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1
The binding of tetrodotoxin and alpha-bungarotoxin to normal and denervated mammalian muscle.河豚毒素和α-银环蛇毒素与正常及去神经支配的哺乳动物肌肉的结合。
J Physiol. 1974 Jul;240(1):199-226. doi: 10.1113/jphysiol.1974.sp010607.
2
The binding of labelled saxitoxin to the sodium channels in normal and denervated mammalian muscle, and in amphibian muscle.标记的石房蛤毒素与正常和去神经支配的哺乳动物肌肉以及两栖动物肌肉中的钠通道的结合。
J Physiol. 1977 Jul;269(2):341-54. doi: 10.1113/jphysiol.1977.sp011905.
3
Appearance of new acetylcholine receptors on the baby chick biventer cervicis and denervated rat diaphragm muscles after blockade with alpha-bungarotoxin.用α-银环蛇毒素阻断后，雏鸡颈二腹肌和去神经大鼠膈肌上新乙酰胆碱受体的出现。
J Physiol. 1977 Jun;268(2):449-65. doi: 10.1113/jphysiol.1977.sp011865.
4
Tetrodotoxin binding to normal depolarized frog muscle and the conductance of a single sodium channel.河豚毒素与正常去极化青蛙肌肉的结合及单个钠通道的电导率。
J Physiol. 1975 May;247(2):483-509. doi: 10.1113/jphysiol.1975.sp010943.
5
Saxitoxin binding to sodium channels of rat skeletal muscles.石房蛤毒素与大鼠骨骼肌钠通道的结合。
J Physiol. 1980 Mar;300:89-103. doi: 10.1113/jphysiol.1980.sp013153.
6
Acetylcholine receptor and ion conductance modulator sites at the murine neuromuscular junction: evidence from specific toxin reactions.小鼠神经肌肉接头处的乙酰胆碱受体和离子电导调节位点：来自特定毒素反应的证据。
Proc Natl Acad Sci U S A. 1973 Mar;70(3):949-53. doi: 10.1073/pnas.70.3.949.
7
Interaction of di-iodinated 125I-labelled alpha-bungarotoxin and reversible cholinergic ligands with intact synaptic acetylcholine receptors on isolated skeletal-muscle fibres from the rat.二碘化的¹²⁵I标记的α-银环蛇毒素与可逆性胆碱能配体与来自大鼠的分离骨骼肌纤维上完整的突触乙酰胆碱受体的相互作用。
Biochem J. 1979 Sep 1;181(3):545-57. doi: 10.1042/bj1810545.
8
Two subtypes of sodium channel with tetrodotoxin sensitivity and insensitivity detected in denervated mammalian skeletal muscle.在去神经支配的哺乳动物骨骼肌中检测到对河豚毒素敏感和不敏感的两种钠通道亚型。
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9
Denervation increases the degradation rate of acetylcholine receptors at end-plates in vivo and in vitro.去神经支配会增加体内和体外终板处乙酰胆碱受体的降解速率。
J Physiol. 1983 Mar;336:159-77. doi: 10.1113/jphysiol.1983.sp014574.
10
Proceedings: The inhibition of alpha-bungarotoxin binding to denervated rat muscle by tubocurarine and other drugs.研究报告：筒箭毒碱及其他药物对α-银环蛇毒素与去神经大鼠肌肉结合的抑制作用。
Br J Pharmacol. 1974 May;51(1):124P-125P.

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SK3 is an important component of K(+) channels mediating the afterhyperpolarization in cultured rat SCG neurones.SK3是钾离子通道的一个重要组成部分，介导培养的大鼠颈上神经节神经元的超极化后电位。
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7
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Br J Pharmacol. 1983 Oct;80(2):235-40. doi: 10.1111/j.1476-5381.1983.tb10025.x.
8
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9
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Neuromuscular blocking agents inhibit receptor-mediated increases in the potassium permeability of intestinal smooth muscle.神经肌肉阻滞剂可抑制受体介导的肠道平滑肌钾通透性增加。
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本文引用的文献

1
The acetylcholine sensitivity of frog muscle fibres after complete or partial devervation.完全或部分去神经支配后青蛙肌肉纤维的乙酰胆碱敏感性
J Physiol. 1960 Apr;151(1):1-23.
2
The antagonism between tubocurarine and substances which depolarize the motor end-plate.筒箭毒碱与使运动终板去极化的物质之间的拮抗作用。
J Physiol. 1960 Jul;152(2):309-24. doi: 10.1113/jphysiol.1960.sp006489.
3
An investigation of spontaneous activity at the neuromuscular junction of the rat.大鼠神经肌肉接头处自发活动的研究。
J Physiol. 1956 Jun 28;132(3):650-66. doi: 10.1113/jphysiol.1956.sp005555.
4
The rate of action of competitive neuromuscular blocking agents.竞争性神经肌肉阻滞剂的作用速率。
J Pharmacol Exp Ther. 1967 Oct;158(1):99-114.
5
An upper limit to the number of sodium channels in nerve membrane?神经膜中钠通道数量的上限？
J Physiol. 1967 Jan;188(1):99-105. doi: 10.1113/jphysiol.1967.sp008126.
6
Voltage clamp experiments on internally perfused giant axons.对内部灌注的巨大轴突进行电压钳实验。
J Physiol. 1965 Oct;180(4):788-820. doi: 10.1113/jphysiol.1965.sp007732.
7
Actions of saxitoxin on peripheral neuromuscular systems.石房蛤毒素对周围神经肌肉系统的作用。
J Physiol. 1965 Sep;180(1):50-66.
8
A new kind of drug antagonism: evidence that agonists cause a molecular change in acetylcholine receptors.一种新型药物拮抗作用：激动剂引起乙酰胆碱受体分子变化的证据。
Mol Pharmacol. 1969 Jul;5(4):394-411.
9
A lesion of the transverse tubules of skeletal muscle.骨骼肌横小管的损伤。
J Physiol. 1969 May;201(3):515-33. doi: 10.1113/jphysiol.1969.sp008770.
10
Ionic conductances of the surface and transverse tubular membranes of frog sartorius fibers.青蛙缝匠肌纤维表面和横管膜的离子电导率。
J Gen Physiol. 1969 Mar;53(3):279-97. doi: 10.1085/jgp.53.3.279.

河豚毒素和α-银环蛇毒素与正常及去神经支配的哺乳动物肌肉的结合。

The binding of tetrodotoxin and alpha-bungarotoxin to normal and denervated mammalian muscle.

作者信息

Colquhoun D, Rang H P, Ritchie J M

出版信息

J Physiol. 1974 Jul;240(1):199-226. doi: 10.1113/jphysiol.1974.sp010607.

DOI:10.1113/jphysiol.1974.sp010607
PMID:4854666
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1330989/
Abstract
  1. The binding of [(3)H]tetrodotoxin and [(125)I]iodo-alpha-bungarotoxin to innervated and denervated rat diaphragm muscle has been measured.2. A saturable component of tetrodotoxin binding, which was inhibited by saxitoxin, was detected in addition to considerable non-saturable binding. The saturable component had an equilibrium constant of K = 6.1 nM (limits 4.7-7.8 nM) and binding capacity M = 2.5 f-mole/mg wet wt. (limits 2.1-2.8 f-mole/mg).3. If the saturable component consisted of one-to-one binding of tetrodotoxin to sodium channels, the density of sodium channels would be about 21/mum(2) of surface membrane, a figure similar to that found in other excitable membranes.4. After denervation the specific tetrodotoxin binding, as measured by the ratio M/K, fell by a factor of 2.8. This change appeared to be due to a fall in binding capacity rather than a decrease in affinity.5. After denervation the maximum rate of rise of the action potential fell by 27% and became partially resistant to tetrodotoxin. The maximum rate of rise was at first reduced by tetrodotoxin in similar concentrations to those affecting normal muscle, but even large concentrations which completely blocked normal muscle only reduced the maximum rate of rise by a factor of about 2.6. Detubulation with glycerol did not appreciably affect the tetrodotoxin sensitivity of normal or denervated muscle.7. Tetrodotoxin resistance was not observed after denervation of the frog sartorius muscle.8. [(125)I]iodo-alpha-bungarotoxin binding amounted to 3.8 +/- 0.7 f-mole/mg in innervated muscle and 44.5 +/- 2.1 f-mole/mg in denervated muscle. Most of the uptake was inhibitable by (+)-tubocurarine.9. The increase in the labelled bungarotoxin binding is much larger than the specific tetrodotoxin binding of innervated muscle, which renders implausible the possibility that the acetylcholine receptors which appear after denervation are related to the tetrodotoxin resistant-sodium channels.
摘要

  1. 已测定[(3)H]河豚毒素和[(125)I]碘α-银环蛇毒素与神经支配和去神经支配的大鼠膈肌的结合情况。

  2. 除了相当数量的非饱和结合外，还检测到一种可被蛤蚌毒素抑制的河豚毒素结合的饱和成分。该饱和成分的平衡常数K = 6.1 nM（范围4.7 - 7.8 nM），结合容量M = 2.5 f - 摩尔/毫克湿重（范围2.1 - 2.8 f - 摩尔/毫克）。

  3. 如果饱和成分由河豚毒素与钠通道的一对一结合组成，钠通道的密度将约为表面膜每平方微米21个，这一数字与在其他可兴奋膜中发现的相似。

  4. 去神经支配后，通过M/K比值测量的特异性河豚毒素结合下降了2.8倍。这种变化似乎是由于结合容量的下降而非亲和力的降低。

  5. 去神经支配后，动作电位的最大上升速率下降了27%，并变得对河豚毒素部分耐受。最初，河豚毒素以与影响正常肌肉相似的浓度降低最大上升速率，但即使是完全阻断正常肌肉的高浓度也仅使最大上升速率降低约2.6倍。用甘油去管化对正常或去神经支配肌肉的河豚毒素敏感性没有明显影响。

  6. 青蛙缝匠肌去神经支配后未观察到河豚毒素耐受性。

  7. [(125)I]碘α-银环蛇毒素结合在神经支配肌肉中为3.8±0.7 f - 摩尔/毫克，在去神经支配肌肉中为44.5±2.1 f - 摩尔/毫克。大部分摄取可被(+)-筒箭毒碱抑制。

  8. 标记的银环蛇毒素结合的增加远大于神经支配肌肉的特异性河豚毒素结合，这使得去神经支配后出现的乙酰胆碱受体与河豚毒素耐受钠通道相关的可能性不大。