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

プロパティ

安全情報

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).