Quisqualamine (original) (raw)
奎可拉明(英語:Quisqualamine)是使君子氨酸的α-脱羧衍生物,以及神经递质谷氨酸和γ-氨基丁酸(GABA)的相关配体。神经兴奋性氨基酸α-脱羧可以产生具有抑制作用的衍生物。因此,与使君子氨酸不同,奎可拉明具有中枢抑制性和神经保护性,并且其作用似乎主要作为GABAA型受体激动剂,并且作为甘氨酸受体的激动剂具有较小程度作用,导致其作用在体外被GABAA拮抗剂如和以及如士的宁所抑制。Mg2 +和,NMDA受体阻滞剂,AMPA和拮抗剂,以及拮抗剂不影响奎可拉明的体外作用,表明它以任何方式不会直接影响离子型谷氨酸受体或GABAB受体。它是否与任何代谢型谷氨酸受体结合并发挥作用尚不清楚。
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dbo:abstract | Quisqualamine is the α-decarboxylated analogue of quisqualic acid, as well as a relative of the neurotransmitters glutamate and γ-aminobutyric acid (GABA). α-Decarboxylation of excitatory amino acids can produce derivatives with inhibitory effects. Indeed, unlike quisqualic acid, quisqualamine has central depressant and neuroprotective properties and appears to act predominantly as an agonist of the GABAA receptor and also to a lesser extent as an agonist of the glycine receptor, due to the facts that its actions are inhibited in vitro by GABAA antagonists like bicuculline and picrotoxin and by the glycine antagonist strychnine, respectively. Mg2+ and , NMDA receptor blockers, CNQX, an antagonist of both the AMPA and kainate receptors, and , a GABAB receptor antagonist, do not affect quisqualamine's actions in vitro, suggesting that it does not directly affect the ionotropic glutamate receptors or the GABAB receptor in any way. Whether it binds to and acts upon any of the metabotropic glutamate receptors like its analogue quisqualic acid however is unclear. (en) 奎可拉明(英語:Quisqualamine)是使君子氨酸的α-脱羧衍生物,以及神经递质谷氨酸和γ-氨基丁酸(GABA)的相关配体。神经兴奋性氨基酸α-脱羧可以产生具有抑制作用的衍生物。因此,与使君子氨酸不同,奎可拉明具有中枢抑制性和神经保护性,并且其作用似乎主要作为GABAA型受体激动剂,并且作为甘氨酸受体的激动剂具有较小程度作用,导致其作用在体外被GABAA拮抗剂如和以及如士的宁所抑制。Mg2 +和,NMDA受体阻滞剂,AMPA和拮抗剂,以及拮抗剂不影响奎可拉明的体外作用,表明它以任何方式不会直接影响离子型谷氨酸受体或GABAB受体。它是否与任何代谢型谷氨酸受体结合并发挥作用尚不清楚。 (zh) |
dbo:iupacName | 2-(2-aminoethyl)-1,2,4-oxadiazolidine-3,5-dione (en) |
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gold:hypernym | dbr:Analogue |
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rdfs:comment | 奎可拉明(英語:Quisqualamine)是使君子氨酸的α-脱羧衍生物,以及神经递质谷氨酸和γ-氨基丁酸(GABA)的相关配体。神经兴奋性氨基酸α-脱羧可以产生具有抑制作用的衍生物。因此,与使君子氨酸不同,奎可拉明具有中枢抑制性和神经保护性,并且其作用似乎主要作为GABAA型受体激动剂,并且作为甘氨酸受体的激动剂具有较小程度作用,导致其作用在体外被GABAA拮抗剂如和以及如士的宁所抑制。Mg2 +和,NMDA受体阻滞剂,AMPA和拮抗剂,以及拮抗剂不影响奎可拉明的体外作用,表明它以任何方式不会直接影响离子型谷氨酸受体或GABAB受体。它是否与任何代谢型谷氨酸受体结合并发挥作用尚不清楚。 (zh) Quisqualamine is the α-decarboxylated analogue of quisqualic acid, as well as a relative of the neurotransmitters glutamate and γ-aminobutyric acid (GABA). α-Decarboxylation of excitatory amino acids can produce derivatives with inhibitory effects. Indeed, unlike quisqualic acid, quisqualamine has central depressant and neuroprotective properties and appears to act predominantly as an agonist of the GABAA receptor and also to a lesser extent as an agonist of the glycine receptor, due to the facts that its actions are inhibited in vitro by GABAA antagonists like bicuculline and picrotoxin and by the glycine antagonist strychnine, respectively. Mg2+ and , NMDA receptor blockers, CNQX, an antagonist of both the AMPA and kainate receptors, and , a GABAB receptor antagonist, do not affect quisq (en) |
rdfs:label | Quisqualamine (en) 奎可拉明 (zh) |
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is foaf:primaryTopic of | wikipedia-en:Quisqualamine |