咪唑二氮䓬Ro 15-4513与化学惊厥剂的相互作用。
Interactions of the imidazodiazepine Ro 15-4513 with chemical convulsants.
作者信息
Lister R G, Nutt D J
机构信息
Laboratory of Clinical Studies, DICBR, NIAAA, Bethesda, MD 20892.
出版信息
Br J Pharmacol. 1988 Jan;93(1):210-4. doi: 10.1111/j.1476-5381.1988.tb11423.x.
Abstract
- The proconvulsant effects of the imidazodiazepine Ro 15-4513, were investigated in mice by use of intravenous infusion of a variety of convulsant drugs. 2. Dose-response and time course studies of Ro 15-4513 against gamma-aminobutyric acid (GABA) antagonists were performed. On the basis of these studies a maximally effective dose of 5 mg kg-1 was administered 5 min before the determination of seizure thresholds in subsequent experiments. 3. Ro 15-4513 (5 mg kg-1) significantly lowered seizure thresholds to pentylenetetrazole, bicuculline and the convulsant benzodiazepine Ro 5-3663, but failed to alter seizure thresholds to picrotoxin, strychnine, caffeine and quipazine. 4. Ro 15-4513 significantly raised seizure threshold to the benzodiazepine receptor inverse agonist methyl 6,7-dimethoxy-4 ethyl-beta-carboline-3-carboxylate (DMCM). 5. These results are discussed in relation to other studies investigating the proconvulsant and alcohol-antagonizing effects of Ro 15-4513.
摘要
- 通过静脉输注多种惊厥药物，研究了咪唑二氮䓬Ro 15 - 4513对小鼠的惊厥前效应。2. 进行了Ro 15 - 4513对抗γ-氨基丁酸（GABA）拮抗剂的剂量反应和时间进程研究。基于这些研究，在随后的实验中，在测定癫痫发作阈值前5分钟给予5 mg kg-1的最大有效剂量。3. Ro 15 - 4513（5 mg kg-1）显著降低了对戊四氮、荷包牡丹碱和惊厥性苯二氮䓬Ro 5 - 3663的癫痫发作阈值，但未能改变对印防己毒素、士的宁、咖啡因和喹哌嗪的癫痫发作阈值。4. Ro 15 - 4513显著提高了对苯二氮䓬受体反向激动剂6,7 - 二甲氧基 - 4 - 乙基 - β-咔啉 - 3 - 羧酸甲酯（DMCM）的癫痫发作阈值。5. 结合其他研究Ro 15 - 4513的惊厥前效应和抗酒精作用的研究对这些结果进行了讨论。
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本文引用的文献
1
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Neuropharmacology. 1980 Oct;19(10):1017-23. doi: 10.1016/0028-3908(80)90014-3.
2
Binding characteristics and interactions of depressant drugs with [35S]t-butylbicyclophosphorothionate, a ligand that binds to the picrotoxinin site.
J Neurochem. 1984 Jan;42(1):221-9. doi: 10.1111/j.1471-4159.1984.tb09721.x.
3
Antagonism of caffeine-induced seizures in mice by Ro15-1788.Ro15 - 1788对咖啡因诱导的小鼠癫痫发作的拮抗作用。
Eur J Pharmacol. 1984 Jan 27;97(3-4):289-93. doi: 10.1016/0014-2999(84)90462-x.
4
Pharmacokinetic studies on Ro 15-1788, a benzodiazepine receptor ligand, in the brain of the rat.对苯二氮䓬受体配体Ro 15 - 1788在大鼠脑中的药代动力学研究。
Brain Res. 1984 Jan 2;290(1):183-6. doi: 10.1016/0006-8993(84)90752-2.
5
The picrotoxin-like action of a convulsant benzodiazepine, Ro5-3663.一种惊厥性苯二氮䓬Ro5-3663的印防己毒素样作用。
Eur J Pharmacol. 1983 Jan 28;87(1):155-8. doi: 10.1016/0014-2999(83)90064-x.
6
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Psychopharmacology (Berl). 1982;78(3):293-5. doi: 10.1007/BF00428169.
7
Classification of some GABA antagonists with regard to site of action and potency in slices of rat cuneate nucleus.一些γ-氨基丁酸拮抗剂在大鼠楔束核切片中的作用位点及效能分类
Eur J Pharmacol. 1982 Jun 4;80(4):347-58. doi: 10.1016/0014-2999(82)90080-2.
8
Adenosine receptors and behavioral actions of methylxanthines.腺苷受体与甲基黄嘌呤的行为作用
Proc Natl Acad Sci U S A. 1981 May;78(5):3260-4. doi: 10.1073/pnas.78.5.3260.
9
GABA-benzodiazepine-barbiturate receptor interactions.γ-氨基丁酸-苯二氮䓬-巴比妥酸盐受体相互作用
J Neurochem. 1981 Jul;37(1):1-13. doi: 10.1111/j.1471-4159.1981.tb05284.x.
10
Studies on the post-ictal rise in seizure threshold.
Eur J Pharmacol. 1981 May 8;71(2-3):287-95. doi: 10.1016/0014-2999(81)90031-5.
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