L-745870 TriHydrochloride

L-745870 TriHydrochlorideCAS号: 866021-03-6分子式: C18H22Cl4N4分子量: 436.21描述储存/保存方法可溶性/溶解性靶点In vivo(体内研究)

产品描述
描述
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.
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
H2O:<40mg>
生物活性
靶点
D3 receptor:2300 nM (Ki), D2 receptor:960 nM (Ki), D4 Receptor:4.3 nM (Ki)
In vivo(体内研究)
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].