L-745870 trihydrochloride 是可透过血脑屏障的、选择性的、具有口服活性的多巴胺D4受体拮抗剂，Ki=0.43 nM，而对 D2(Ki为 960 nM) 和 D3(Ki为 2300 nM) 受体的亲和力相对较弱，对 5-HT2受体，sigma 位点和 α-肾上腺素受体表现出中等亲和力。

L-745870 trihydrochloride is a highly potent and selective D4 dopamine receptor antagonist. L-745870 trihydrochloride exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors and shows weaker affinity for D2 and D3 receptors.

L-745870 has favorable pharmacokinetic properties in both rats and monkeys, and shows excellent brain permeability and a high brain-to-plasma ratio in rats [1]. L-745870 (10 mg/kg p.o.) at 30 mg/kg caused mild sedation and extrapyramidal motor symptoms, especially bradykinesia, following oral administration to squirrel monkeys. Lower doses of L-745870 had no apparent behavioral effects in monkeys [1].

866021-03-6

C18H22Cl4N4

436.21

L-745,870 trihydrochloride;L-745870三盐酸盐

H2O:<40mg>Powder: -20°C for 3 years
In solvent: -80°C for 2 years