L-745870 Inhibitor

Solid. Powder

98.00%

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

326.82

<1mg/ml refers to the product slightly soluble or insoluble

C18H19ClN4

ClC(C=C1)=CC=C1N(CC2)CCN2CC3=CNC4=NC=CC=C43

158985-00-3

Human dopamine D4 receptor: ic50 0.43nM (ki)
Human dopamine D2 receptor: ic50 960nM (ki)
Human dopamine D3 receptor: ic50 2300nM (ki)

L-745870 has good pharmacokinetic properties (20-60% oral bioavailability and plasma t1/2 2.1-2.8 hours) in both rat and monkey, and excellent brain penetration with the high brain to plasma ratios in the rat. L-745870 has no effect on apomorphine-induced stereotypy in rats but does induce catalepsy in mice, albeit at a high dose of 100mg/kg p.o. that is likely to occupy D2 receptors in vivo. Evaluation of L-745870 in surrogate marker assays shows that this compound is freely available for biological activity in the brain and L-745870(5 to 60mg/kg; p.o.) treatment, would occupy 50% D4 receptors in the brain. Following oral administration to squirrel monkeys, L745870 (10mg/kg p.o.) causes mild sedation and extrapyramidal motor symptoms, notably bradykinesia became apparent at 30mg/kg. High doses of L-745870 might also be expected to induce extrapyramidal symptoms in primates because the levels in the CNS at these doses would be sufficient to antagonize D2 receptors. Lower doses of L-745870 has no observable behavioral effects in monkeys[1][2].

GPCR/G Protein; Dopamine Receptor; Neuroscience