2-(4-苯基哌啶基)环己醇（AH5183）阻断作用的研究
Studies on the blocking action of 2-(4-phenyl piperidino) cyclohexanol (AH5183).
作者信息
Marshall I G
出版信息
Br J Pharmacol. 1970 May;38(3):503-16. doi: 10.1111/j.1476-5381.1970.tb10592.x.
Abstract
- AH5183 (2-(4-phenyl piperidino) cyclohexanol) produced neuromuscular block of slow onset in rapidly stimulated nerve-skeletal muscle preparations of the rat, chicken and cat.2. The neuromuscular block was not antagonized by neostigmine, tetraethylammonium (TEA) or choline. The rate of onset of transmission failure was enhanced by factors which increase the release of acetylcholine.3. It was concluded that the neuromuscular blocking activity was primarily pre-junctional in origin, being due either to a non-competitive action on the choline transport mechanism, or to an intracellular action on acetylcholine metabolism.4. In high doses AH5183 possessed local anaesthetic activity, but this was considered insufficient to bring about the failure of neuromuscular transmission.5. AH5183 also produced a block of sympathetically innervated preparations that was indistinguishable from that produced by an alpha-adrenoceptor blocking drug.
摘要
AH5183（2-（4-苯基哌啶基）环己醇）在大鼠、鸡和猫的快速刺激神经-骨骼肌标本中产生起效缓慢的神经肌肉阻滞。
新斯的明、四乙铵（TEA）或胆碱不能拮抗这种神经肌肉阻滞。增加乙酰胆碱释放的因素可加快传递失败的起效速率。
得出的结论是，神经肌肉阻滞活性主要源于接头前，要么是对胆碱转运机制的非竞争性作用，要么是对乙酰胆碱代谢的细胞内作用。
高剂量时，AH5183具有局部麻醉活性，但认为这不足以导致神经肌肉传递失败。
AH5183还可使交感神经支配的标本产生阻滞，这与α-肾上腺素受体阻断药产生的阻滞无法区分。
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本文引用的文献
1
On the nature of inhibition in the intestine.论肠道抑制的本质。
J Physiol. 1930 Sep 18;70(2):145-57. doi: 10.1113/jphysiol.1930.sp002683.
2
The action of d-tubocurarine and of decamethonium on respiratory and other muscles in the cat.d-筒箭毒碱和十烃季铵对猫呼吸肌及其他肌肉的作用。
J Physiol. 1951 Feb;112(3-4):311-31. doi: 10.1113/jphysiol.1951.sp004531.
3
MECHANISM OF THE ANTAGONISM BY TETRAETHYLAMMONIUM OF NEUROMUSCULAR BLOCK DUE TO D-TUBOCURARINE OR CALCIUM DEFICIENCY.四乙铵对由d -筒箭毒碱或钙缺乏引起的神经肌肉阻滞的拮抗机制。
Nature. 1963 Aug 17;199:702-3. doi: 10.1038/199702a0.
4
Effects of calcium on the conductance change of the end-plate membrane during the action of transmitter.钙对递质作用期间终板膜电导变化的影响。
J Physiol. 1963 Jun;167(1):141-55. doi: 10.1113/jphysiol.1963.sp007137.
5
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.
6
A comparison between the effects of edrophonium and choline in the skeletal muscles of the cat.依酚氯铵与胆碱对猫骨骼肌作用的比较。
Br J Pharmacol Chemother. 1959 Dec;14(4):456-66. doi: 10.1111/j.1476-5381.1959.tb00949.x.
7
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Int Rev Neurobiol. 1960;2:77-97. doi: 10.1016/s0074-7742(08)60120-8.
8
The isolated chick biventer cervicis nerve-muscle preparation.离体鸡颈二腹肌神经-肌肉标本。
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9
The anticurare activity of tetraethylammonium (TEA).四乙铵（TEA）的抗箭毒活性。
Acta Pharmacol Toxicol (Copenh). 1958;14(4):317-32.
10
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