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.
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
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Neuropharmacology. 1980 Jan;19(1):39-45. doi: 10.1016/0028-3908(80)90164-1.
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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.
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Neuropharmacology. 1983 Feb;22(2):157-64. doi: 10.1016/0028-3908(83)90003-5.
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