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类固醇衍生物RU5135对抑制性氨基酸的拮抗作用。

Antagonism of inhibitory amino acids by the steroid derivative RU5135.

作者信息

Simmonds M A, Turner J P

出版信息

Br J Pharmacol. 1985 Mar;84(3):631-5. doi: 10.1111/j.1476-5381.1985.tb16143.x.

DOI:10.1111/j.1476-5381.1985.tb16143.x
PMID:3986429
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1987146/
Abstract

The steroid derivative RU5135 has been tested for its ability to antagonize glycine and the gamma-aminobutyric acid (GABA) analogue muscimol on isolated preparations of rat optic nerve and cuneate nucleus, respectively. On the cuneate nucleus, RU5135 antagonized muscimol in a competitive manner with a pA2 value of 8.31. RU5135 shared a common site of action with bicuculline that was separate from the picrotoxin site. On the optic nerve, RU5135 antagonized glycine with a pA2 of 7.67. It shared a common site of action with strychnine.

摘要

已对类固醇衍生物RU5135分别在大鼠视神经和楔状核的离体标本上拮抗甘氨酸和γ-氨基丁酸（GABA）类似物蝇蕈醇的能力进行了测试。在楔状核上，RU5135以竞争性方式拮抗蝇蕈醇，其pA2值为8.31。RU5135与荷包牡丹碱具有共同的作用位点，该位点与印防己毒素位点不同。在视神经上，RU5135以7.67的pA2拮抗甘氨酸。它与士的宁具有共同的作用位点。

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本文引用的文献

1
Evidence that bicuculline and picrotoxin act at separate sites to antagonize gamma-aminobutyric acid in rat cuneate nucleus.荷包牡丹碱和印防己毒素在大鼠楔状核中作用于不同位点以拮抗γ-氨基丁酸的证据。
Neuropharmacology. 1980 Jan;19(1):39-45. doi: 10.1016/0028-3908(80)90164-1.
2
Depolarizing responses to glycine, beta-alanine and muscimol in isolated optic nerve and cuneate nucleus.离体视神经和楔束核中对甘氨酸、β-丙氨酸和蝇蕈醇的去极化反应。
Br J Pharmacol. 1983 Jul;79(3):799-806. doi: 10.1111/j.1476-5381.1983.tb10018.x.
3
Regular and lasting neocortical spiking produced by systemic administration of a steroid derivative in the rat.通过对大鼠全身给药一种类固醇衍生物产生规律且持久的新皮质放电。
Neuropharmacology. 1983 Feb;22(2):157-64. doi: 10.1016/0028-3908(83)90003-5.
4
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.
5
A steroid derivative, R 5135, antagonizes the GABA/benzodiazepine receptor interaction.一种类固醇衍生物R 5135可拮抗γ-氨基丁酸/苯二氮䓬受体相互作用。
Neuropharmacology. 1981 Apr;20(4):357-61. doi: 10.1016/0028-3908(81)90009-5.
6
Presynaptic actions of gamma-aminobutyric acid and some antagonists in a slice preparation of cuneate nucleus.γ-氨基丁酸及某些拮抗剂在楔状核脑片制备中的突触前作用
Br J Pharmacol. 1978 Jul;63(3):495-502. doi: 10.1111/j.1476-5381.1978.tb07803.x.