LE 300

Description

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).

Uses

LE 300 is a potent and selective dopamine receptor antagonist.

Definition

ChEBI: LSM-2007 is a member of indoles.

Biological Activity

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 .

storage

Room temperature