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[抗刺激剂对肌肉收缩机制和神经系统的作用]

[Actions of counterirritants on the muscle contractile mechanism and nervous system].

作者信息

Futami T

出版信息

Nihon Yakurigaku Zasshi. 1984 Mar;83(3):207-18.

PMID:6327474
Abstract

Studies were conducted on the actions of counterirritants on muscle contractile mechanisms and nerve conduction in both isolated and intact preparations. Neuromuscular transmission was noncompetitively blocked with menthol and methyl salicylate (MS) and recovered to the control level after they were washed out. Contractions of the isolated frog rectus in response to ACh and electrical stimulation were antagonized with menthol, MS, and camphor; and the action of nonylic vanillyl amide ( NVA ) became irreversible at high concentration. Menthol and MS produced muscle contraction per se at high concentration and enhanced the caffeine elicited contractile activity. The enhancement was also seen with camphor. The amplitude of the action potential was reduced with menthol, camphor, and MS in a dose and time dependent manner in the isolated frog sciatic nerve. This action was also confirmed in the intraaxonal recordings and was more easily influenced in the small fibres than the large ones. Conduction of primary afferents from muscle and motoneuron was weakly restrained 30 min after the external application of plasters which contained menthol or camphor on the hair-removed skin of cat's hind limb. The refractory period was also apt to be prolonged, and there was an obvious disappearance of group II and III inhibition after the external application of menthol plasters without any effects on group Ia and group Ib inhibition. concentrations of menthol, camphor, and MS in the muscle that were percutaneously absorbed after the external application of plasters containing these drugs in usual dosage were 10 approximately 30, (ca.) 5, and 5 approximately micrograms/g tissue, respectively. These findings suggest that menthol, camphor, and MS have conductive anesthetic activities mainly being attributable to a suppression of Na+ activation, and they cause an inhibition of nerve conduction, neuromuscular transmission and excitation contraction coupling, and stabilization on the membrane of the ACh receptor. When plasters containing menthol or camphor, in high dose, are externally applied on the skin, weak conductive anesthetic actions are thought to appear which result from the percutaneously absorbed drugs. Counterirritants , in high dose, cause an enhancement on caffeine elicited contraction and muscle contraction.

摘要

研究了抗刺激剂对离体和完整标本中肌肉收缩机制和神经传导的作用。薄荷醇和水杨酸甲酯(MS)可非竞争性阻断神经肌肉传递,冲洗后恢复至对照水平。薄荷醇、MS和樟脑可拮抗离体青蛙直肠对乙酰胆碱(ACh)和电刺激的收缩反应;高浓度时,壬酸香草酰胺(NVA)的作用不可逆。薄荷醇和MS在高浓度时可引起肌肉收缩,并增强咖啡因引起的收缩活性。樟脑也有此增强作用。在离体青蛙坐骨神经中,薄荷醇、樟脑和MS可使动作电位幅度呈剂量和时间依赖性降低。在轴内记录中也证实了这一作用,且小纤维比大纤维更容易受影响。在猫后肢脱毛皮肤上外用含薄荷醇或樟脑的膏药30分钟后,肌肉和运动神经元的初级传入纤维传导受到轻微抑制。不应期也易于延长,外用薄荷醇膏药后,II组和III组抑制明显消失,而对Ia组和Ib组抑制无任何影响。外用常用剂量含这些药物的膏药后,经皮吸收到肌肉中的薄荷醇、樟脑和MS浓度分别约为10~30、(约)5和5~微克/克组织。这些发现表明,薄荷醇、樟脑和MS具有传导麻醉活性,主要归因于对Na+激活的抑制,它们可抑制神经传导、神经肌肉传递和兴奋收缩偶联,并稳定乙酰胆碱受体膜。当高剂量含薄荷醇或樟脑的膏药外用在皮肤上时,经皮吸收的药物会产生微弱的传导麻醉作用。高剂量的抗刺激剂会增强咖啡因引起的收缩和肌肉收缩。

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