LE 300 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
LE300 is a dopamine D
1-like receptor antagonist (K
is = 1.9 and 7.5 nM in CHO cell membranes expressing human dopamine D
1 and D
5 receptors, respectively) and antagonist of the serotonin (5-HT) receptor subtype 5-HT
2A (pA
2 = 8.32 in a rat tail artery assay). It is selective for dopamine D
1 and D
5 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 (ED
50 = 0.94 mg/kg), which is predictive for antipsychotic-like activity. It also reduces locomotor activity in the open field test in rats (ED
50 = 0.74 mg/kg).
Verwenden
LE 300 is a potent and selective dopamine receptor antagonist.
Biologische Aktivit?t
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 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
