Barnett A, Goldstein J, Fiedler E, Taber R
Eur J Pharmacol. 1975 Jan;30(1):23-8. doi: 10.1016/0014-2999(75)90197-1.
Some narcotic drugs have been reported to produce increases in muscle tone in rats. In our laboratory we have found that etonitazine produces a 'lead-pipe' rigidity of the trunk and limb musculature. The reported studies were conducted to characterize etonitazine-induced rigidity more fully, to compare the degree of rigidity with that produced by morphine, codeine and methadone, and to assess the sensitivity of this rigidity to centrally acting muscle relaxants. Of the 4 narcotics tested, etonitazine was far more potent than methadone or morphine for producing rigidity; codeine did not produce peak rigidity comparable to the other 3 narcotics. Etonitazine-induced rigidity occurs at a supraspinal level since the effect was prevented by spinal transsection. Etonitazine-induced rigidity was prevented by the narcotic antagonists cyclazocine, pentazocine and naloxone but not by the serotonin depletor, p-chlorophenylalanine. Etonitazine-induced rigidity was antagonized by centrally acting muscle relaxants, including diazepam, methocarbamol, carisoprodol and zoxazolamine; in agreement with their relative clinical muscle relaxant potencies, diazepam is the most potent antagonist of etonitazine-induced rigidity.
据报道,某些麻醉药物会使大鼠的肌张力增加。在我们实验室,我们发现依托尼嗪会使躯干和肢体肌肉组织产生“铅管样”强直。开展这些已报道的研究是为了更全面地描述依托尼嗪诱导的强直,将强直程度与吗啡、可待因和美沙酮所产生的强直程度进行比较,并评估这种强直对中枢性肌肉松弛剂的敏感性。在所测试的4种麻醉药物中,依托尼嗪产生强直的效力远高于美沙酮或吗啡;可待因未产生与其他3种麻醉药物相当的强直峰值。依托尼嗪诱导的强直发生在脊髓以上水平,因为脊髓横断可阻止这种效应。依托尼嗪诱导的强直可被麻醉拮抗剂环唑辛、喷他佐辛和纳洛酮阻断,但不能被5-羟色胺耗竭剂对氯苯丙氨酸阻断。依托尼嗪诱导的强直可被中枢性肌肉松弛剂拮抗,包括地西泮、美索巴莫、卡立普多和唑沙胺;与它们相对的临床肌肉松弛效力一致,地西泮是依托尼嗪诱导的强直的最有效拮抗剂。