趙国举, 趙嬌玲, 胡崇家. 力可拉明与加兰他明对胆碱反应系统的影响J. 药学学报, 1965, 12(1): 36-44.
引用本文: 趙国举, 趙嬌玲, 胡崇家. 力可拉明与加兰他明对胆碱反应系统的影响J. 药学学报, 1965, 12(1): 36-44.
CHAO KUO-CHUE, CHAO JIAO-LING AND Hu CHUNG-CHIA, . THE EFFECT OF GALANTHAMINE AND LYCORAMINE ON THE CHOLINE REACTIVE SYSTEMJ. Acta Pharmaceutica Sinica, 1965, 12(1): 36-44.
Citation: CHAO KUO-CHUE, CHAO JIAO-LING AND Hu CHUNG-CHIA, . THE EFFECT OF GALANTHAMINE AND LYCORAMINE ON THE CHOLINE REACTIVE SYSTEMJ. Acta Pharmaceutica Sinica, 1965, 12(1): 36-44.

力可拉明与加兰他明对胆碱反应系统的影响

THE EFFECT OF GALANTHAMINE AND LYCORAMINE ON THE CHOLINE REACTIVE SYSTEM

  • 摘要: 力可拉明与加兰他明系由紫花石蒜及臭水仙中提得,本文报导了它们的碘甲烷盐对胆碱反应系统的影响.力可拉明与加兰他明静脉注射于家兔及猫引起血压下降、肠张力及蠕动加强,可为阿托品对抗.其0.5%的溶液不同程度地收缩家兔的瞳孔.较高浓度的加兰他明(1×10-6克/毫升)与力可拉明(1×10-5克/毫升)可使离体豚鼠迴肠收缩,较低浓度加强乙酰胆碱、氯化钡与组织胺对肠段的收缩作用,对M-胆碱反应系统的作用加兰他明比力可拉明大5-10倍.在水蛭背肌及蛙腹直肌标本上,证明加兰他明加强乙酰胆碱的作用稍大于力可拉明.在猫与大白鼠的试验证明该二药加强了刺激神经所致的腓肠肌收缩作用,对大白鼠坐骨神经-腓肠肌标本的作用与刺激频率及剂量有关,高频(25-100次/秒)和大剂量引起肌缩抑制者较多,而低频(5-10次/秒)和小剂量绝大多数引起肌缩加强.加兰他明比力可拉明作用约大5倍.如预先用阿托品处理,大量乙酰胆碱引起的肌缩抑制,加兰他明与力可拉明均可使之加强.加兰他明、力可拉明和新斯的明可对抗箭毒所引起的肌肉松弛,但对琥珀酰胆碱则反加重.加兰他明与力可拉明类似新斯的明能对抗TEA,C6所致的神经节阻断,亦能加强电刺激交感节前纤维所致的瞬膜收缩.力可拉明的中枢M-与N-胆碱反应系统的兴奋作用较明显,而加兰他明则较弱.静脉注射加兰他明、力可拉明与新斯的明对小白鼠的LD50分别为0.958,16.65,0.174毫克/公斤,中毒症状为流涎、震颤、抽搐,动物死于呼吸麻痹.

     

    Abstract: The cholinergic effect of the methiodides of galanthamine and lycoramine, two alko- loids extracted from Lycoris sqamigera Maxim. and Narcissus papyraceus Ker-Gawl, was studied. Given intravenously, lycoramine and galanthamine caused, in rabbits and cats, a fall of blood pressure as well as an increase of the tonus and peristalsis of intestine. These responses could be antagonized by atropine. Solutions of galanthamine and lycora- mine (both 0.5%) caused contraction of the pupil of rabbits to a variable extent. Galanthamine (1×10-6g/c.c.) and lycoramine (1×10-5g/c.c.) produced contraction of iso- lated guinea-pig ileum and still lower concentrations of both preparations increased the contraction induced by acetylcholine, BaCl2,and histamine. The effect of galanthamine on the M-choline reactive system was 5-10 times stronger than that of lycoramine. It was shown that galanthamine and lycoramine increased the response caused by acetylcholine in the frog rectus and the leech dorsal-muscle, the effect of galanthamine being slightly stronger than lycoramine. In cats and rats, the two drugs caused an in- crease of contracting response of gastrocnemius muscle to nerve stimulation. The effect of galanthamine and lycoramine on the nervemuscle preparations was concerned with stimulating frequencies and doses. Higher frequencies (25-100/sec) and larger doses caused, in many instances, depression of muscle contration; but lower frequencies (5-10/ sec) and smaller doses produced, in most instances, muscle contraction. The effect of galanthamine was 5 times stronger than that of lycoramine. After treatment with atro- pine, the cholinesterase inhibitors, galanthamine, and lycoramine were found to increase the depression of muscle contraction induced by acetylcholine in large doses. Galan- thamine, lycoramine, and neostigmine antagonized muscle paralysis induced by d-tubo- curarine, but not by succinylcholine. Like neostigmine, galanthamine and lycoramine antagonized the ganglionic blockade produced by TEA and C6, and also increased the contraction response of nictitating mem- brane to nerve stimulation. The stimulating effect of lycoramine on the central M- and N-choline reactive system was stronger than that of galanthamine, In mice, the LD50 of galanthamine, lycoramine, and neostigmine were found to be 0.958, 16.65, 0,174 mg/kg respectively. The usual toxic symptoms were: salivation, twitching, and convulsion. The animals died usually of respiratory paralysis.

     

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