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卡马西平对肌梭放电的影响。

Effects of carbamazepine on muscle spindle discharges.

作者信息

Hershkowitz N, Raines A

出版信息

J Pharmacol Exp Ther. 1978 Mar;204(3):581-91.

PMID:147337
Abstract

Spinal and alpha-chloralose anesthetized cats were prepared for single unit recording from fibers originating in deefferented spindles of the triceps surae muscles. Carbamazepine (CBZ), 200 and 300 mg/kg, suspended in 1% methylcellulose in saline was administered i.p. and plasma concentrations were determined by gas liquid chromatography. Stretch induced by a 500 g weight drop was used to evaluate spontaneous, static stretch, and poststretch spindle activity, while stretch induced by stimulation of the antagonist muscle group was used to evaluate a phasic stretch response. Preparations were monitored from 15 minutes before to 90 minutes after drug administration. CBZ produced a concentration-dependent depression of most aspects of spindle activity at concentrations ranging from approximately 9 to 45 microgram/ml. Activity during the poststretch period exhibited the greatest sensitivity to CBZ depression, spontaneous and static stretch activity exhibited intermediate sensitivity and phasic responses were relatively insensitive. No difference between Ia and II sensory endings were observed. Spindle depression was evident at concentrations which had no effect on axonal conduction velocity. The possible influence of this peripheral activity of CBZ is discussed with regard to neurotoxicity and use in the treatment of various neuropathological states.

摘要

将脊髓和用α-氯醛糖麻醉的猫制备好,以便从起源于腓肠肌去传入肌梭的纤维进行单单位记录。将200和300毫克/千克的卡马西平(CBZ)悬浮于含1%甲基纤维素的生理盐水中,经腹腔注射给药,并通过气相液相色谱法测定血浆浓度。用500克重物下落引起的拉伸来评估自发、静态拉伸和拉伸后肌梭活动,而通过刺激拮抗肌群引起的拉伸来评估相位拉伸反应。在给药前15分钟至给药后90分钟对制备物进行监测。在浓度约为9至45微克/毫升的范围内,CBZ对肌梭活动的大多数方面产生浓度依赖性抑制。拉伸后期间的活动对CBZ抑制表现出最大敏感性,自发和静态拉伸活动表现出中等敏感性,相位反应相对不敏感。未观察到Ia和II感觉末梢之间的差异。在对轴突传导速度无影响的浓度下,肌梭抑制就很明显。关于CBZ的这种外周活动对神经毒性以及在治疗各种神经病理状态中的应用的可能影响进行了讨论。

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