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莫罗卡星的一般药理学特性。

General pharmacological properties of muroctasin.

作者信息

Kojima H, Hirohashi M, Kasai Y, Takasuna K, Fukumoto C, Akashi A

机构信息

Research Institute, Daiichi Seiyaku Co., Ltd., Tokyo, Japan.

出版信息

Arzneimittelforschung. 1988 Jul;38(7A):1002-9.

PMID:3190791
Abstract

General pharmacological effects of N2-[(N-acetyl-muramoyl)-L-alanyl-D-isoglutaminyl]-N6-stearoyl-L-ly sine MDP-Lys(L18), muroctasin) were examined and the following results were obtained. 1. Central nervous system: MDP-Lys(L18) had no effect on behavior, spontaneous motor activity, electroshock- and chemoshock-induced convulsions, hexobarbital sleeping time, pain threshold (mice), conditioned avoidance response (rats) at a dose of 0.4 mg/kg, s.c. and EEG as well as spinal reflex (cats) at a dose of 0.4 mg/kg, i.v. It produced a significant elevation in body temperature (rabbits) at doses of 13 micrograms/kg, s.c. and greater. 2. Respiratory and cardiovascular system (dogs): MDP-Lys(L18) did not show any significant effect on respiratory and cardiovascular functions at a dose of 0.4 mg/kg i.v. 3. Autonomic nervous system: MDP-Lys(L18) induced a miosis (rabbits) at doses of 13 micrograms/kg s.c. and greater. It did not affect norepinephrine-induced pressor and acetylcholine-induced depressor responses (dogs) and contraction of the nictitating membrane induced by electrical stimulation (cats) at a dose of 0.4 mg/kg i.v. 4. Smooth muscles: In the experiments using the isolated ileum, vas deferens, trachea (guinea pigs) and uterus (rats), MDP-Lys(L18) showed neither spasmogenic nor spasmolytic activity at a concentration of 4 x 10(-6) g/ml. Gastrointestinal propulsion (mice), gastric mucosa, gastric emptying rate and gastric secretion (rats) were not affected by this drug at a dose of 0.4 mg/kg s.c. MDP-Lys(L18) did not influence gastrointestinal motility (dogs) at a dose of 0.4 mg/kg, i.v. 5. Miscellaneous: MDP(L-18) suppressed carrageenan-induced edema (rats) at doses of 0.13 mg/kg s.c. and greater.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

研究了N2-[(N-乙酰基-胞壁酰基)-L-丙氨酰-D-异谷氨酰胺基]-N6-硬脂酰-L-赖氨酸MDP-Lys(L18,mur octasin)的一般药理作用,获得以下结果。1. 中枢神经系统:MDP-Lys(L18)在皮下注射剂量为0.4mg/kg时,对行为、自发运动活动、电休克和化学休克诱发的惊厥、己巴比妥睡眠时间、痛阈(小鼠)、条件回避反应(大鼠)均无影响;静脉注射剂量为0.4mg/kg时,对脑电图及脊髓反射(猫)也无影响。皮下注射剂量为13μg/kg及以上时,可使体温显著升高(兔)。2. 呼吸和心血管系统(犬):静脉注射剂量为0.4mg/kg时,MDP-Lys(L18)对呼吸和心血管功能无显著影响。3. 自主神经系统:皮下注射剂量为13μg/kg及以上时,MDP-Lys(L18)可引起瞳孔缩小(兔)。静脉注射剂量为0.4mg/kg时,对去甲肾上腺素引起的升压反应和乙酰胆碱引起的降压反应(犬)以及电刺激诱发的瞬膜收缩(猫)均无影响。4. 平滑肌:在使用离体回肠、输精管、气管(豚鼠)和子宫(大鼠)的实验中,浓度为4×10(-6)g/ml时,MDP-Lys(L18)既无致痉活性也无解痉活性。皮下注射剂量为0.4mg/kg时,该药物对胃肠推进(小鼠)、胃黏膜、胃排空率和胃分泌(大鼠)均无影响。静脉注射剂量为0.4mg/kg时,MDP-Lys(L18)对胃肠蠕动(犬)无影响。5. 其他:皮下注射剂量为0.13mg/kg及以上时,MDP(L-18)可抑制角叉菜胶诱导的水肿(大鼠)。(摘要截短至250字)

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