(3S)-3-amino-1-hydroxy-1,2,3,4-tetrahydroquinolin-2-one

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

  H315：皮膚刺激

  H319：強い眼刺激

  H332：吸入すると有害

  H335：呼吸器への刺激のおそれ

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

(3S)-3-amino-1-hydroxy-1,2,3,4-tetrahydroquinolin-2-one 化学特性,用途語,生産方法

• 酵素阻害剤

  This systemically available KAT II inhibitor (FW = 178.19 g/mol; CAS 34783-48-7; IUPAC: (3S)-3-amino-1-hydroxy-3,4-dihydroquinolin-2(1H)- one) irreversibly inhibits kynurenine amino transferase II, or KAT II, with Ki = 23 nM, kinact/Ki 112,000 M–1 s –1 , IC50 = 263 nM, and PartitionCoefficientn-octanol/H2O = 3 x 108. This inhibitor most likely makes an enamine adduct with enzyme-bound pyridoxal-P. Rationale: Kynurenate is a tryptophan-derived endogenous antagonist for glutamate and a7-nicotinic acetylcholine receptors in the brain. Increased levels are observed postmortem in the brains of patients with a range of neurocognitive disorders, including schizophrenia. Kynurenate may well contribute to the cognitive symptoms of these conditions. Pharmacology: PF-04859989 restores glutamate release "transients" evoked by ejections of nicotine into the prefrontal cortex of rats exhibiting elevated kynurenate levels. Systemic administration of PF-04859989 30 min prior to administration of Lkynurenine (but not when administered 30 min after L-kynurenine) restores glutamatergic transients recorded up to 120 min after the administration of the KAT II inhibitor. Furthermore, the KAT-II inhibitor significantly reverses L-kynurenine-induced elevations of brain KYNA levels. The KATII inhibitor does not affect nicotine-evoked glutamatergic transients in rats not pre-treated with L-kynurenine

(3S)-3-amino-1-hydroxy-1,2,3,4-tetrahydroquinolin-2-one 生産企業

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