A METHOD FOR ASSESSING EFFECTS OF DRUGS ON CENTRAL ACTIONS OF 5-HYDROXYTRYPTAMINE

A METHOD FOR ASSESSING EFFECTS OF DRUGS ON CENTRAL ACTIONS OF 5-HYDROXYTRYPTAMINE
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DOI:
10.1111/j.1476-5381.1963.tb01302.x
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发表时间:
1963-01-01
期刊:
BRITISH JOURNAL OF PHARMACOLOGY AND CHEMOTHERAPY
影响因子:
--
通讯作者:
PICKERING, RW
PICKERING, RW
中科院分区:
其他
文献类型:
--
作者:
CORNE, SJ;WARNER, BT;PICKERING, RW

文献摘要

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向小鼠体内注射5-羟色氨酸会产生一种特有的头部抽动。在给定的观察期内,这种反应可以通过观察至少出现一次头部抽动的小鼠的比例(量化反应)或通过计算每只小鼠的头部抽动次数(分级反应)来定量评估。描述了一种基于量子响应来研究中心作用化合物对头部抽动反应的影响的方法。有证据表明,头部抽动是由于5-羟色氨酸脱羧基形成的5-羟色胺的中枢作用。单胺氧化酶抑制剂和苯妥英钠可增强头部抽动。被测试的拮抗剂包括脱羧酶抑制剂、5-羟色胺拮抗剂、一些抗组胺药、主要镇静剂以及止痛和拟交感药物。既不能增强也不能抑制这种反应的药物包括巴比妥酸盐和小剂量镇静剂。这种方法在可能具有中心作用的化合物的初步检查中可能是有价值的。
Injection of 5-hydroxytryptophan into mice produces a characteristic head-twitch. For a given period of observation this response may be assessed quantitatively either by observing the proportion of mice showing at least one head-twitch (a quantal response) or by counting the number of head-twitches for each mouse ( a graded response). A method, based on the quantal response, of investigating the effect of centrally acting compounds on the head-twitch response is described. Evidence is presented that the head-twitches are due to a central action of 5-hydroxytryptamine formed by decarboxylation of 5-hydroxytryptophan. Head-twitches are potentiated by monoamine oxidase inhibitors by phenytoin. Antagonists tested include an inhibitor of decarboxylase, antagonists of 5-hydroxytryptamine, some antihista-mines, major tranquillizers and analgesic and sympathomimetic drugs. Drugs which neither potentiate nor inhibit the response include barbiturates and minor tranquillizers. The method may be valuable in the preliminary examination of compounds likely to have a central action.