(2-ベンジルピペリジノ)[4-(2′-メトキシビフェニル-4-イル)-1H-1,2,3-トリアゾール-1-イル]ケトン

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

• 注意書き

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P270：この製品を使用する時に、飲食または喫煙をしないこ と。

  P301+P312：飲み込んだ場合：気分が悪い時は医師に連絡する こと。

  P330：口をすすぐこと。

  P501：内容物/容器を．．．に廃棄すること。

(2-ベンジルピペリジノ)[4-(2′-メトキシビフェニル-4-イル)-1H-1,2,3-トリアゾール-1-イル]ケトン 価格

(2-ベンジルピペリジノ)[4-(2′-メトキシビフェニル-4-イル)-1H-1,2,3-トリアゾール-1-イル]ケトン 化学特性,用途語,生産方法

• 使用

  Endocannabinoids such as 2-arachidonoyl glycerol (2-AG; ) and arachidonoyl ethanolamide (AEA; ) are biologically active lipids that are involved in a number of synaptic processes including activation of cannabinoid receptors. Monoacylglycerol lipase (MAGL) is a serine hydrolase responsible for the hydrolysis of 2-AG to arachidonic acid and glycerol, thus terminating its biological function. MJN110 is an N-hydroxysuccinimidyl carbamate that inhibits MAGL (IC50 = 9.1 nM) and to a lesser extent ABHD6 with potent selectivity over FAAH (IC50 > 10 μM) and other brain serine hydrolases. It can inhibit 2-AG hydrolysis (IC50 = 2.1 nM) with no effect on AEA hydrolysis up to 50 μM. At 5 mg/kg, MJN110 has been shown to alleviate mechanical allodynia in a rat model of diabetic neuropathy.[Cayman Chemical]

• Biochem/physiol Actions

  MJN110 is a potent selective inhibitor of MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) with >10,000 selectivity over FAAH, the hydrolase that degrades the endocannabinoid anandamide (AEA). MJN110 inhibits rat, mouse and human MAGL with IC50 values ranging from < 100 nM in rat to an IC50 of ~1 nM with 10- and 100-fold selectivity over closely related ABHD6, a serine hydrolase that acts as an alternative hydrolase of 2-AG, and LYPLA1/2 in human PC3 cells. MJN110 showed potent anti-hyperalgesic activity in a rat model of diabetic neuropathy, showing a therapeutic potential for treating diabetes chronic pain.

(2-ベンジルピペリジノ)[4-(2′-メトキシビフェニル-4-イル)-1H-1,2,3-トリアゾール-1-イル]ケトン 生産企業

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(2-ベンジルピペリジノ)[4-(2′-メトキシビフェニル-4-イル)-1H-1,2,3-トリアゾール-1-イル]ケトン スペクトルデータ(¹HNMR)