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Bicuculline is a phthalide-isoquinoline compound that is a light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungosa, and several Corydalis species (all in subfamily Fumarioideae, previously known as family Fumariaceae). Since it blocks the inhibitory action of GABA receptors, the action of bicuculline mimics epilepsy; it also causes convulsions. This property is utilized in laboratories around the world in the in vitro study of epilepsy, generally in hippocampal or cortical neurons in prepared brain slices from rodents. This compound is also routinely used to isolate glutamatergic (excitatory amino acid) receptor function.

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  • Bicucullin (de)
  • Bicuculline (en)
  • Bicucullina (it)
  • ビククリン (ja)
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  • Bicucullin ist ein Alkaloid und ein potenter, selektiver und kompetitiver GABAA-Rezeptor-Antagonist. (de)
  • La bicucullina è una sostanza organica identificata nel 1932 in un estratto di Dicentra cucullaria. È un antagonista del recettore GABA A (si lega alla subunità β). (it)
  • ビククリン(Bicuculline)は、フタリド-イソキノリン化合物であり、GABAA受容体の光感受性競合阻害薬である。1932年に植物のアルカロイド抽出物から同定された。Dicentra cucullaria、Adlumia fungosa、キケマン属の数種(いずれもケマンソウ亜科)から単離されている。 リガンド依存性のイオンチャネル型GABAA受容体は塩化物イオンを神経細胞内に流入させ活動を抑制するもので、ベンゾジアゼピン系抗不安薬の主要な標的ともなる。ビククリンは主にこの受容体を阻害し、てんかんに類似した作用や痙攣を引き起こす。この特性のため、世界中の研究室で齧歯類の脳切片(海馬や大脳皮質)などの神経細胞を用いたてんかんのin vitro 研究に利用されている。また、グルタミン酸受容体の機能を薬理学的に分離するためにも日常的に使用されている。 GABAA受容体に対する半数阻害濃度(IC50)は3μMである。ビククリンに対する感受性は、ではGABAA受容体の定義における主要な基準として定義されている。 を遮断する目的でも使用される。 (ja)
  • Bicuculline is a phthalide-isoquinoline compound that is a light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungosa, and several Corydalis species (all in subfamily Fumarioideae, previously known as family Fumariaceae). Since it blocks the inhibitory action of GABA receptors, the action of bicuculline mimics epilepsy; it also causes convulsions. This property is utilized in laboratories around the world in the in vitro study of epilepsy, generally in hippocampal or cortical neurons in prepared brain slices from rodents. This compound is also routinely used to isolate glutamatergic (excitatory amino acid) receptor function. (en)
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