5-メチル-5,16-ジアザテトラシクロ[15.4.0.02,15.08,13]ヘニコサン-1(17),2(15),8,10,12,18,20-ヘプタエン

5-メチル-5,16-ジアザテトラシクロ[15.4.0.02,15.08,13]ヘニコサン-1(17),2(15),8,10,12,18,20-ヘプタエン 価格

5-メチル-5,16-ジアザテトラシクロ[15.4.0.02,15.08,13]ヘニコサン-1(17),2(15),8,10,12,18,20-ヘプタエン 化学特性,用途語,生産方法

• 説明

  LE300 is a dopamine D₁-like receptor antagonist (K_is = 1.9 and 7.5 nM in CHO cell membranes expressing human dopamine D₁ and D₅ receptors, respectively) and antagonist of the serotonin (5-HT) receptor subtype 5-HT_2A (pA₂ = 8.32 in a rat tail artery assay). It is selective for dopamine D₁ and D₅ over D_2L and D_4.4 receptors (K_is = 44.7 and 109 nM, respectively). LE300 inhibits the conditioned avoidance response in the pole-jump test in rats (ED₅₀ = 0.94 mg/kg), which is predictive for antipsychotic-like activity. It also reduces locomotor activity in the open field test in rats (ED₅₀ = 0.74 mg/kg).

• 使用

  LE 300 is a potent and selective dopamine receptor antagonist.

• 生物活性

  Potent and selective dopamine D 1 receptor antagonist (K i values are 0.08-1.9 nM and 6-45 nM for D 1 and D 2 receptors respectively). Also displays moderate affinity for the 5-HT 2A receptor (K i = 20 nM). Active in vivo .

5-メチル-5,16-ジアザテトラシクロ[15.4.0.02,15.08,13]ヘニコサン-1(17),2(15),8,10,12,18,20-ヘプタエン 生産企業

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274694-98-3, 5-メチル-5,16-ジアザテトラシクロ[15.4.0.02,15.08,13]ヘニコサン-1(17),2(15),8,10,12,18,20-ヘプタエン キーワード