219-36.
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Curare-like activity of some bis-choline derivatives.某些双胆碱衍生物的箭毒样活性。
Nature. 1951 Mar 31;167(4248):527-8. doi: 10.1038/167527a0.
7
Neuromuscular blocking action of succinyldicholine stereoisomers.琥珀酰二胆碱立体异构体的神经肌肉阻滞作用。
J Pharm Pharmacol. 1961 Nov;13:703-4. doi: 10.1111/j.2042-7158.1961.tb11897.x.
8
THE EFFECTS OF SYMPATHOMIMETIC AMINES ON CHRONICALLY DENERVATED SKELETAL MUSCLES.拟交感神经胺对长期去神经支配骨骼肌的影响。
Br J Pharmacol Chemother. 1965 Feb;24(1):98-109. doi: 10.1111/j.1476-5381.1965.tb02083.x.
9
SPONTANEOUS FIBRILLARY ACTIVITY OF DENERVATED MUSCLE.失神经肌肉的自发性纤维活动。
Nature. 1964 Jan 11;201:160-2. doi: 10.1038/201160a0.
10
Actions of triethylcholine on neuromuscular transmission.三乙胆碱对神经肌肉传递的作用。
Br J Pharmacol Chemother. 1961 Oct;17(2):176-95. doi: 10.1111/j.1476-5381.1961.tb01278.x.