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新型大环内酯类抗生素米卡霉素(MOM)的一般药理学研究。1. 对中枢神经系统的作用(作者译)

[General pharmacological studies on a new macrolide antibiotic, miokamycin (MOM). 1. Effects on the central nervous system (author's transl)].

作者信息

Shibata U, Yamaki Y, Asaoka H, Sugiyama S, Takeda U, Nishimori T, Kobayashi F, Hori K

出版信息

Jpn J Antibiot. 1981 May;34(5):734-46.

PMID:6974788
Abstract

Behavioral and electroencephalographic (EEG) effects on a new macrolide antibiotic miokamycin (MOM), 9,3"-diacetylmidecamycin, were investigated in mice, rats and rabbits after oral administration. MOM caused a decrease in the spontaneous motor activity, a slight increase in the effect of megibal seizure at a dose of 1,000 mg (Potency)/kg, and an increase in the number of deaths on the maximal electroshock seizure after administration of doses more than 100 mg (Potency)/kg. Even at a dose of 1,000 mg (Potency)/kg, however, MOM showed no effects on general behavior, rectal temperature, traction test, inclined screen test, rotarod performance, thiopental-induced sleep, pentetrazol seizure, fighting behavior induced by electric stimulation and conditioned avoidance response. EEG effects in unanesthetized rabbits with permanent electrode implants were studied. MOM showed no effects on spontaneous EEG, arousal response to mesencephalic reticular stimulation, photic driving response, evoked cortical response by ventralis posterolateralis stimulation and afterdischarge elicited by hippocampal stimulation at a dose of 1,000 mg (Potency)/kg. Consequently, it can be concluded that MOM has no specific pharmacological effects on the central nervous system. Behavior effects of MOM metabolisms, Mb-1, Mb-2, Mb-6 an Mb-12, were almost the same as those of MOM in the mode of action.

摘要

在小鼠、大鼠和兔子口服新的大环内酯类抗生素米卡霉素(MOM,9,3"-二乙酰麦迪霉素)后,研究了其对行为和脑电图(EEG)的影响。MOM导致自发运动活动减少,在剂量为1000mg(效价)/kg时,大发作的效应略有增加,在给予超过100mg(效价)/kg的剂量后,最大电休克发作的死亡数增加。然而,即使在剂量为1000mg(效价)/kg时,MOM对一般行为、直肠温度、牵引试验、倾斜屏幕试验、转棒性能、硫喷妥钠诱导的睡眠、戊四氮惊厥、电刺激诱导的格斗行为和条件回避反应均无影响。研究了对植入永久电极的未麻醉兔子的脑电图影响。在剂量为1000mg(效价)/kg时,MOM对自发脑电图、对中脑网状刺激的觉醒反应、光驱动反应、腹后外侧刺激诱发的皮层反应以及海马刺激诱发的后放电均无影响。因此,可以得出结论,MOM对中枢神经系统没有特定的药理作用。MOM的代谢产物Mb-1、Mb-2、Mb-6和Mb-12的行为效应在作用方式上与MOM几乎相同。

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