4-アミノ-5-ヘキセン酸

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 危険有害性情報

  H225：引火性の高い液体および蒸気

  H370：臓器の障害

• 注意書き

  P210：熱/火花/裸火/高温のもののような着火源から遠ざ けること。－禁煙。

  P260：粉じん/煙/ガス/ミスト/蒸気/スプレーを吸入しないこ と。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P301+P310：飲み込んだ場合：直ちに医師に連絡すること。

  P311：医師に連絡すること。

4-アミノ-5-ヘキセン酸 価格

4-アミノ-5-ヘキセン酸 化学特性,用途語,生産方法

• 効能

  抗けいれん薬, 抗てんかん薬

• 商品名

  サブリル (サノフィ)

• 説明

  Vigabatrin, the gamma-vinyl derivative of GABA, is a new anticonvulsant reportedly effective in the treatment of intractable seizures unresponsive to currently available therapy. Mechanistically vigabatrin is a potent irreversible GABA aminotransferase inhibitor which modifies the enzyme's active-site by Michael addition. Other potential indications have been suggested for vigabatrin, including depression and schizophrenia.

• 化学的特性

  White or almost white powder.

• 使用

  Vigabatrin is a selective GABA transaminase inhibitor.

• 定義

  ChEBI: A gamma-amino acid having a gamma-vinyl GABA structure. It is an irreversible inhibitor of gamma-aminobutyric 664 acid transaminase

• 世界保健機関（WHO）

  Vigabatrin, an irreversible inhibitor of GABA-transaminase was introduced in 1989 as a anticonvulsant for management of epilepsy unresponsive to other antiepilepsy agents. In 1991 it was refused registration in Norway because it induced toxic changes, including microvacuolation in the brain of two animal species, at doses that are close to therapeutic dosage levels in man. It is still marketed in Sweden and the United Kingdom.

• 生物学の機能

  Vigabatrin (Sabril) is a relatively specific irreversible inhibitor of GABA-transaminase (GABA-T), the major enzyme responsible for the metabolism of GABA in the mammalian CNS. As a result of inhibition of GABA-T, there is an increase in the concentration of GABA in the brain and consequently an increase in inhibitory neurotransmission. Vigabatrin is well absorbed orally and is distributed to all body systems.The major route of elimination for vigabatrin is renal excretion of the parent compound; no metabolites have been identified in humans.
  At present, the primary indication for vigabatrin is in the treatment of patients with partial seizures, but it appears to be an effective and generally well tolerated antiepileptic medication for other seizure types as well. It should not be used in patients with absence epilepsy or with myoclonic seizures. Vigabatrin is not approved as an AED in the United States, although it is approved in many other countries.

• 一般的な説明

  Vigabatrin, a 4-vinyl analog of GABA, produces its pharmacologicalaction by irreversibly blocking GABA catabolismcatalyzed by GABA-T as discussed earlier. It is marketedin Europe and Canada as an adjunctive treatment ofpatients with partial seizures, but it has yet to gain FDA approvalin the United States even after extensive clinical trials.The main concern with this drug is its ability to causea reversible visual field defect associated with retinal functionin the eyes.

• 生物活性

  Selective GABA-T inhibitor. Anticonvulsant.

• 合成

  The reaction of 1,4-dichloro-2- butene with diethyl malonate in the presence of sodium ethoxide as catalyst in refluxing ethanol gives 1,1-bis(ethoxycarbonyl)-2-vinylcyclopropane (8), which by reaction with gaseous ammonia in DMF is converted into 3-carboxamido- 5-vinyl-2-pyrrolidone (9). This compound is treated with HCl in refluxing acetic acid to yield vigabatrin.
  

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