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苯二氮䓬受体配体对印防己毒素和戊四氮诱发癫痫发作的双向作用。

Bidirectional effects of benzodiazepine receptor ligands against picrotoxin- and pentylenetetrazol-induced seizures.

作者信息

Jensen L H, Petersen E N

出版信息

J Neural Transm. 1983;58(3-4):183-91. doi: 10.1007/BF01252804.

DOI:10.1007/BF01252804
PMID:6319592
Abstract

The dose response curves of picrotoxin-induced seizures and pentylenetetrazol-induced seizures were shifted to the right by the benzodiazepine (BZ) receptor agonist lorazepam, and to the left by the inverse agonists, DMCM, ZK 90886, FG 7142 and CGS 8216. The BZ receptor antagonists ZK 93426 and Ro 15-1788 had no effect on the dose response curves. The anticonvulsive action of lorazepam and the proconvulsive action of DMCM against picrotoxin-induced seizures and against pentylenetetrazol-induced seizures was inhibited by low doses of ZK 93426 and Ro 15-1788. These results indicate that the bidirectional effects of benzodiazepine receptor ligands on picrotoxin and pentylenetetrazol induced seizures is actually mediated through benzodiazepine receptors.

摘要

印防己毒素诱发癫痫和戊四氮诱发癫痫的剂量反应曲线,被苯二氮䓬(BZ)受体激动剂劳拉西泮向右移动,而被反向激动剂DMCM、ZK 90886、FG 7142和CGS 8216向左移动。BZ受体拮抗剂ZK 93426和Ro 15 - 1788对剂量反应曲线无影响。低剂量的ZK 93426和Ro 15 - 1788可抑制劳拉西泮的抗惊厥作用以及DMCM对印防己毒素诱发癫痫和戊四氮诱发癫痫的促惊厥作用。这些结果表明,苯二氮䓬受体配体对印防己毒素和戊四氮诱发癫痫的双向作用实际上是通过苯二氮䓬受体介导的。

相似文献

1
Bidirectional effects of benzodiazepine receptor ligands against picrotoxin- and pentylenetetrazol-induced seizures.苯二氮䓬受体配体对印防己毒素和戊四氮诱发癫痫发作的双向作用。
J Neural Transm. 1983;58(3-4):183-91. doi: 10.1007/BF01252804.
2
DMCM: a potent convulsive benzodiazepine receptor ligand.DMCM:一种强效的惊厥性苯二氮䓬受体配体。
Eur J Pharmacol. 1983 Oct 14;94(1-2):117-24. doi: 10.1016/0014-2999(83)90448-x.
3
Chronic treatment with lorazepam and FG 7142 may change the effects of benzodiazepine receptor agonists, antagonists and inverse agonists by different mechanisms.长期使用劳拉西泮和FG 7142可能通过不同机制改变苯二氮䓬受体激动剂、拮抗剂和反向激动剂的作用。
Eur J Pharmacol. 1987 Jan 20;133(3):309-17. doi: 10.1016/0014-2999(87)90027-6.
4
Audiogenic seizures in DBA/2 mice discriminate sensitively between low efficacy benzodiazepine receptor agonists and inverse agonists.DBA/2小鼠的听源性惊厥能灵敏地区分低效苯二氮䓬受体激动剂和反向激动剂。
Life Sci. 1983 Jul 25;33(4):393-9. doi: 10.1016/s0024-3205(83)80014-9.
5
Lorazepam and FG 7142 induce tolerance to the DMCM antagonistic effect of benzodiazepine receptor ligands.
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6
Evaluation of the beta-carboline ZK 93 426 as a benzodiazepine receptor antagonist.β-咔啉ZK 93426作为苯二氮䓬受体拮抗剂的评估。
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On the convulsant action of Ro 5-4864 and the existence of a micromolar benzodiazepine binding site in rat brain.关于Ro 5-4864的惊厥作用以及大鼠脑中微摩尔级苯二氮䓬结合位点的存在
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A benzodiazepine antagonist action of CL 218,872.
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Modification of seizures elicited by the benzodiazepine Ro 5-3663--a comparison with picrotoxin.苯二氮䓬Ro 5-3663引发的癫痫发作的改变——与印防己毒素的比较。
J Pharm Pharmacol. 1984 Dec;36(12):837-40. doi: 10.1111/j.2042-7158.1984.tb04888.x.
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A partial agonist at the anticonvulsant benzodiazepine receptor: reversal of the anticonvulsant effects of Ro 15-1788 with CGS-8216.抗惊厥苯二氮䓬受体的部分激动剂:CGS - 8216对Ro 15 - 1788抗惊厥作用的逆转。
Brain Res. 1984 Jan 23;291(2):388-90. doi: 10.1016/0006-8993(84)91275-7.

引用本文的文献

1
Evaluation of the beta-carboline ZK 93 426 as a benzodiazepine receptor antagonist.β-咔啉ZK 93426作为苯二氮䓬受体拮抗剂的评估。
Psychopharmacology (Berl). 1984;83(3):249-56. doi: 10.1007/BF00464789.
2
Benzodiazepine ligands, nociception and 'defeat' analgesia in male mice.
Psychopharmacology (Berl). 1987;91(3):305-15. doi: 10.1007/BF00518182.
3
Intrinsic actions of the benzodiazepine receptor antagonist Ro 15-1788.苯二氮䓬受体拮抗剂Ro 15 - 1788的内在作用。
Psychopharmacology (Berl). 1986;88(1):1-11. doi: 10.1007/BF00310505.

本文引用的文献

1
A simplified method of evaluating dose-effect experiments.一种评估剂量效应实验的简化方法。
J Pharmacol Exp Ther. 1949 Jun;96(2):99-113.
2
Methyl-beta-carboline-induced convulsions are antagonized by Ro 15-1788 and by propyl-beta-carboline.Ro 15 - 1788和丙基-β-咔啉可拮抗甲基-β-咔啉诱发的惊厥。
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Behavioural evidence for partial agonist properties of RO 15-1788, a benzodiazepine receptor antagonist.苯二氮䓬受体拮抗剂RO 15 - 1788部分激动剂特性的行为学证据
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Convulsions induced by submaximal dose of pentylenetetrazol in mice are antagonized by the benzodiazepine antagonist Ro 15-1788.苯二氮䓬拮抗剂Ro 15 - 1788可拮抗小鼠中由次最大剂量戊四氮诱导的惊厥。
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Proconvulsant action of CGS 8216.
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7
DMCM: a potent convulsive benzodiazepine receptor ligand.DMCM:一种强效的惊厥性苯二氮䓬受体配体。
Eur J Pharmacol. 1983 Oct 14;94(1-2):117-24. doi: 10.1016/0014-2999(83)90448-x.
8
Audiogenic seizures in DBA/2 mice discriminate sensitively between low efficacy benzodiazepine receptor agonists and inverse agonists.DBA/2小鼠的听源性惊厥能灵敏地区分低效苯二氮䓬受体激动剂和反向激动剂。
Life Sci. 1983 Jul 25;33(4):393-9. doi: 10.1016/s0024-3205(83)80014-9.
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Do benzodiazepine receptors mediate the anticonflict action of pentobarbital?
Life Sci. 1983 May 9;32(19):2241-6. doi: 10.1016/0024-3205(83)90422-8.
10
beta-Carbolines enhance shock-induced suppression of drinking in rats.β-咔啉增强大鼠休克诱导的饮水抑制。
Proc Natl Acad Sci U S A. 1983 Apr;80(7):2072-6. doi: 10.1073/pnas.80.7.2072.