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氨基甲酸酯类抗胆碱酯酶在牛气管平滑肌中产生的挛缩。

Contractures produced by carbamate anticholinesterases in bovine tracheal smooth muscle.

作者信息

Kirkpatrick C T, Rooney P J

出版信息

Clin Exp Pharmacol Physiol. 1982 Nov-Dec;9(6):603-11. doi: 10.1111/j.1440-1681.1982.tb00831.x.

Abstract
  1. In isolated strips of bovine tracheal muscle the carbamate anticholinesterases, neostigmine and eserine caused similar, slowly-developing, sustained spasms which were concentration-related in the range 10(-7)-10(-4) mol/l; these spasms could be abolished either by withdrawing the anticholinesterase or by addition of atropine (5 X 10(-7) mol/l). 2. Depletion of tissue stores of acetylcholine using hemicholinium-3 with or without electrical stimulation rendered the muscle unresponsive to neostigmine (10(-6) mol/l). Responses to acetylcholine itself were not impaired. 3. A low concentration of neostigmine (10(-8) mol/l) did not cause spasm but enhanced the contractile response of bovine trachealis to acetylcholine, carbachol and histamine. This concentration of neostigmine also increased the muscle's contraction upon exposure to a high-potassium solution, even in the presence of atropine (5 X 10(-7) mol/l). 4. It is concluded that neostigmine and eserine cause spasm not only by preventing breakdown of endogenously released acetylcholine but also by stimulating release of acetylcholine from nerve terminals and by a non-specific enhancement of muscle contraction.
摘要
  1. 在离体的牛气管肌条中,氨基甲酸酯类抗胆碱酯酶、新斯的明和毒扁豆碱引起相似的、缓慢发展的持续性痉挛,在10⁻⁷ - 10⁻⁴mol/L范围内与浓度相关;这些痉挛可通过撤去抗胆碱酯酶或加入阿托品(5×10⁻⁷mol/L)而消除。2. 使用半胱氨酸-3耗尽组织中的乙酰胆碱储备,无论有无电刺激,均可使肌肉对新斯的明(10⁻⁶mol/L)无反应。对乙酰胆碱本身的反应未受损害。3. 低浓度的新斯的明(10⁻⁸mol/L)不会引起痉挛,但可增强牛气管肌对乙酰胆碱、卡巴胆碱和组胺的收缩反应。即使在存在阿托品(5×10⁻⁷mol/L)的情况下,这种浓度的新斯的明也会增加肌肉在暴露于高钾溶液时的收缩。4. 得出的结论是,新斯的明和毒扁豆碱引起痉挛不仅是通过阻止内源性释放的乙酰胆碱的分解,还通过刺激神经末梢释放乙酰胆碱以及非特异性增强肌肉收缩。

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