蜘蛛毒素argiotoxin636与N-甲基-D-天冬氨酸受体复合物上的一个Mg2+位点结合。
The spider toxin, argiotoxin636, binds to a Mg2+ site on the N-methyl-D-aspartate receptor complex.
作者信息
Reynolds I J
机构信息
Department of Pharmacology, University of Pittsburgh, PA 15261.
出版信息
Br J Pharmacol. 1991 Jun;103(2):1373-6. doi: 10.1111/j.1476-5381.1991.tb09796.x.
Abstract
- The mechanism of action of the arylalkylamine spider toxin, argiotoxin636, on the N-methyl-D-aspartate (NMDA) receptor was investigated by use of [3H]-dizocilpine binding to well-washed membranes obtained from rat brain. 2. Argiotoxin636 decreased [3H]-dizocilpine binding with an apparent potency of about 3 microM. The inhibition of [3H]-dizocilpine by argiotoxin636 was insensitive to the concentration of glutamate, glycine and spermidine in the assay. 3. Argiotoxin636 alone had no effect on the dissociation of [3H]-dizocilpine. However, argiotoxin636 reversed the actions of Mg2+ on the dissociation of [3H]-dizocilpine by decreasing the apparent potency of Mg2+. Argiotoxin636 also reversed the action of Ca2+ on the dissociation of [3H]-dizocilpine. 4. These results suggest that argiotoxin636 exerts a novel inhibitory effect on the NMDA receptor complex by binding to one of the Mg2+ sites located within the NMDA-operated ion channel.
摘要
- 通过使用[3H] - 地佐环平与从大鼠脑获得的充分洗涤的膜结合，研究了芳基烷基胺蜘蛛毒素argiotoxin636对N - 甲基 - D - 天冬氨酸（NMDA）受体的作用机制。2. Argiotoxin636降低[3H] - 地佐环平结合，其表观效力约为3 microM。在测定中，argiotoxin636对[3H] - 地佐环平的抑制作用对谷氨酸、甘氨酸和亚精胺的浓度不敏感。3. 单独的argiotoxin636对[3H] - 地佐环平的解离没有影响。然而，argiotoxin636通过降低Mg2 +的表观效力来逆转Mg2 +对[3H] - 地佐环平解离的作用。Argiotoxin636也逆转Ca2 +对[3H] - 地佐环平解离的作用。4. 这些结果表明，argiotoxin636通过与位于NMDA操作离子通道内的Mg2 +位点之一结合，对NMDA受体复合物发挥新的抑制作用。
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本文引用的文献
1
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Nature. 1984;309(5965):261-3. doi: 10.1038/309261a0.
2
Magnesium gates glutamate-activated channels in mouse central neurones.镁离子控制小鼠中枢神经元中谷氨酸激活的通道。
Nature. 1984;307(5950):462-5. doi: 10.1038/307462a0.
3
Structures and biological activities of three synaptic antagonists from orb weaver spider venom.圆蛛毒液中三种突触拮抗剂的结构与生物活性
Biochem Biophys Res Commun. 1987 Oct 29;148(2):678-83. doi: 10.1016/0006-291x(87)90930-2.
4
Pharmacology of the glutamate receptor.
Prog Neurobiol. 1988;30(5):399-435. doi: 10.1016/0301-0082(88)90009-3.
5
Spider toxin blocks excitatory amino acid responses in isolated hippocampal pyramidal neurons.蜘蛛毒素可阻断离体海马锥体神经元中兴奋性氨基酸反应。
Neurosci Lett. 1987 Aug 31;79(3):326-30. doi: 10.1016/0304-3940(87)90453-8.
6
The novel anticonvulsant MK-801 binds to the activated state of the N-methyl-D-aspartate receptor in rat brain.新型抗惊厥药MK-801与大鼠脑中N-甲基-D-天冬氨酸受体的激活状态相结合。
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7
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Brain Res. 1985 Nov 4;346(2):397-9. doi: 10.1016/0006-8993(85)90878-9.
8
9
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10
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