リルゾール

化学名:リルゾール

CAS番号.1744-22-5

英語名:Riluzole

CBNumberCB3353226

MFC8H5F3N2OS

MW234.2

别名

2-アミノ-6-(トリフルオロメトキシ)ベンゾチアゾール

リルゾール

2-アミノ-6(トリフルオロメトキシ)ベンゾチアゾール

リルゾール物理性質

融点	116-118°C
沸点	296.3±50.0 °C(Predicted)
比重(密度)	1.572±0.06 g/cm3(Predicted)
貯蔵温度	2-8°C
溶解性	DMSO：「25」mg/mL
外見	個体
酸解離定数(Pka)	2.96±0.10(Predicted)
色	白い
Merck	14,8223
安定性：	-20°C の DMSO またはエタノール溶液で最大 2 か月間保存できます。
InChI	InChI=1S/C8H5F3N2OS/c9-8(10,11)14-4-1-2-5-6(3-4)15-7(12)13-5/h1-3H,(H2,12,13)
InChIKey	FTALBRSUTCGOEG-UHFFFAOYSA-N
SMILES	S1C2=CC(OC(F)(F)F)=CC=C2N=C1N

安全性情報

主な危険性	T,Xi
Rフレーズ	25
Sフレーズ	45
RIDADR	UN 2811 6.1/PG 3
WGK Germany	3
RTECS 番号	DL2830000
Hazard Note	Irritant
国連危険物分類	6.1
容器等級	II
HSコード	29342000
ストレージクラス	6.1A - Combustible acute toxic Cat. 1 and 2 very toxic hazardous materials
Hazard Classifications	Acute Tox. 2 Oral
毒性	LD50 in mice (mg/kg): 46 i.p.; 67 orally (Mizoule)

危険有害性情報のコード(GHS)

外観
白色～うすい黄色、結晶～結晶性粉末
効能
神経細胞保護薬, グルタミン酸伝達阻害薬
商品名
リルテック (サノフィ)
説明
Rilutek was launched in Germany, the UK and US (orphan drug status) for treatment of amyotrophic lateral sclerosis (ALS) and is the first drug approved for this indication. A one step synthesis from 4-(trifluoromethoxy)aniline provides a supply of the compound. The source of its neuroprotective and anticonvulsant activity is not clearly understood. It antagonizes excitatory amino acids and blocks presynaptic release of glutamate, is an antagonist of NMDA-induced acetylcholine release and inhibited glutamate and quisqualate induced increases in cGMP but does not bind to NMDA or Kainic receptors. Rilutek has no affinity for glutamate, GABAbenzodiazepine, glycine and adenosine receptors. It easily crosses the blood brain barrier and depresses glutamatergic neurotransmission, stabilizes voltagedependent Na channels in their inactive form and activates G-protein dependent processes.
化学的特性
White Crystalline Solid
使用
Labeled Riluzole, intended for use as an internal standard for the quantification of Riluzole by GC- or LC-mass spectrometry.
生物活性
Novel psychotropic agent with anticonvulsant, hypnotic, anxiolytic, anti-ischemic and anesthetic properties. Riluzole is able to act as a glutamate release inhibitor, blocks voltage-dependent Na + channels and inhibits GABA uptake by striatal synaptosomes.

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