LE 300

LE 300 화학적 특성, 용도, 생산

• 개요

  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).

• 용도

  LE 300 is a potent and selective dopamine receptor antagonist.

• 생물학적 활성

  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 .

LE 300 공급 업체

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