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纯氯化毒蕈碱的药理作用。

Pharmacological actions of pure muscarine chloride.

作者信息

FRASER P J

出版信息

Br J Pharmacol Chemother. 1957 Mar;12(1):47-52. doi: 10.1111/j.1476-5381.1957.tb01361.x.

Abstract

The action of chromatographically pure crystalline muscarine chloride, prepared from Amanita muscaria, has been compared with acetylcholine chloride (ACh) on a number of different organs from a variety of species. Muscarine caused spasm in vivo and in vitro of muscles of the gut, uterus, urinary bladder, and bronchus. It also caused contraction of the horse ureter and carotid artery chain in vitro and slowed the isolated auricles of the guinea-pig and rabbit, and the frog heart.Muscarine caused a drop in blood pressure, although in vitro it produced either constriction or dilatation of the blood vessels of the rabbit ear.All these actions resembled those of acetylcholine, though muscarine was usually more potent. Muscarine effects were readily prevented by atropine sulphate. It had a slight action on the frog rectus abdominis muscle, causing a contracture at high concentrations. Muscarine was destroyed neither by pepsin nor by boiling at any pH. It was inactive by mouth in a monkey in a quantity many times that which would cause poisoning by ingestion of Amanita muscaria in the human being. Muscarine neither inhibited nor was hydrolysed by either true- or pseudo-cholinesterase. Muscarine chloride did not cause paralysis of the neuromuscular junctions of the rat diaphragm or of the cat gastrocnemius.

摘要

从毒蝇伞中制备的色谱纯结晶氯化毒蕈碱的作用,已与氯化乙酰胆碱(ACh)在多种物种的一些不同器官上进行了比较。毒蕈碱在体内和体外均可引起肠道、子宫、膀胱和支气管肌肉痉挛。它还能使马输尿管和颈动脉链在体外收缩,并使豚鼠、兔的离体心耳以及蛙心的跳动减慢。毒蕈碱可导致血压下降,尽管在体外它会使兔耳血管出现收缩或扩张。所有这些作用都与乙酰胆碱的作用相似,不过毒蕈碱通常效力更强。硫酸阿托品能轻易地阻止毒蕈碱的作用。它对蛙腹直肌有轻微作用,在高浓度时会引起挛缩。毒蕈碱既不会被胃蛋白酶破坏,也不会在任何pH值下煮沸而被破坏。给猴子口服大量毒蕈碱(该量是人类因摄入毒蝇伞而中毒剂量的许多倍)时,毒蕈碱并无活性。毒蕈碱既不会被真性胆碱酯酶也不会被假性胆碱酯酶抑制或水解。氯化毒蕈碱不会导致大鼠膈肌或猫腓肠肌的神经肌肉接头麻痹。

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