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美《科学》杂志第212卷第4493期(1981年)报道:目前欧洲正对一种强有效的镇痛剂进行临床试验。此镇痛剂与吗啡一样有强烈的止痛作用。但是它通过一种完全不同的机制起作用,并且不会成瘾。以上是此剂的发现人皇家丹麦药学院克罗斯加德-拉森(Poul Krogsgaard-Larsen)在美国化学协会的会议上所作的报告的内容。此化合物在结构上是Muscimol的一种类似物。Muscimol是毒性蘑菇Amarita muscaria的二种活性成分之一。Muscimol本身在结构上和大脑神经介质GABA(γ-氨基丁酸)有关,不过,用于人类时毒性太大。新的制剂tetrahydroisooxazolo-(5,4-c)-pyridine-3-o1(TH1P)是一部分分子结构严密的Muscimol的一种变异体,它在临床研究中显示的毒性非常小。
U.S. Science Volume 212, Issue 4493 (1981): Currently, a clinical trial of a potent analgesic is underway in Europe. This analgesic has the same strong analgesic effect as morphine. But it works through a completely different mechanism and is not addictive. These are the findings of the discovery by Poul Krogsgaard-Larsen at the meeting of the American Chemical Society at the Royal Danish College of Pharmacy. This compound is structurally an analogue of Muscimol. Muscimol is one of two active ingredients of the toxic mushroom Amarita muscaria. Muscimol itself is structurally related to the brain’s neurotransmitter GABA (gamma-aminobutyric acid), but is toxic when used in humans. The new formulation, tetrahydroisooxazolo- (5,4-c) -pyridine-3-o1 (TH1P), is a variant of Muscimol with a very tight molecular structure that shows very little toxicity in clinical studies.