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新型镇痛药奈福泮作用机制的电生理研究

Electrophysiological investigations on the mode of action of nefopam, a novel analgesic agent.

作者信息

Irikura T, Hirayama T, Taga F

出版信息

Jpn J Pharmacol. 1981 Oct;31(5):815-22. doi: 10.1254/jjp.31.815.

DOI:10.1254/jjp.31.815
PMID:7311174
Abstract

The mode of action of nefopam, a novel analgesic, on the splanchnic afferent pathway was investigated using electrophysiological methods. Nefopam (2.5 and 5.0 mg/kg, i.v.) caused arousal patterns in spontaneous rabbit EEG. In intact cats, nefopam (1.0, 2.5 and 5.0 mg/kg, i.v.) suppressed the evoked potentials recorded from the posterior sigmoid gyrus of the cortex, N. ventralis posterolateralis and N. centralis medialis of the thalamus and the ventrolateral funiculus of the spinal cord following splanchnic nerve stimulation without inhibiting potentials in the thalamocortical pathways. These depressant effects were not antagonized by a narcotic antagonist, levallorphan (0.5 mg/kg, i.v.). The inhibitory effect of nefopam on the spinal potential evoked by splanchnic nerve stimulation was not observed in spinal cats (C1-C2 transection) and pentobarbital-anesthetized cats. These results suggest that nefopam may inhibit the splanchnic afferent pathways in the spinal cord by reinforcing descending inhibitory systems originating in the supra-spinal structure, in a manner which differs from that seen with morphine.

摘要

采用电生理方法研究了新型镇痛药奈福泮对内脏传入通路的作用方式。奈福泮(静脉注射2.5和5.0毫克/千克)可引起兔脑电图的觉醒模式。在完整的猫中,奈福泮(静脉注射1.0、2.5和5.0毫克/千克)可抑制在刺激内脏神经后从皮质后乙状结肠回、丘脑腹后外侧核和丘脑中央内侧核以及脊髓腹外侧索记录到的诱发电位,而不抑制丘脑皮质通路中的电位。这些抑制作用不能被麻醉拮抗剂左洛啡烷(静脉注射0.5毫克/千克)所拮抗。在脊髓猫(C1-C2横断)和戊巴比妥麻醉的猫中未观察到奈福泮对内脏神经刺激诱发的脊髓电位的抑制作用。这些结果表明,奈福泮可能通过加强源自脊髓上结构的下行抑制系统来抑制脊髓中的内脏传入通路,其方式与吗啡不同。

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1
Electrophysiological investigations on the mode of action of nefopam, a novel analgesic agent.新型镇痛药奈福泮作用机制的电生理研究
Jpn J Pharmacol. 1981 Oct;31(5):815-22. doi: 10.1254/jjp.31.815.
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The effects of nefopam on blood acid-base status in the rabbit: interactions with morphine in the mouse and rabbit.奈福泮对家兔血液酸碱状态的影响:与吗啡在家鼠和家兔体内的相互作用。
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Analgesic studies with nefopam hydrochloride.盐酸奈福泮的镇痛研究。
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Spinal and Supraspinal sites for morphine and nefopam analgesia in the mouse.小鼠中吗啡和奈福泮镇痛的脊髓和脊髓上部位。
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[Effects of morphine on evoked potential recorded from pain-afferent pathways (author's transl)].吗啡对痛觉传入通路记录的诱发电位的影响(作者译)
Nihon Yakurigaku Zasshi. 1977 Jul;73(5):625-31. doi: 10.1254/fpj.73.625.