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连续数日给药后苯巴比妥耐受性的产生(作者译)

[Development of tolerance of phenobarbital after administration over several days (author's transl)].

作者信息

Schmidt D, Kupferberg H J, Yonekawa W, Penry J K

出版信息

Arzneimittelforschung. 1978;28(9):1515-6.

PMID:582547
Abstract

In mice daily testing by maximal electroshock (MES) and pentylenetetrazole infusion (PTZ) 2 h after an i.p. injection of 25 mg/kg penobarbital (PB) was performed on days 1, 2, 4 through 8. The first twitch was delayed as compared to NaCl controls (50.4 +/- 4.8 s; 36.6 +/- 3.6 s; n = 53) on day 2, 4, 6 through 8. There was no tolerance of the PTZ induced tonic extension with Pb-treatment. In contrast, MES-tested mice developed tolerance, at day 5 the number of protected animals fell to about 50%. In view of the constant phenobarbital levels in plasma, a functional tolerance was assumed. The development of tolerance seemed to be connected with the spread of the discharge but not with discharge of the neurones themselves since it was observed only with MES but not wih PTZ-testing.

摘要

在小鼠中,于第1、2、4至8天,在腹腔注射25mg/kg苯巴比妥(PB)2小时后,通过最大电休克(MES)和戊四氮输注(PTZ)进行每日测试。与氯化钠对照组(50.4±4.8秒;36.6±3.6秒;n = 53)相比,在第2、4、6至8天,首次抽搐出现延迟。用铅处理后,未出现对PTZ诱导的强直性伸展的耐受性。相比之下,经MES测试的小鼠产生了耐受性,在第5天,受保护动物的数量降至约50%。鉴于血浆中苯巴比妥水平恒定,推测存在功能性耐受性。耐受性的发展似乎与放电的扩散有关,而与神经元自身的放电无关,因为仅在MES测试中观察到,而在PTZ测试中未观察到。

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